Arvin Dar: Publications

The Arvin Dar Lab

Arvin Dar: Publications


Marsiglia WM, Chow A, Khan ZM, He L, Dar A.C. Live-cell target engagement of allosteric MEKi on MEK-RAF/KSR-14-3-3 complexes. Nat Chem Biol. 2023 Nov 2. doi: 10.1038/s41589-023-01454-8. PMID: 37919548.

Rialdi A, Duffy M, Scopton AP, Fonseca F, Zhao JN, Schwarz M, Molina-Sanchez P, Mzoughi S, Arceci E, Abril-Fornaguera J, Meadows A, Ruiz de Galarreta M, Torre D, Reyes K, Lim YT, Rosemann F, Khan ZM, Mohammed K, Wang X, Yu X, Lakshmanan M, Rajarethinam R, Tan SY, Jin J, Villanueva A, Michailidis E, De Jong YP, Rice CM, Marazzi I, Hasson D, Llovet JM, Sobota RM, Lujambio A, Guccione E, Dar A.C. WNTinib is a multi-kinase inhibitor with specificity against β-catenin mutant hepatocellular carcinoma. Nat Cancer. 2023 Aug;4(8):1157-1175. doi: 10.1038/s43018-023-00609-9. PMID: 37537299.

Dar, A.C. and Brady, D.C. RASopathy mutations open new insights into the mechanism of BRAF activation. Preview, Molecular Cell. Nov 17, 2022 ;82(22):4192-4193. doi: 10.1016/j.molcel.2022.10.034.

Khan ZM, Real AM, Marsiglia WM, Chow A, Duffy ME, Yerabolu JR, Scopton AP, Dar A.C. Structural basis for the action of the drug trametinib at KSR-bound MEK. Nature. 2020 Dec;588(7838):509-514. doi: 10.1038/s41586-020-2760-4. PMID: 32927473.

Liu He and Dar, A.C. Targeting Drug-Resistance Mutations in ALK. News and Views, Nature Cancer. June 20, 2022; 3(6):659-661. doi: 10.1038/s43018-022-00390-1.

Schwarz, M., Torre, D., Lozano-Ojalvo, D., Tan, A., Tabaglio, T., Mzoughi, S. Sanchez-Tarjuelo, R.,…Marsiglia, W., Carreno, J., Dar, A.,…Bertoletti, A., Ochando, J., Guccione, E. A rapid and scalable PCR-based test to detect SARS-CoV-2 cellular immunity. Nature Biotechnology, 2022. 40(11):1680-1689. doi: 10.1038/s41587-022-01347-6. Epub 2022 Jun 13.

Brady, D.C., Hmeljak, J., Dar, A.C. Understanding and drugging RAS: 40 years to break the tip of the iceberg. Disease, Models, and Mechanisms. 2022. Feb 1;15(2):dmm049519. doi: 10.1242/dmm.049519. Epub 2022 Mar 4. 

Chow, A. Khan, Z., Marsiglia, W, Dar, A.C. Conformational control and regulation of the pseudokinase KSR via small molecule interactions. Methods in Enzymology. 2022;667:365-402. doi: 10.1016/bs.mie.2022.03.039. Epub 2022 Apr 25.

Smith, R.H.B., Khan, Z., Real, A., Mack, S., Man-Un Ung, P., Scopton, A.P., Silber, L., Schlessinger, A.*, and Dar, A.C.*. Type II Binders Targeting the ‘GLR-out’ Conformation of the Pseudokinase STRADa. Biochemistry, 2021. PMID 33440120.

Real, A.M., Marsiglia, W.M., and Dar, A.C. Ploidy Leads a Molecular Motor to Walk Different Paths to Drug Resistance. Cell Chem Bio. 2020. PMID 32679092.

Smith, R., Dar, A.C.*, Schlessinger, A.*. PyVOL: a PyMOL plugin for visualization, comparison and volume calculation for drug-binding sites. BioRxiv. 2019. Doi:

Jia Xin Yu, Amanda J. Craig, Mary E. Duffy, Carlos Villacorta Martin, Veronica Miguela, Marina Ruiz de Galarreta, Alexander P. Scopton, Lisa Silber, Andres Y. Maldonado, Alex Rialdi, Ernesto Guccione, Amaia Lujambio, Augusto Villanueva, and Arvin C. Dar. Phenotype-based screens with conformation-specific inhibitors reveal p38 gamma and delta as targets for HCC polypharmacology. Molecular Cancer Therapeutics. 2019. PMID 31213506.

Ung, PMU, Sonoshita, M., Scopton, A.P., Dar, A.C., Cagan, R.L., Schlessinger, A. Integrated computation and Drosophila cancer model platform captures previously unappreciated chemicals perturbing a kinase network. April 26, 2019.  Plos Comp. Bio. PMID: 31026276 

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. PMID: 31196969  

Masahiro Sonoshita*, Alex P. Scopton*, Peter M.-U. Ung, Matthew A. Murray, Lisa Silber, Andres Maldonado, Alex Real, Avner Schlessinger, Ross L. Cagan*, and Arvin C. Dar*. A Whole Animal Platform to Advance A Clinical Kinase Inhibitor Into New Disease Space. Nature Chemical Biology. Jan. 22, 2018. PMID: 29355849.

Neil Dhawan*, Alex P. Scopton*, and Arvin C. Dar. Small Molecule Stabilization of the KSR Inactive State Antagonizes Oncogenic Ras Signaling. Nature. 2016 Sep 1;537(7618):112-116. doi: 10.1038/nature19327. PMID: 27556948.

Levin VA, Tonge PJ, Gallo JM, Birtwistle MR, Dar A.C., 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:vi1-vi26. doi: 10.1093/neuonc/nov169. PubMed PMID: 26403167; PubMed Central PMCID: PMC4581696.

Mendez AS, Alfaro J, Morales-Soto MA, Dar A.C., 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. PMID: 25986605.

Israelow, B., Mullokandov, G., Agudo, J., Sourisseau, M., Bashir, A., Maldonado, A.Y., Dar, A.C., Brown, B.D., Evans, M.J. Hepatitis C virus genetics affects miR-122 requirements and response to miR-122 inhibitors. Nat. Commun. Nov. 5:5408. 2014. PMID: 25403145.

Dar, A.C. A Pickup in pseudokinase activity. Biochemical Society Transactions. Aug; 41(4): 987-94. 2013. PMID: 23863168. 

Zhang C, Lopez MS, Dar A.C., 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, A.C.*, Das, T.K.*, Shokat, K.M., Cagan, R.L. Chemical Genetic Discovery of Targets and Anti-targets for Cancer Polypharmacology. Nature, 486: 80-4. June 6, 2012.

Dar, A.C. and Shokat K.M. The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling.  Annual Reviews Biochem. Vol 80: 769-795, June 7, 2011.

Brennan, D.F.*, Dar, A.C.*, Hertz, N.T., Chao, W., Burlingame, A.L., Shokat, K.M., Barford, D. A RAF-induced allosteric transition of KSR stimulates phosphorylation of MEK. Nature. 472: 366-9, Apr. 21, 2011.

Hertz, N.T., Wang, B.T., Allen, J.J., Zhang, C., Dar, A.C., Burlingame, A.L., Shokat, K.M. Chemical Genetic Approach for Kinase-Substrate Mapping by Covalent Capture of Thiophosphopeptides and Analysis by Mass Spectrometry. Curr. Protoc. Chem. Biol. 2:15-36, 2010.

Dar, A.C., Lopez, M.S., Shokat, K.M. Small molecule recognition of c-Src via the Imatinib-binding conformation. Chemistry and Biology. Vol. 15, 1015-22, October 20, 2008. PMID: 18940662. 

Dar, A.C., Dever, T.E., Sicheri, F. Higher-order substrate recognition of eIF2a by the RNA-dependent protein kinase PKR. Cell. Vol.122, 887-900, September 23, 2005.