Publications

Smith RHB, Khan ZM, Ung PM, Scopton AP, Silber L, Mack SM, Real AM, Schlessinger A, Dar AC. Type II Binders Targeting the “GLR-Out” Conformation of the Pseudokinase STRADα. Biochemistry. 2021 Feb 2;60(4):289-302.

Khan ZM, Real AM, Marsiglia WM, Chow A, Duffy ME, Yerabolu JR, Scopton AP, Dar AC. Structural basis for the action of the drug trametinib at KSR-bound MEK. Nature. 2020 Dec;588(7838):509-514.

Smith RH, Dar AC, Schlessinger A. PyVOL: a PyMOL plugin for visualization, comparison, and volume calculations of drug-binding sites. bioRxiv2019 October.

Real AM, Marsiglia WM, Dar AC. Ploidy Leads a Molecular Motor to Walk Different Paths to Drug Resistance. Cell Chem Biol. 2020 Jul 16;27(7):770-772.

Yu JX, Craig AJ, Duffy ME, Villacorta-Martin C, Miguela V, Ruiz de Galarreta M, Scopton AP, Silber L, Maldonado AY, Rialdi A, Guccione E, Lujambio A, Villanueva A, Dar AC. Phenotype-Based Screens with Conformation-Specific Inhibitors Reveal p38 Gamma and Delta as Targets for HCC Polypharmacology. Mol Cancer Ther. 2019 Sep;18(9):1506-1519.

Huang KL, Wu Y, Primeau T, Wang YT, Gao Y, McMichael JF, Scott AD, Cao S, Wendl MC, Johnson KJ, Ruggles K, Held J, Payne SH, Davies S, Dar A, Kinsinger CR, Mesri M, Rodriguez H, Ellis MJ, Townsend RR, Chen F, Fenyö D, Li S, Liu T, Carr SA, Ding L. Regulated Phosphosignaling Associated with Breast Cancer Subtypes and Druggability. Mol Cell Proteomics. 2019 Aug;18(8):1630-1650.

Ung PMU, Sonoshita M, Scopton AP, Dar AC, Cagan RL, Schlessinger A. Integrated computational and Drosophila cancer model platform captures previously unappreciated chemicals perturbing a kinase network. PLoS Comput Biol. 2019 Apr 26;15(4):e1006878.

Sonoshita M, Scopton AP, Ung PMU, Murray MA, Silber L, Maldonado AY, Real A, Schlessinger A, Cagan RL, Dar AC. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat Chem Biol. 2018 Mar;14(3):291-298.

Levin VA, Abrey LE, Heffron TP, Tonge PJ, Dar AC, Weiss WA, Gallo JM. CNS Anticancer Drug Discovery and Development: 2016 conference insights. CNS Oncol. 2017 Jul;6(3):167-177.

Dhawan NS, Scopton AP, Dar AC. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116.

Levin VA, Tonge PJ, Gallo JM, Birtwistle MR, Dar AC, Iavarone A, Paddison PJ, Heffron TP, Elmquist WF, Lachowicz JE, Johnson TW, White FM, Sul J, Smith QR, Shen W, Sarkaria JN, Samala R, Wen PY, Berry DA, Petter RC. CNS Anticancer Drug Discovery and Development Conference White Paper. Neuro Oncol. 2015 Nov;17 Suppl 6(Suppl 6):vi1-26.

Mendez AS, Alfaro J, Morales-Soto MA, Dar AC, McCullagh E, Gotthardt K, Li H, Acosta-Alvear D, Sidrauski C, Korennykh AV, Bernales S, Shokat KM, Walter P. Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic. Elife. 2015 May 19;4:e05434.

Israelow B, Mullokandov G, Agudo J, Sourisseau M, Bashir A, Maldonado AY, Dar AC, Brown BD, Evans MJ. Hepatitis C virus genetics affects miR-122 requirements and response to miR-122 inhibitors. Nat Commun. 2014 Nov 18;5:5408.

Dar AC. A pickup in pseudokinase activity. Biochem Soc Trans. 2013 Aug;41(4):987-94.

Zhang C, Lopez MS, Dar AC, Ladow E, Finkbeiner S, Yun CH, Eck MJ, Shokat KM. Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology. ACS Chem Biol. 2013 Sep 20;8(9):1931-8.

Dar AC, Das TK, Shokat KM, Cagan RL. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature. 2012 Jun 6;486(7401):80-4.

Brennan DF, Dar AC, Hertz NT, Chao WC, Burlingame AL, Shokat KM, Barford D. A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK. Nature. 2011 Apr 21;472(7343):366-9.

Dar AC, Shokat KM. The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling. Annu Rev Biochem. 2011;80:769-95.

Hertz NT, Wang BT, Allen JJ, Zhang C, Dar AC, Burlingame AL, Shokat KM. Chemical genetic approach for kinase-substrate mapping by covalent capture of thiophosphopeptides and analysis by mass spectrometry. Curr Protoc Chem Biol. 2010 Mar 1;2(1):15-36.

Seo EJ, Liu F, Kawagishi-Kobayashi M, Ung TL, Cao C, Dar AC, Sicheri F, Dever TE. Protein kinase PKR mutants resistant to the poxvirus pseudosubstrate K3L protein. Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):16894-9.

Dar AC, Lopez MS, Shokat KM. Small molecule recognition of c-Src via the Imatinib-binding conformation. Chem Biol. 2008 Oct 20;15(10):1015-22.

Dar AC, Dever TE, Sicheri F. Higher-order substrate recognition of eIF2alpha by the RNA-dependent protein kinase PKR. Cell. 2005 Sep 23;122(6):887-900.

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