Publications

Jin Lab Full Publication List

Dr. Jin Google Scholar Citations

Jin Lab Recent Publications

2019

Yu, X.; Huang, X. -P.; Kenakin, T.;  Slocum, S.; Chen, X.; Martini, M.; Liu, J.; Jin, J. Design, Synthesis and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). J. Med. Chem. 2019 Just Accepted.

Gao, Y.; Haren, M.; Moret, E. E.; Rood, J. J. M.; Sartini, D.; Salvucci, A.; Emanuelli, M.; Carveur, P.; Babault, N.; Jin, J.; Martin, N. I. Bisubstrate Inhibitors of Nicotinamide N- Methyltransferase (NNMT) with Enhanced Activity. J. Med. Chem. 2019 Just Accepted. DOI: https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00413

Xiong, Y.; Greschik, H.; Johansson, C.; Seifert, L.; Bacher, J.; Park, K. -S.; Babault, N.; Martini, M.; Fagan, V.; Li, F.; Chau, I.; Christott, T.; Dilworth, D.; Barsyte-Lovejoy, D.; Vedadi, M.; Arrowsmith, C.; Brennan, P.; Fedorov, O.; Jung, M.; Farnie, G.; Liu, J.; Oppermann, U.; Schüle, R.; Jin, J. Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). J. Med. Chem. 2019 Just accepted. DOI: https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00522

He, X.; Zhu, Y.; Lin, Y. -C.; Li, M.; Du, J.; Dong, H.; Sun, D. J.; Zhu, L.; Wang, H.; Ding, Z.; Zhang, Lei.; Zhang, Lianjun.; Zhao, D.; Wang, Z.; Wu, H.; Zhang, H.; Jiang, W.; Xu, Y.; Jin, J.; Shen, Y.; Perry, J.; Zhao, X.; Zhang, B.; Liu, S.; Xue, S. -L.; Shen, B.; Chen, C. -W.; Chen, J.; Khaled, S.; Kuo, Y. -H.; Marcucci, G.; Luo, Y.; Li, L. PRMT1-mediated FLT3 arginine methylation promotes maintenance of FLT3-ITD+ Acute Myeloid Leukemia. Blood 2019, just accepted. DOI: https://doi.org/10.1182/blood.2019001282

MacDonald, I. A.; Butler, K. V.; Herring, L. E.; Clinkscales, S. E.; Yelagandula, R.; Stecher, K.; Bell, O.; Graves, L. M.; Jin, J.; Hathaway, N. A. Pathway-Based High-Throughput Chemical Screen Identifies Compounds That Decouple Heterochromatin Transformations. SLAS DISCOVERY: Advancing Life Sciences R&D. May 2019. PMID:31145866, PMCID: in progress.

Chen, S.; Wiewiora, R. P.; Meng, F.; Babault, N.; Ma, A.; Yu, W.; Qian, K.; Hu, H.; Zou, H.; Wang, J.; Fan, S.; Blum, G.; Pittella-Silva, F.; Beauchamp, K. A.; Tempel, W.; Jiang, H.; Chen, K.; Skene, R. J.; Zheng, Y. G.; Brown, P. J.; Jin, J.; Luo, C.; Chodera, J. D.; Luo, M. The Dynamic Conformational Landscape of the Protein Methyltransferase SETD8. eLife 2019, 8, e45403. PMID : 31081496, PMCID: in progress.

MacNevin, C. J.; Watanabe, T.; Weitzman, M.; Gulyani, A.; Fuehrer, S.; Pinkin, N. K.; Tian, X.; Liu, F.; Jin, J.; Hahn, K. M. Membrane-permeant, environment-sensitive dyes generate biosensors within living cells. J. Am. Chem. Soc. 2019, 141, 18, 7275-7282. PMID:30994345, PMCID: in progress.

Shen, Y.; McCorvy, J. D.; Martini, M. L.; Rodriguiz, R. M.; Progorelov, V. M.; Ward, K. M.; Wetsel, W. C.; Liu, J.; Roth, B. L.; Jin, J. D2 Dopamine Receptor G protein-biased Partial Agonists Based on Cariprazine. J. Med. Chem. 2019, 62(9), 4755-4771. PMID:30964661, PMCID: PMC6509010.

Lima-Fernandes, E.; Murison, A.; Medina, T.S.; Wang, Y.; Ma, A.; Leung, C.; Luciani, G. M.; Haynes, J.; Pollett, A.; Zeller, C.; Duan, S.; Kreso, A.; Barsyte-Lovejoy, D.; Wouters, B. G.; Jin, J.; De Carvalho, D. D.; Lupien, M.; Arrowsmith, C. H.; O’Brien, C. A. Targeting bivalency de-represses Indian Hedgehog and inhibits self-renewal of colorectal cancer-initiating cells. Nat. Commun. 2019, 10(1), 1436. PMID: 30926792, PMCID : PMC6441108.

Martini, M. L.; Liu, J.; Ray, C.; Yu, X.; Huang, X –P.; Urs, A.; Urs, N. M.; McCorvy, J.; Caron, M. G.; Roth, B. L.; Jin, J. Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D1 Receptor Agonists. J. Med. Chem. 2019, 62(7), 3753-3772. PMID: 30875219, PMCID: in progress.

Kaniskan, H. Ü.; Jin J. Selective, Small-Molecule Inhibitors of Protein Methyltransferases. Epigenetic Drug Discovery, Second ed., Weinheim: VCH-Wiley 2019, 201-220.

Veo, B.; Danis, E.; Pierce, A.; Sola, I.; Wang, D.; Foreman, N. K.; Jin, J.; Ma, A.; Serkova, N.; Venkataraman, S.; Vibhakar, R. Combined functional genomic and chemical screens identify SETD8 as a therapeutic target in MYC-driven medulloblastoma. JCI Insight 2019, 4(1), e122933. PMID: 30626740, PMCID:PMC6485357.

Scheer, S.; Ackloo, S.; Medina, T. S.; Schapira, M.; Li, F.; Ward, J. A.; Lewis, A. M.; Northrop, J. P.; Richardson, P. L.; Kaniskan, H. Ü.; Shen, Y.; Liu, J.; Smil, D.; McLeod, D.; Zepeda-Velazquez, C. A.; Luo, M.; Jin, J.; Barsyte-Lovejoy, D.; Huber, K. V. M.; De Carvalho, D. D.; Vedadi, M.; Zaph, C.; Brown, P. J.; Arrowsmith, C. H.  A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat. Commun. 2019, 10, 19. PMID:30604761, PMCID:PMC6318333.

Allen, D. C.; Carlson, T. L.; Xiong, Y.; Jin, J.; Grant, K. A.; Cuzon Carlson, V. C.* A comparative study of the pharmacokinetics of clozapine N-oxide and clozapine N-oxide hydrochloride salt in rhesus macaques. Journal of Pharmacology and Experimental Therapeutics , , PMCID:PMC6337003

2018

Chiarella, A. M.; Wang, T. A.; Butler, K. V.; Jin, J.; Hathaway, N. A. Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers. J Vis Exp 2018, 139, e58222. PMID: 30295665, PMCID: PMC6235244

Zhao, N.; Sebastiano, V.; Moshkina, N.; Mena, N.; Hultquist, J.; Jimenez-Morales, D.; Ma, Y.; Rialdi, A.; Albrecht, R.; Fenouil, R.; Sánchez-Aparicio, M. T.; Ayllon, J.; Ravisankar, S.; Haddad, B.; Ho, J. S. Y.; Low, D.; Jin, J.; Yurchenko, V.; Prinjha, R. K.; Tarakhovsky, A.; Squatrito, M.; Pinto, D.; Allette, K.; Byun, M.; Smith, M. L.; Sebra, R.; Guccione, E.; Tumpey, T.; Krogan, N.; Greenbaum, B.; van Bakel, H.; García-Sastre, A.; Marazzi, I.* Influenza virus infection causes global RNAPII termination defects. Nature Structural & Molecular Biology 2018, 25, 885-893. PMID: 30177761,  PMCID: in progress.

McCorvy, J. D.*; Wacker, D.; Wang, S.; Agegnehu, B.; Liu, J.; Lansu, K.; Tribo, A. R.; Olsen, R. H. J.; Che, T.; Jin, J.; Roth, B. L.* Structural determinants of 5-HT2B receptor activation and biased agonism. Nature Structural & Molecular Biology 2018, 25, 787-796. PMID: 30127358,  PMCID: PMC6237183

Thompson, K. J.; Khajehali, E.; Bradley, S. J.; Navarrete, J. S.; Huang, X.-P.; Slocum, S.; Jin, J.; Liu, J.; Xiong, Y.; Olsen, R.; DiBerto, J.; Boyt, K. M.; Pina, M. M.; Pati, D.; Molloy, C.; Bundgaard, C.; Sexton, P. M.; Kash, T. L.; Krashes, M. J.; Christopoulos, A.; Roth, B. L.*; Tobin, A. B.* DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo ACS Pharmacology & Translational Science 2018, 1, 61-72. PMID:30868140, PMCID:PMC6407913

Pellock, S. J.; Creekmore, B. C.; Walton, W. G.; Mehta, N.; Biernat, K. A.; Cesmat, A. P.; Ariyarathna, Y.; Dunn, Z. D.; Li, B.; Jin, J.; James, L. I.; Redinbo, M. R.* Gut Microbial β-Glucuronidase Inhibition via Catalytic Cycle Interception. ACS Central Science 2018, 4, 868-879PMID:30062115, PMCID: PMC6062831

Zhang, C.; Han, X.-R.; Yang, X.; Jiang, B.; Liu, J.*; Xiong, Y.*; Jin, J.* Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). European Journal of Medicinal Chemistry 2018, 151, 304-314. PMID: 29627725,  PMCID: PMC5924614

Zhang, T.; Wu, J.; Ungvijanpunya, N.; Jackson-Weaver, O.; Gou, Y.; Feng, J.; Ho, T. V.; Shen, Y.; Liu, J.; Richard, S.; Jin, J.; Hajishengallis, G.; Chai, Y.; Xu, J.* Smad6 Methylation Represses NFκB Activation and Periodontal Inflammation. Journal of Dental Research 2018, 7, 810-819. PMID: 29420098, PMCID: in progress.

Wang, D.-y.; Kosowan, J.; Samsom, J.; Leung, L.; Zhang, K.-l.; Li, Y.-x.; Xiong, Y.; Jin, J.; Petronis, A.; Oh, G.; Wong, A. H. C.* Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice. Acta Pharmacologica Sinica 2018, 39, 866-874. PMID: 29417943,  PMCID: PMC5943902

Babault, N.; Allali-Hassani, A.; Li, F.; Fan, J.; Yue, A.; Ju, K.; Liu, F.*; Vedadi, M.*; Liu, J.*; Jin, J.* Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT). Journal of Medicinal Chemistry 2018, 61, 1541-1551. PMID: 29320176, PMCID: PMC5823789

Kaniskan, H. Ü.; Eram, M. S.; Zhao, K.; Szewczyk, M. M.; Yang, X.; Schmidt, K.; Luo, X.; Xiao, S.; Dai, M.; He, F.; Zang, I.; Lin, Y.; Li, F.; Dobrovetsky, E.; Smil, D.; Min, S.-J.; Lin-Jones, J.; Schapira, M.; Atadja, P.; Li, E.; Barsyte-Lovejoy, D.; Arrowsmith, C. H.; Brown, P. J.; Liu, F.*; Yu, Z.*; Vedadi, M.*; Jin, J.* Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). Journal of Medicinal Chemistry 2018, 61, 1204-1217. PMID: 29244490, PMCID: PMC5808361

Morini, M. F.; Giampietro, C.; Corada, M.; Pisati, F.; Lavarone, E.; Cunha, S. I.; Conze, L. L.; O’Reilly, N. J.; Joshi, D.; Kjaer, S.; George, R.; Nye, E.; Ma, A.; Jin, J.; Mitter, R.; Lupia, M.; Cavallaro, U.; Pasini, D.; Calado, D. P.; Dejana, E.*; Taddei, A.* VE-Cadherin-Mediated Epigenetic Regulation of Endothelial Gene Expression. Circulation Research 2018, 122, 231-245. PMID: 29233846, PMCID: PMC5771688

McCorvy, J. D.; Butler, K. V.; Kelly, B.; Rechsteiner, K.; Karpiak, J.; Betz, R. M.; Kormos, B. L.; Shoichet, B. K.; Dror, R. O.*; Jin, J.*; Roth, B. L.* Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs. Nature Chemical Biology 2018, 14, 126-134. PMID: 29227473, PMCID: PMC5771956

Butler, K. V.;  Chiarella, A. M.; Jin, J. *; Hathaway N. A.* Targeted Gene Repression Using Novel Bifunctional Molecules to Harness Endogenous Histone Deacetylation Activity ACS Synth. Biol. 2018, 7, 38-45. PMID: 29073761, PMCID: PMC5775041

Kaniskan, H. Ü.*; Martini, M. L.; Jin, J.* Inhibitors of Protein Methyltransferases and Demethylases. Chemical Reviews 2018, 118, 989-1068. PMID: 28338320, PMCID: PMC5610952

2017

Alzrigat, M.*; Párraga, A. A.; Majumder, M. M.; Ma, A.; Jin, J.; Österborg, A.; Nahi, H.; Nilsson, K.; Heckman, C. A.; Öberg, F.; Kalushkova A.; Jernberg-Wiklund H.* The polycomb group protein BMI-1 inhibitor PTC-209 is a potent anti-myeloma agent alone or in combination with epigenetic inhibitors targeting EZH2 and the BET bromodomains Oncotarget 20178, 103731–103743. PMID: 2829262596  PMCID: PMC5732762

Butler, K. V.; MacDonald, I. A.; Hathaway, N. A.; Jin, J.* Report And Application Of A Tool Compound Dataset. Journal of Chemical Information and Modeling 2017, 57, 2699–2706. PMID: 29035535  PMCID: PMC5705340

Xiong, Y.; Li, F.; Babault, N.; Wu, H.; Dong, A.; Zeng, H.; Chen, X.; Arrowsmith, C. H.; Brown, P. J.; Liu, J.; Vedadi, M.*; Jin, J.* Structure-Activity Relationship studies of G9a-Like protein (GLP) inhibitors. Bioorganic & Medicinal Chemistry 2017, 25, 4414-4423. PMID: 28662962  PMCID: PMC5562403

Kaniskan, H. Ü.*; Jin, J.* Recent progress in developing selective inhibitors of protein methyltransferases. Current Opinion in Chemical Biology 2017, 39, 100-108. PMID: 28662389  PMCID: PMC5624721

Rizq, O.; Mimura, N.*; Oshima, M.; Saraya, A.; Koide, S.; Kato, Y.; Aoyama, K.; Nakajima-Takagi, Y.; Wang, C.; Chiba, T.; Ma, A.; Jin, J.; Iseki, T.; Nakaseko, C.; Iwama, A.* Dual inhibition of EZH2 and EZH1 sensitizes PRC2-dependent tumors to proteasome inhibition. Clinical Cancer Research 2017,

Jain, R.; Butler, K. V.; Coloma, J.; Jin, J.; Aggarwal, A. K.* Development of a S-adenosylmethionine analog that intrudes the RNA-cap binding site of Zika methyltransferase. Scientific Reports 2017, 7, 1632. PMID: 28487506  PMCID: PMC5431627

Lansu, K.; Karpiak, J.; Liu, J.; Huang, X.-P.; McCorvy, J. D.; Kroeze, W. K.; Che, T.; Nagase, H.; Carroll, F. I.; Jin, J.; Shoichet, B. K.; Roth, B. L.* In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat. Chem. Biol. 2017, 13, 529-536. PMID: 28288109  PMCID: PMC5391270

Beak, J. Y.; Huang, W.; Parker, J. S.; Hicks, S. T.; Patterson, C.; Simpson, P. C.; Ma, A.; Jin, J.; Jensen, B. C.* An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity. JACC: Basic to Translational Science 2017, 2, 39-53. PMID: 28286875  PMCID: PMC5343290

Huang, Q.; He, S.; Tian, Y.; Gu, Y.; Chen, P.; Li, C.; Huang, J.; Liu, Y.; Yu, H.; Jin, M.; Hu, S.; Tong, Q.; Ma, A.; Jin, J.; Hexner, E.; Fung, H.; Reshef, R.; Zhang, Y.*; Zhang, Y.* Hsp90 inhibition destabilizes Ezh2 protein in alloreactive T cells and reduces graft-versus-host disease in mice. Blood 2017, . PMID:28246193  PMCID: PMC5437825

Xiong, Y.; Li, F.; Babault, N.; Dong, A.; Zeng, H.; Wu, H.; Chen, X.; Arrowsmith, C. H.; Brown, P. J.; Liu, J.; Vedadi, M.*; Jin, J.* Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. J. Med. Chem. 2017, 60, 1876-1891. PMID: 28135087  PMCID: PMC5352984

Veschi, V.; Liu, Z.; Voss, T. C.; Ozbun, L.; Gryder, B.; Yan, C.; Hu, Y.; Ma, A.; Jin, J.; Mazur, S. J.; Lam, N.; Souza, B. K.; Giannini, G.; Hager, G. L.; Arrowsmith, C. H.; Khan, J.; Appella, E.; Thiele, C. J.* Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma. Cancer Cell 2017, 31, 50-63. PMID: 28073004  PMCID: PMC5233415

Alzrigat, M.*; Párraga, A. A.; Agarwal, P.; Zureigat, H.; Österborg, A.; Nahi, H.; Ma, A.; Jin, J.; Nilsson, K.; Öberg, F.; Kalushkova, A.; Jernberg-Wiklund, H.* EZH2 inhibition in multiple myeloma downregulates myeloma associated oncogenes and upregulates microRNAs with potential tumor suppressor functions. Oncotarget 2017, 8, 10213-10224. PMID: 28052011  PMCID: PMC5354653

Kim, Y.; Lee, H.-M.; Xiong, Y.; Sciaky, N.; Hulbert, S. W.; Cao, X.; Everitt, J. I.; Jin, J.; Roth, B. L.*; Jiang, Y.-h.* Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. Nat. Med. 2017, 23, 213-222. PMID: 28024084  PMCID: PMC5589073

2016

Urs, N. M.; Gee, S. M.; Pack, T. F.; McCorvy, J. D.; Evron, T.; Snyder, J. C.; Yang, X.; Rodriguiz, R. M.; Borrelli, E.; Wetsel, W. C.; Jin, J.; Roth, B. L.; O’Donnell, P.; Caron, M. G.* Distinct cortical and striatal actions of a β-arrestin–biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties. Proceedings of the National Academy of Sciences 2016, 113, E8178-E8186. PMID: 27911814  PMCID: PMC5167191

Chen, X.; McCorvy, J. D.; Fischer, M. G.; Butler, K. V.; Shen, Y.; Roth, B. L.*; Jin, J.* Discovery of G Protein-biased D2 Dopamine Receptor Partial Agonists. J. Med. Chem. 2016, 59, 10601-10618. PMID: 27805392  PMCID: PMC5148701

Butler, K. V.; Ma, A.; Yu, W.; Li, F.; Tempel, W.; Babault, N.; Pittella-Silva, F.; Shao, J.; Wang, J.; Luo, M.; Vedadi, M.; Brown, P. J.; Arrowsmith, C. H.; Jin, J.* Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase. J. Med. Chem. 2016, 59, 9881-9889. PMID: 27804297  PMCID: PMC5148670

Shen, Y.; Szewczyk, M. M.; Eram, M. S.; Smil, D.; Kaniskan, H. Ü.; de Freitas, R. F.; Senisterra, G.; Li, F.; Schapira, M.; Brown, P. J.; Arrowsmith, C. H.; Barsyte-Lovejoy, D.; Liu, J.*; Vedadi, M.*; Jin, J.* Discovery of a Potent, Selective and Cell-active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J. Med. Chem. 2016, 59, 9124-9139. PMID: 27584694  PMCID: PMC5063716

Yang, X.; Li, F.; Konze, K. D.; Meslamani, J.; Ma, A.; Brown, P. J.; Zhou, M.-M.; Arrowsmith, C. H.; Kaniskan, H. Ü.; Vedadi, M.*; Jin, J.* Structure–Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors. J. Med. Chem. 2016, 59, 7617-7633. PMID: 27468126  PMCID: PMC5003625

Kaniskan, H. U.; Eram, M. S.; Liu, J.; Smil, D.; Martini, M. L.; Shen, Y.; Santhakumar, V.; Brown, P. J.; Arrowsmith, C. H.; Vedadi, M.*; Jin, J.* Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1). MedChemComm 2016, 7, 1793-1796. PMID: 28042453  PMCID: PMC5198778

Rialdi, A., Campisi, L., Zhao, N., Lagda, A. C., Pietzsch, C., Ho, J. S. Y., Martinez-Gil1, L., Fenouil, R., Chen, X., Edwards, M., Metreveli, G., Jordan, S., Peralta, Z., Munoz-Fontela, C., Bouvier, N., Merad, M., Jin, J., Weirauch, M., Heinz, S., Benner, C., van Bake, H., Basler, C., García-Sastre, A., Bukreyev, A., Marazzi, I.* “Topoisomerase 1 inhibition suppresses inflammatory genes and protects from death by inflammation” Science 2016, 352, aad7993. PMID: 27127234  PMCID: PMC5193222

Butler, K. V.;  Bohn, K.;  Hrycyna, C. A.*; Jin, J.* “Non-substrate based, small molecule inhibitors of the human isoprenylcysteine carboxyl methyltransferase” MedChemComm 2016, 7, 1016-1021. PMCID: PMC4990076

Wagner, T.; Greschik, H.; Burgahn, T.; Schmidtkunz, K.; Schott, A.-K.; McMillan, J.; Baranauskienė, L.; Xiong, Y.; Fedorov, O.; Jin, J.; Oppermann, U.; Matulis, D.; Schüle, R.; Jung, M*. “Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform” Nucleic Acids Research 2016, 44, e88. PMID: 26893353  PMCID: PMC4872087

Agarwal, P.; Alzrigat, M.; Párraga, A. A.; Enroth, S.; Singh, U.; Ungerstedt, J.; Österborg, A.; Brown, P. J.; Ma, A.; Jin, J.; Nilsson, K.; Öberg, F.; Kalushkova, A.*; Jernberg-Wiklund, H*. “Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target” Oncotarget 2016, 7, 6809-6823. PMID: 26755663  PMCID: PMC4872750

Eram, M. S.; Shen, Y.; Szewczyk, M.; Wu, H.; Senisterra, G.; Li, F.; Butler, K. V.; Kaniskan, H. Ü.; Speed, B. A.; dela Seña, C.; Dong, A.; Zeng, H.; Schapira, M.; Brown, P. J.; Arrowsmith, C. H.; Barsyte-Lovejoy, D.; Liu, J.*; Vedadi, M.*; Jin, J.* “A Potent, Selective and Cell-active Inhibitor of Human Type I Protein Arginine Methyltransferases” ACS Chemical Biology 2016, 11, 772-781. PMID: 26598975  PMCID: PMC4798913

Park, S. M.; Chen, M.; Schmerberg, C. M.; Dulman, R. S.; Rodriguiz, R. M.; Caron, M. G.; Jin, J.; Wetsel, W. C.* “Effects of [beta]-Arrestin-Biased Dopamine D2 Receptor Ligands on Schizophrenia-like Behavior in Hypoglutamatergic Mice” Neuropsychopharmacology 2016, 41, 704-715. PMID: 26129680  PMCID: PMC4707817

2015

Huang, X.-P.; Karpiak, J.; Kroeze, W. K.; Zhu, H.; Chen, X.; Moy, S. S.; Saddoris, K. A.; Nikolova, V. D.; Farrell, M. S.; Wang, S.; Mangano, T. J.; Deshpande, D. A.; Jiang, A.; Penn, R. B.; Jin, J.; Koller, B. H.; Kenakin, T.; Shoichet, B. K.*; Roth, B. L.* “Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65” Nature 2015, 527, 477-483. PMID: 26550826  PMCID: PMC4796946

Simon, J. M.; Parker, J. S.; Liu, F.; Rothbart, S. B.; Ait-Si-Ali, S.; Strahl, B. D.; Jin, J.; Davis, I. J.; Mosley, A. L.; Pattenden, S. G.* “A Role for Widely Interspaced Zinc Finger (WIZ) in Retention of the G9a Methyltransferase on Chromatin” Journal of Biological Chemistry, 2015, 290, 26088-26102. PMID: 26338712 PMCID: PMC4646261

Wallace, B. D.; Roberts, A. B.; Pollet, R. M.; Ingle, J. D.; Biernat, K.; Venkatesh, M.K.; Guthrie, L.; O’Neal, S. K.; Robinson, S. J.; Dollinger, M.; Figueroa, E.; McShane, S. R.; Jin, J.; Frye, S. V.; Zamboni, W. C.; Pepe-Ranney, C.; Mani, S.; Kelly, L.; Redinbo, M. R.* “Structure and Inhibition of Microbiome β-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity” Chemistry & Biology, 2015, 22, 1238-1249. PMID: 26364932 PMCID: PMC4575908

Arrowsmith, C. H.; Audia, J. E.; Austin, C.; Baell, J.; Bennett, J.; Blagg, J.; Bountra, C.; Brennan, P. E.; Brown, P. J.; Bunnage, M. E.; Buser-Doepner, C.; Campbell, R. M.; Carter, A. J.; Cohen, P.; Copeland, R. A.; Cravatt, B.; Dahlin, J. L.; Dhanak, D.; Edwards, A. M.; Frye, S. V.; Gray, N.; Grimshaw, C. E.; Hepworth, D.; Howe, T.; Huber, K. V. M.; Jin, J.; Knapp, S.; Kotz, J. D.; Kruger, R. G.; Lowe, D.; Mader, M. M.; Marsden, B.; Mueller-Fahrnow, A.; Muller, S.; O’Hagan, R. C.; Overington, J. P.; Owen, D. R.; Rosenberg, S. H.; Roth, B.; Ross, R.; Schapira, M.; Schreiber, S. L.; Shoichet, B.; Sundstrom, M.; Superti-Furga, G.; Taunton, J.; Toledo-Sherman, L.; Walpole, C.; Walters, M. A.; Willson, T. M.; Workman, P.; Young, R. N.; Zuercher, W. J. “The promise and peril of chemical probes” Nature Chemical Biology 2015, 11, 536-541. PMID: 26196764  PMCID: PMC4706458

Wang, L.; Xie, L.; Ramachandran, S.; Lee, Y.; Yan, Z.; Zhou, L.; Krajewski, K.; Liu, F.; Zhu, C.; Chen, David J.; Strahl, Brian D.; Jin, J.; Dokholyan, Nikolay V.*; Chen, X.* “Non-canonical Bromodomain within DNA-PKcs Promotes DNA Damage Response and Radioresistance through Recognizing an IR-Induced Acetyl-Lysine on H2AX” Chemistry & Biology 2015, 22, 849-861. PMID: 26119999  PMCID: PMC4695401

Xu, B.; Konze, K. D.; Jin, J.; Wang, G. G.* “Targeting EZH2 and PRC2 dependence as novel anti-cancer therapy” Experimental Hematology 2015, 43, 698-712. PMID: 26027790  PMCID: PMC4706459

Abou El Hassan, M.; Huang, K.; Eswara, M. B. K.; Zhao, M.; Song, L.; Yu, T.; Liu, Y.; Liu, J. C.; McCurdy, S.; Ma, A.; Wither, J.; Jin, J.; Zacksenhaus, E.; Wrana, J. L.; Bremner, R.* “Cancer Cells Hijack PRC2 to Modify Multiple Cytokine Pathways” PLoS ONE 2015, 10, e0126466. PMID: 26030458  PMCID: PMC4450877

Stuhlmiller, Timothy J.; Miller, Samantha M.; Zawistowski, Jon S.; Nakamura, K.; Beltran, Adriana S.; Duncan, James S.; Angus, Steven P.; Collins, Kyla A. L.; Granger, Deborah A.; Reuther, Rachel A.; Graves, Lee M.; Gomez, Shawn M.; Kuan, P.-F.; Parker, Joel S.; Chen, X.; Sciaky, N.; Carey, Lisa A.; Earp, H. S.; Jin, J.; Johnson, Gary L.* Inhibition of Lapatinib-Induced Kinome Reprogramming in ERBB2-Positive Breast Cancer by Targeting BET Family Bromodomains. Cell Reports 2015, 11, 390-404. PMID: 25865888  PMCID: PMC4408261

Kaniskan, H. Ü.; Szewczyk, M. M.; Yu, Z.; Eram, M. S.; Yang, X.; Schmidt, K.; Luo, X.; Dai, M.; He, F.; Zang, I.; Lin, Y.; Kennedy, S.; Li, F.; Dobrovetsky, E.; Dong, A.; Smil, D.; Min, S.-J.; Landon, M.; Lin-Jones, J.; Huang, X.-P.; Roth, B. L.; Schapira, M.; Atadja, P.; Barsyte-Lovejoy, D.; Arrowsmith, C. H.; Brown, P. J.; Zhao, K.*; Jin, J.*; Vedadi, M.* “A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)” Angewandte Chemie International Edition 2015, 54, 5166-5170. PMID: 25728001  PMCID: PMC4400258

Chen, X.; Choo, H.; Huang, X.-P.; Yang, X.; Stone, O.; Roth, B. L.*; Jin, J.* “The First Structure-activity Relationship Studies for Designer Receptors Exclusively Activated by Designer Drugs (DREADDs)” ACS Chemical Neuroscience 20156, 476-484. PMID: 25587888  PMCID: PMC4368042

Kaniskan, H. Ü.; Konze, K.D.; Jin, J.* “Selective Inhibitors of Protein Methyltransferases” J. Med. Chem. 2015, 58, 1596-1629. PMID: 25406853  PMCID: PMC4345896

Kaniskan, H. Ü.; Jin, J.* “Chemical Probes of Histone Lysine Methyltransferases” ACS Chem. Biol. 2015, 10, 40-50. PMID: 25423077  PMCID: PMC4301070

Xu, B.; On, D. M.; Ma, A.; Parton, T.; Konze, K.D.; Pattenden, S. G.; Allison, D.F.; Cai, L.; Rockowitz, S.; Liu, S.; Liu, Y.; Li, F.; Vedadi, M.; Frye, S. V.; Garcia, B. A.; Zheng, D.; Jin, J.; Wang, G. G.* “Selective Inhibition of EZH2 and EZH1 Enzymatic Activity by a Small Molecule Suppresses MLLrearranged Leukemia” Blood, 2015, 125, 346-357. PMID: 25395428  PMCID: PMC4287641

2014

Katona, B., Liu, Y., Ma, A., Jin, J., Hua, X.* “EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells” Cancer Biology & Therapy2014, 15, 1677-1687. PMID: 25535899  PMCID: PMC4622469

Liu, C.; Yu, Y.; Liu, F.; Wei, X.; Wrobel, J. A.; Gunawardena, H. P.; Zhou, L.; Jin, J.; Chen, X.* “A chromatin activity-based chemoproteomic approach reveals a transcriptional repressome for gene-specific silencing” Nature Communications, 2014, 5, 5733. PMID: 25502336  PMCID: PMC4360912

Ma, A.; Yu, W.; Xiong, Y.; Butler, K. V.; Brown, P. J.; Jin, J.* “Structure-activity Relationship Studies of SETD8 Inhibitors”  MedChemComm20145, 1892-1898. PMID: 25554733  PMCID: PMC4278651

Ma, A.; Yu, W.; Li, F.; Bleich, R. M.; Herold, J. M.; Butler, K. V.; Norris, J. L.; Korboukh, V.; Tripathy, A.; Janzen, W. P.; Arrowsmith, C. H.; Frye, S. V.; Vedadi, M.; Brown, P. J.; Jin, J.* “Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8” J. Med. Chem. 2014, 57, 6822-6833. PMID: 25032507  PMCID: PMC4136711

Sundriyal, S.; Malmquist, N. A.; Caron, J.;Blundell, S.; Liu, F.; Chen, X.; Srimongkolpithak, N.; Jin, J.; Charman, S. A.; Scherf, A.; Fuchter, M. J.* “Development of Diaminoquinazoline Histone Lysine Methyltransferase Inhibitors as Potent Blood-stage Anti-Malarial Compounds” ChemMedChem, 2014, 9, 2360-2373. PMID: 25044750  PMCID: PMC4177335

Wright, B. D.; Loo, L.; Street, S. E.; Ma, A.; Taylor-Blake, B.; Stashko, M.A.; Jin, J.; Janzen, W. P.; Frye, S. V.; Zylka, M. J.* “The Lipid Kinase PIP5K1C Regulates Pain Signaling and Sensitization” Neuron, 2014, 82, 836-847. PMID: 24853942  PMCID: PMC4074510

Konze, K. D.; Pattenden, S. G.; Liu, F.; Barsyte-Lovejoy, D.; Li, F.; Simon, J. M.; Davis, I. J.; Vedadi, M.; Jin, J.* “A Chemical Tool for in vitro and in vivo Precipitation of the Lysine Methyltransferase G9a” ChemMedChem, 20149, 549-553. (Cover storyPMID: 24443078  PMCID: PMC4005005

Lehnertz, B.; Pabst, C.; Su, L.; Miller, M.; Liu, F.; Yi, L.; Zhang, R.; Krosl, J.; Yung, E.; Kirschner, J.; Rosten, P.; Underhill, T. M.; Jin, J.; Hébert, J.; Sauvageau, G.; Humphries, R. K.; Rossi, F. M.* “The Methyltransferase G9a Regulates HoxA9-Dependent Transcription in AML” Genes & Development, 2014, 28, 317-327. PMID: 24532712  PMCID: PMC3937511

Zhou, B.; Damrauer, J. S.; Hadzic, T.; Jeong, Y.; Clark, K.; Fan, C.; Murphy, L.; Lee, C. Y.; Troester, M. A.; Miller, C. R.; Jin, J.; Darr, D.; Perou, C. M.; Levine, R.; Diehn, M.; Kim, W. Y. “Erythropoietin Promotes Breast Tumorigenesis Through Tumor Initiating Cell Self-renewal”, Journal of Clinical Investigation, 2014124, 553-563. PMID: 24435044  PMCID: PMC3904607

2013

Liu, F.; Barsyte-Lovejoy, D.; Li, F.; Xiong, Y.; Korboukh, V.; Huang, X. P.; Allali-Hassani, A.; Janzen, W. P.; Roth, B. L.; Frye, S. V.; Arrowsmith, C. H.; Brown, P. J.; Vedadi, M.; Jin, J.* “Discovery of an in vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP” J. Med. Chem. 201356, 8931-8942. PMID: 24102134  PMCID: PMC3880643

Konze, K. D.; Ma, A.; Li, F.; Barsyte-Lovejoy, D.; Parton, T.; MacNevin, C. J.; Liu, F.; Gao, C.; Huang, X. P.; Kuznetsova, E.; Rougie, M.; Jiang, A.; Pattenden, S. G.; Norris, J. L.; James, L. I.; Roth, B. L.; Brown, P. J.; Frye, S. V.; Arrowsmith, C. H.; Hahn, K. M.; Wang, G. G.; Vedadi, M.; Jin, J.* “An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1”, ACS Chemical Biology20138, 1324-1334. (the most read article since online publication on 4/8/2013PMID: 23614352  PMCID: PMC3773059

Liu, F.; Li, F.; Ma, A.; Dobrovetsky, E.; Dong, A.; Gao, C.; Korboukh, I.; Liu, J.; Smil, D.; Brown, P. J.; Frye, S. V.; Arrowsmith, C. H.; Schapira, M.; Vedadi, M.*; Jin, J.* “Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors” J. Med. Chem. 201356, 2110-2124. PMID: 23445220  PMCID: PMC4319713

James, L. I.; Barsyte-Lovejoy, D.; Zhong, N.; Krichevsky, L.; Korboukh, V. K.; Herold, J. M.; MacNevin, C. J.; Norris, J. L.; Sagum, C. A.; Tempel, W.; Marcon, E.; Guo, H.; Gao, C.; Huang, X.-P.; Duan, S.; Emili, A.; Greenblatt, J. F.; Kireev, D. B.; Jin, J.; Janzen, W. P.; Brown, P. J.; Bedford, M. T.; Arrowsmith, C. H.*; Frye, S. V.* “Discovery of a Chemical Probe for the L3MBTL3 Methyllysine Reader Domain” Nat. Chem. Biol. 20139, 184-191. PMID: 23292653  PMCID: PMC3577944

James, L. I.; Korboukh, V. K.; Krichevsky, L.; Baughman, B.; Herold, J. M.; Norris, J. L.; Jin, J.; Kireev, D. B.; Janzen, W. P.; Arrowsmith, C. H.; Frye, S. V.* “Small-Molecule Ligands of Methyl-Lysine Binding Proteins: Optimization of Selectivity for L3MBTL3” J. Med. Chem. 201356, 7358-7371. PMID: 24040942  PMCID: PMC3846386

Cooper, M. J.; Cox, N. J.; Zimmerman, E. I.; Dewar, B. J.; Duncan, J. S.; Whittle, M. C.; Nguyen, T. A.; Jones, L. S.; Roy, S. G.; Smalley, D. M.; Kuan, P. F.; Richards, K. L.; Christopherson, R. I.; Jin, J.; Frye, S. V.; Johnson, G. L.; Baldwin, A. S.; Graves; L. M.* “Application of Multiplexed Kinase Inhibitor Beads to Study Kinome Adaptations in Drug Resistant Leukemia” PLoS ONE20138, e66755. PMID: 23826126  PMCID: PMC3691232

Alam, M. R.; Ming, X.; Nakagawa, O.; Jin, J.; Juliano, R. L. “Covalent Conjugation of Oligonucleotides with Cell-Targeting Ligands” Bioorg. Med. Chem. 201321, 6217-6223. PMID: 23777829  PMCID: PMC3789861

Blancafort, P.*; Jin, J.; Frye, S. V. “Writing and Re-Writing the Epigenetic Code of Cancer Cells: From Engineered Proteins to Small Molecules” Mol Pharmacol 201383, 563-576. PMID: 23150486  PMCID: PMC3920093

2012

Chen, X.; Sassano, M. F.; Zheng, L.; Setola, V.; Chen, M.; Bai, X.; Frye, S. V.; Wetsel, W. C.; Roth, B. L.*; Jin, J.* “Structure-Functional Selectivity Relationship Studies of Beta-arrestin-biased Dopamine D2 Receptor Agonists” J. Med. Chem. 2012, 55, 7141-7153. PMID: 22845053  PMCID: PMC3443605

Korboukh, I.; Hull-Ryde, E. A.; Rittiner, J. E.; Randhawa, A. S.; Coleman, J.; Fitzpatrick, B. J.; Setola, V.; Janzen, W. P.; Frye, S. V.; Zylka, M. J.*; Jin, J.* “Orally Active Adenosine A1 Receptor Agonists with Antinociceptive Effects in Mice” Journal of Medicinal Chemistry 2012, 55, 6467-6477. (Highlighted by Pain Research ForumPMID: 22738238  PMCID: PMC3501123

Siarheyeva, A.; Senisterra, G.; Allali-Hassani, A.; Dong, A.; Dobrovetsky, E.; Wasney, Gregory A.; Chau, I.; Marcellus, R.; Hajian, T.; Liu, F.; Korboukh, I.; Smil, D.; Bolshan, Y.; Min, J.; Wu, H.; Zeng, H.; Loppnau, P.; Poda, G.; Griffin, C.; Aman, A.; Brown, Peter J.; Jin, J.; Al-awar, R.; Arrowsmith, Cheryl H.; Schapira, M.*; Vedadi, M.* “An Allosteric Inhibitor of Protein Arginine Methyltransferase 3” Structure 2012, 20, 1425-1435. PMID: 22795084

Roberts, P. J.; Usary, J. E.; Darr, D. B.; Dillon, P. M.; Pfefferle, A. D.; Whittle, M. C.; Duncan, J. S.; Johnson, S. M.; Combest, A. J.; Jin, J.; Zamboni, W. C.; Johnson, G. L.; Perou, C. M.*; Sharpless, N. E.* “Combined PI3K/mTOR and MEK Inhibition Provides Broad Anti-Tumor Activity in Faithful Murine Cancer Models” Clinical Cancer Research2012, 18, 5290-5303. PMID: 22872574  PMCID: PMC3715399

Duncan, J. S.; Whittle, M. C.; Nakamura, K.; Abell, A. N.; Midland, A. A.; Zawistowski, J. S.; Johnson, N. L.; Granger, D. A.; Jordan, N. V.; Darr, D. B.; Usary, J.; Kuan, P.-F.; Smalley, D. M.; Major, B.; He, X.; Hoadley, K.; Sharpless, N. E.; Perou, C. M.; Gomez, S. M.; Chen, X.; Jin, J.; Frye, S. V.; Earp, H. S.; Graves, L. M.; Johnson, G. L.* “Dynamic Reprogramming of the Kinome In Response to Targeted MEK Inhibition In Triple Negative Breast Cancer” Cell, 2012, 149, 307-321. (Highlighted by Faculty of 1000PMID: 22500798  PMCID: PMC3328787

Huang, H.-S.; Allen, J. A.; Mabb, A. M.; King, I. F.; Miriyala, J.; Taylor-Blake, B.; Sciaky, N.; Dutton Jr, J. W.; Lee, H.-M.; Chen, X.; Jin, J.; Bridges, A. S.; Zylka, M. J.*; Roth, B. L.*; Philpot, B. D.* “Topoisomerase Inhibitors Unsilence the Dormant Allele of Ube3a in Neurons” Nature, 2012, 481, 185-189. (Highlighted in Science, Nature, the Scientist, and many others and listed as one of top 10 Scientific Achievements of 2011 by NIMHPMID: 22190039  PMCID: PMC3257422

Rittiner, J. E.; Korboukh, I.; Hull-Ryde, E.; Jin, J.; Janzen, W. P.; Frye, S. V.; Zylka, M. J.* “AMP Is an Adenosine A1 Receptor Agonist” J. Bio. Chem. 2012, 287, 5301-5309. PMID: 22215671  PMCID: PMC3285310

Jin, Q.; Davis, R. S.; Bullion, A. M.; Jin, J.; Wang, Y.; Widdowson, K. L.; Palovich, M. R.; Foley, J. J.; Schmidt, D. B.; Buckley, P. T.; Webb, E. F.; Salmon, M.; Belmonte, K. E.; Sarau, H. M.; Busch-Petersen, J.* “Tyrosine Urea Muscarinic Acetylcholine Receptor Antagonists: Achiral Quaternary Ammonium Groups” Bioorg. Med. Chem. Lett. 2012, 22, 7087-7091. PMID: 23099092

Wang, X. F.; Tian, X. T.; Ohkoshi, E.; Qin, B.; Liu, Y. N.; Wu, P. C.; Hour, M. J.; Hung, H. Y.; Qian, K.; Huang, R.; Bastow, K. F.; Janzen, W. P.; Jin, J.; Morris-Natschke, S. L.; Lee, K. H.; Xie, L.* “Design and Synthesis of Diarylamines and Diarylethers as Cytotoxic Antitumor Agents”. Bioorg. Med. Chem. Lett. 2012, 22, 6224-6228. PMID: 22932313

Herold, J. M.; James, L. I.; Korboukh, V. K.; Gao, C.; Coil, K. E.; Bua, D. J.; Norris, J. L.; Kireev, D. B.; Brown, P. J.; Jin, J., Janzen, W. P.; Gozani, O.; Frye, S. V.*  “Structure-Activity Relationships of Methyl-Lysine Reader Antagonists” MedChemComm, 2012, 3, 45-51. PMID: N/A

He, Y.; Korboukh, I.; Jin, J.*; Huang, J.* “Targeting protein lysine methylation and demethylation in cancers” Acta Biochim Biophys Sin, 2012, 44, 70-79. PMID: 22194015  PMCID: PMC3244655

2011

Allen, J. A.; Yost, J. M.; Setola, V.; Chen, X.; Sassano, M. F.; Chen, M.; Peterson, S.; Yadav, P. N.; Huang, X.-P.; Feng, B.; Jensen, N. H.; Che, X.; Bai, X.; Frye, S. V.; Wetsel, W. C.; Caron, M. G.; Javitch, J. A.; Roth, B. L.*; Jin, J.* “Discovery of Beta-Arrestin-Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy” PNAS, 2011, 108, 18488-18493.  (highlighted by SciBX as a cover story (2011, 4(44), doi:10.1038/scibx.2011.1224), Schizophrenia Research Forum, and Faculty of 1000). PMID: 22025698  PMCID: PMC3215024

Vedadi, M.; Barsyte-Lovejoy, D.; Liu, F.; Rival-Gervier, S.; Allali-Hassani, A.; Labrie, V.; Wigle, T. J.; DiMaggio, P. A.; Wasney, G. A.; Siarheyeva, A.; Dong, A.; Tempel, W.; Wang, S.-C.; Chen, X.; Chau, I.; Mangano, T.; Huang, X.-P.; Simpson, C. D.; Pattenden, S. G.; Norris, J. L.; Kireev, D. B.; Tripathy, A.; Edwards, A.; Roth, B. L.; Janzen, W. P.; Garcia, B. A.; Petronis, A.; Ellis, J.; Brown, P. J.; Frye, S. V.; Arrowsmith, C. H.*; Jin, J.* “A Chemical Probe Selectively Inhibits G9a and GLP Methyltransferase Activity in Cells” Nature Chemical Biology, 2011, 7, 566-574. (Highlighted by News and Views in Nature Chemical Biology (2011, 7, 499-500), SciBX (2011, 4(31), doi:10.1038/scibx.2011.890). PMID: 21743462  PMCID: PMC3184254

Liu, F.; Barsyte-Lovejoy, D.; Allali-Hassani, A.; He, Y.; Herold, J. M.; Chen, X.; Yates, C. M.; Frye, S. V.; Brown, P. J.; Huang, J.; Vedadi, M.; Arrowsmith, C. H.; Jin, J.*  “Optimization of Cellular Activity of G9a Inhibitors 7-Aminoalkoxy-quinazolines” J. Med. Chem. 2011, 54, 6139-6150. PMID: 21780790  PMCID: PMC3171737

Morales-Ramos, A. I.*; Li, Y.; Hilfiker, M.; Mecom, J. S.; Eidam, P.; Shi, D.; Tseng, P.-S.; Brooks, C.; Zhang, D.; Wang, N.; Jaworski, J.; Morrow, D.; Fries, H.; Edwards, R. Jin, J.* “Structure-Activity Relationship Studies of Novel 3-Oxazolidinedione-6-Naphthyl-2-Pyridinones as Potent and Orally Bioavailable EP3 Receptor Antagonists” Bioorg. Med. Chem. Lett. 2011, 21, 2806-2811. PMID: 21514150

Yost, J. M.; Korboukh, I.; Liu, F.; Gao, C.; Jin, J.* “Targets in Epigenetics: Inhibiting the Methyl Writers of the Histone Code” Current Chemical Genomics, 2011, 5, 72-84. PMID: 21966347  PMCID: PMC3178896

Chen, X.; Jin, J.* book chapter “Small Molecule Inhibitors as Targeted Cancer Therapeutics” in The Molecular Basis of Human Cancer, Second Edition (Springer Press), 2011, in press. PMID: N/A

Herold, J. M.; Wigle, T. J.; Norris, J. L.; Lam, R.; Korboukh, V. K.; Gao, C.; Ingerman, L. A.; Kireev, D. B.; Senisterra, G.; Vedadi, M.;Tripathy, A.; Brown, P. J.; Arrowsmith, C. H.; Jin, J.; Janzen, W. P.; Frye, S. V.* “Small Molecule Ligands of Methyl-Lysine Binding Proteins” J. Med. Chem. 2011, 54, 2504-2511. PMID: 21417280  PMCID: PMC3109722

Evans, K, A.*; Shearer, B. G.; Wisnoski, D. D.; Shi, D.; Sparks, S. M.; Sternbach, D. D.; Winegar, D. A,; Billin, A. N.; Britt, C.; Way,J. M.; Epperly, A. H.; Leesnitzer, L. M.; Merrihew, R. V.; Xu, R. X.; Lambert, M. H.; Jin, J. “Phenoxyacetic Acids as PPARd Partial Agonists: Synthesis, Optimization, and In Vivo Efficacy” Bioorg. Med. Chem. Lett. 2011, 21, 2345-2350. PMID: 21414782

2010

Liu, F.; Chen, X.; Allali-Hassani, A.; Quinn, A. M.; Wigle, T. J.; Wasney, G. A.; Dong, A.; Senisterra, G.; Chau, I.; Siarheyeva, A.; Norris, J. L.; Kireev, D. B.; Jadhav, A.; Herold, J. M.; Janzen, W. P.; Arrowsmith, C. H.; Frye, S. V.; Brown, P. J.; Simeonov, A.; Vedadi, M.; Jin, J.*  “Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines” J. Med. Chem. 2010, 53, 5844-5857. PMID: 20614940  PMCID: PMC2920043

Jin, J.*; Morales-Ramos, A.; Eidam, P.; Mecom, J.; Li, Y.; Brooks, C.; Hilfiker, M.; Zhang, D.; Wang, N.; Shi, D.; Tseng, P.-S.; Wheless, K.; Budzik, B.; Evans, K.; Jaworski, J.; Jugus, J.; Leon, L.; Wu, C.; Pullen, M.; Karamshi, B.; Rao, P.; Ward, E.; Laping, N.; Evans, C.; Leach, C.; Holt, D.; Su, X.; Morrow, D.; Fries, H.; Thorneloe, K.; Edwards, R. “Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists” ACS Med. Chem. Lett. 2010, 1, 316-320. (Highlighted as a feature article in the October issuePMID: 24900213  PMCID: PMC4007852

Budzik, B.; Garzya, V.; Shi, D.; Walker, G.; Woolley-Roberts, M.; Pardoe, J.; Lucas, A. J.; Tehan, B.; Rivero, R. A.; Langmead, C. L.; Watson, J.; Wu, Z.; Forbes, I. T.; Jin, J.* “Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-penetrant, and Orally Active M1 mAChR Agonists” ACS Med. Chem. Lett. 2010, 1, 244-248. (Highlighted as a feature article in the September issuePMID: 24900202  PMCID: PMC4007837

Wigle, T. J.; Provencher, L. M.; Norris, J. L.; Jin, J.; Brown, P. J.; Frye, S. V.; Janzen, W. P.* “Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis” Chemistry & Biology 2010, 17, 695-704. (Cover storyPMID: 20659682  PMCID: PMC2914686

Johnson, S.; Torrice, C.; Bell, J.; Monahan, K.; Jiang, Q.; Wang, Y.; Ramsey, M.; Jin, J.; Wong, K.; Su, L.; Zhou, D.; Sharpless, N.* “Mitigation of hematologic radiation toxicity in mice through pharmacological quiescence induced by CDK4/6” Journal of Clinical Investigation 2010, 120, 2528–2536. PMID: 20577054  PMCID: PMC2898594

Frye, S. V.*; Heightman, T.; Jin, J. “Targeting Methyl Lysine” Annual Reports in Medicinal Chemistry 2010, 45, 329-343. PMID: N/A

Janzen, W. P.*; Wigle, T. J.; Jin, J.; Frye, S. V. “Epigenetics: Tools and Technologies” Drug Discovery Today: Technologies 2010, 7, e59-e65. PMID: 21243036  PMCID: PMC3018755

Li, Y. H.*; Tseng, P.-S.; Evans, K. A.; Jaworski, J.-P.; Morrow, D. M.; Fries, H. E.; Wu, C. W.; Edwards, R. M.; Jin, J.* “3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists” Bioorg. Med. Chem. Lett. 2010, 20, 6744-6747. PMID: 20926294

Budzik, B.; Garzya, V.; Shi, D.; Walker, G.; Lauchart, Y.; Lucas, A. J.; Rivero, R. A.; Langmead, C. L.; Watson, J.; Wu, Z.; Forbes, I. T.; Jin, J.* “2’ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling” Bioorg. Med. Chem. Lett. 2010, 20, 3545-3549. PMID: 20483599

Budzik, B.; Garzya, V.; Shi, D.; Foley, J. J.; Rivero, R. A.; Langmead, C. L.; Watson, J.; Wu, Z.; Forbes, I. T.; Jin, J.* “2’ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR” Bioorg. Med. Chem. Lett. 2010, 20, 3540-3544. PMID: 20483611

Budzik, B. W.; Evans, K, A.*; Wisnoski, D. D.; Jin, J.; Rivero, R. A.; Szewczyk, G. R.; Jayawickreme, C.; Moncol, D. L.; Yu, H. “Synthesis and Structure-activity Relationships of a Series of 3-Aryl-4-isoxazolecarboxamides as a New Class of TGR5 Agonists” Bioorg. Med. Chem. Lett. 2010, 20, 1363-1367. PMID: 20097073

2009

Liu, F.; Chen, X.; Allali-Hassani, A.; Quinn, A. M.; Wasney, G. A.; Dong, A.; Barsyte, D.; Kozieradzki, I.; Senisterra, G.; Chau, I.; Siarheyeva, A.; Kireev, D. B.; Jadhav, A.; Herold, J. M.; Frye, S. V.; Arrowsmith, C. H.; Brown, P. J.; Simeonov, A.; Vedadi, M.; Jin, J.* “Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a” J. Med. Chem. 2009, 52, 7950-7953. PMID: 19891491  PMCID: PMC2825141

Evans, K, A.*; Budzik, B. W.; Ross, S. A.; Wisnoski, D. D.; Jin, J.; Rivero, R. A.; Vimal, M.; Szewczyk, G. R.; Jayawickreme, C.; Moncol, D. L.; Rimele, T. J.; Armour, S. L.; Weaver, S. P.; Griffin, R. J.; Tadepalli, S. M.; Jeune, M. R.; Shearer, T. W.; Chen, Z. B.; Chen, L.; Hertzog, D. L.; Anderson, D. L.; Becherer, D.; De Los Frailes, M.; Colilla, F. J. “Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists” J. Med. Chem. 2009, 52, 7962-7965. PMID: 19902954

Jugus, M. J.; Jaworski, J. P.; Patra, P. B.; Jin, J.; Morrow, D. M.; Laping, N. J.; Edwards, R. M.; Thorneloe, K. S.* “Dual Modulation of Uninary Bladder Activity and Urine Flow by Prostanoid EP3 Receptors in the Conscious Rat” Br. J. Pharmacol. 2009, 158, 372-381. PMID: 19486006  PMCID: PMC2795235

Hilfiker, M. A.*; Wang, N.; Hou, X.; Du, Z.; Pullen, M. A.; Nord, M.; Nagilla, R.; Fries, H. E.; Wu, C. W.; Sulpizio, A. C.; Jaworski, J. P.; Morrow, D.; Edwards, R. M.; Jin, J. “Discovery of Novel Aminothiadiazole Amides as Selective EP3 Receptor Antagonists” Bioorg. Med. Chem. Lett. 2009, 19, 4292-4295. PMID: 19487124

Budzik, B. W.*; Wang, Y.*; Shi, D.; Wang, F.; Xie, H.; Wan, Z.; Zhu, C.; Foley, J. J.; Rao, P.; Kallal, L. A.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Laine, D. I.; Jin, J.* “M3 Muscarinic Acetylcholine Receptor Antagonists: SAR and Optimization of Bi-aryl Amines” Bioorg. Med. Chem. Lett. 2009, 19, 1686-1690. PMID: 19243945

Li, Y. H.*; Zhang, L.; Tseng, P. S.; Zhang, Y.; Jin, Y.; Shen, J. K.; Jin, J. “A Facile One-pot  Synthesis of 3-Unsubstituted-2,4-oxazolidinediones via in situ Generation of Carbamate From α-Hydroxyesters Using Trichloroacetyl Isocyanate” Tetrahedron Letters 2009, 50, 790-792. PMID: N/A

Wang, Y.*; Busch-Petersen, J.; Wang, F.; Kiesow T. J.; Graybill, T. L.; Jin, J.; Palovich, M.; Foley, J. J.; Hunsberger, G. E.; Schmidt, D. B.; Sarau, H. M.; Spudich, E. A.; Wu, Z.; Fisher, L. S.; McQueney, M. S.; Rivero, R. A.; Widdowson, K. L. “Camphor Sulfonamides and Derivatives as Novel, Potent and Selective CXCR3 Antagonists” Bioorg. Med. Chem. Lett. 2009, 19, 114-118. PMID: 19014886

2008

Jin, J.*; Budzik, B. W.; Wang, Y.; Shi, D.; Wang, F.; Xie, H.; Wan, Z.; Zhu, C.; Foley, J. J.; Webb, E. F.; Berlanga, M.; Burman, M.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Laine, D. I.* “Discovery of Bi-phenyl Piperazines as Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists” J. Med. Chem. 2008, 51, 5915-5918. PMID: 18798607

Jin, J.*; Wang, Y.; Shi, D.; Wang, F.; Davis, R. S.; Jin, Q.; Fu, W.; Foley, J. J.; Webb, E. F.; Dehaas, C. J.; Berlanga, M.; Burman, M.; Sarau, H. M.; Morrow, D. M.; Rao, P.; Kallal, L. A.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Busch-Petersen, J.* “Discovery of Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists” J. Med. Chem. 2008, 51, 4866-4869. PMID: 18680280

Su, X.*; Leon, L. A.; Wu, C. W.; Morrow, D. M.; Jaworski, J. P.; Heibler, J. P.; Lashinger, E. S. R.; Jin, J.; Edwards, R. M.; Laping, N. J. “Modulation of Bladder Function by Prostaglandin EP3 Receptors In the Central Nervous System” Am. J. Physiology – Renal Physiology 2008, 295, F984-F994. PMID: 18632791

Jin, J.*; Wang, Y.*; Shi, D.; Wang, F.; Fu, W.; Davis, R. S.; Jin, Q.; Foley, J. J.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Busch-Petersen, J. “Muscarinic Acetylcholine Receptor Antagonists: SAR and Optimization of Tyrosine Ureas” Bioorg. Med. Chem. Lett. 2008, 18, 5481-5486. PMID: 18818072

Wang, Y.*; Wu, Z.; Guida, B. F.; Lawrence, S. K.; Neeb, M. J.; Rivero, R. A.; Douglas, S. A.; Jin, J.*  “N-Alkyl-5H-pyrido[4,3-b]indol-1-amines and Derivatives as Novel Urotensin-II Receptor Antagonists” Bioorg. Med. Chem. Lett. 2008, 18, 4936-4939. PMID: 18768319

Jin, J.*; An, M.; Sapienza, A.; Aiyar, N. V.; Naselsky, D.; Sarau, H. M.; Foley, J. J.; Salyers, K. L.; Knight, S. D.; Keenan, R. M.; Rivero, R. A.; Dhanak, D.; Douglas, S. A. “Urotensin-II Receptor Antagonists: Synthesis and SAR of N-cyclic Azaalkyl Benzamides” Bioorg. Med. Chem. Lett. 2008, 18, 3950-3954. PMID: 18573659

McAtee, J. J.*; Dodson, J. W.; Dowdell, S. E.; Erhard, K. F.; Girard, G. R.; Goodman, K. B.; Hilfiker, M. A.; Jin, J.; Sehon, C. A.; Sha, D.; Shi, D.; Wang, F.; Wang, G. Z.; Wang, N.; Wang, Y.; Viet, A. Q.; Yuan, C. K.; Zhang, D.; Aiyar, N. V.; Behm, D. J.; Carballo, L. H.; Evans, C.; Fries, H. E.; Nagilla, R.; Roethke, T. J.; Xu, X.; Douglas, S. A.; Neeb, M. J. “Potent and Selective Small-Molecule Human Urotensin-II Antagonists with Improved Pharmacokinetic Profiles” Bioorg. Med. Chem. Lett. 2008, 18, 3716-3719. PMID: 18524591

Jin, J.*; Wang, Y.; Wang, F.; Shi, D.; Erhard, K. F.; Wu, Z.; Guida, B. F.; Lawrence, S. K.; Behm, D. J.; Disa, J.; Vaidya, K. S.; Evans, C.; McMillan, L. J.; Rivero, R. A.; Neeb, M. J.; Douglas, S. A. “2-Aminomethyl Piperidines as Novel Urotensin-II Receptor Antagonists” Bioorg. Med. Chem. Lett. 2008, 18, 2860-2864. PMID: 18420409