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S. Malek · SciRah

Researcher profile · Semantic Scholar

S. Malek

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S. Malek — researcher profile on SciRah

h-index: 35
Works: 106
Citations: 7,338

Most-cited papers

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
G. Hatzivassiliou, Kyung Song, Ivana Yen, B. Brandhuber +17 more
2010Nature1,611 citations
Semantic Scholar
RAS-targeted therapies: is the undruggable drugged?
Amanda R. Moore, S. Rosenberg, F. McCormick, S. Malek
2020Nature reviews. Drug discovery940 citations Open access
Semantic Scholar
Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity
T. Maurer, L. Garrenton, A. Oh, Keith E Pitts +16 more
2012Proceedings of the National Academy of Sciences of the United States of America585 citations Open access
Semantic Scholar
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
G. Hatzivassiliou, Jacob R. Haling, Hui-Fen Chen, Kyung Song +17 more
2013Nature302 citations
Semantic Scholar
Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.
A. Boudreau, Hans E. Purkey, A. Hitz, K. Robarge +31 more
2016Nature Chemical Biology264 citations Open access
Semantic Scholar
Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling.
Jacob R. Haling, J. Sudhamsu, Ivana Yen, S. Sideris +11 more
2014Cancer Cell215 citations Open access
Semantic Scholar
Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2.
S. A. Foster, D. Whalen, A. Özen, M. Wongchenko +17 more
2016Cancer Cell187 citations Open access
Semantic Scholar
IκBβ, but Not IκBα, Functions as a Classical Cytoplasmic Inhibitor of NF-κB Dimers by Masking Both NF-κB Nuclear Localization Sequences in Resting Cells*
S. Malek, Yi Chen, T. Huxford, G. Ghosh
2001Journal of Biological Chemistry158 citations Open access
Semantic Scholar
Mechanism of κB DNA binding by Rel/NF-κB dimers*
C. Phelps, L. L. Sengchanthalangsy, S. Malek, G. Ghosh
2000Journal of Biological Chemistry117 citations Open access
Semantic Scholar
X-ray Crystal Structure of an IκBβ·NF-κB p65 Homodimer Complex*
S. Malek, De-Bin Huang, T. Huxford, S. Ghosh +1 more
2003Journal of Biological Chemistry114 citations Open access
Semantic Scholar
ARAF mutations confer resistance to the RAF inhibitor belvarafenib in melanoma
Ivana Yen, Frances Shanahan, Jeeyun Lee, Yong S. Hong +35 more
2021Nature112 citations Open access
Semantic Scholar
RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy
Kyung Song, K. Edgar, Emily J. Hanan, M. Hafner +23 more
2021bioRxiv98 citations Open access
Semantic Scholar
Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.
P. Dragovich, Ben Fauber, L. Corson, Charles Z. Ding +20 more
2013Bioorganic & Medicinal Chemistry Letters91 citations Open access
Semantic Scholar
Non-Covalent Wild-Type-Sparing Inhibitors of EGFR T790M
Ho-June Lee, G. Schaefer, T. Heffron, Lily Shao +11 more
2012Cancer Discovery87 citations Open access
Semantic Scholar
Negative regulation of RAF kinase activity by ATP is overcome by 14-3-3-induced dimerization
Nicholas P. D. Liau, T. Wendorff, J. Quinn, M. Steffek +9 more
2020Nature Structural & Molecular Biology78 citations
Semantic Scholar
IkappaBbeta, but not IkappaBalpha, functions as a classical cytoplasmic inhibitor of NF-kappaB dimers by masking both NF-kappaB nuclear localization sequences in resting cells.
S. Malek, Y. Chen, T. Huxford, G. Ghosh
2001Journal of Biological Chemistry74 citations
Semantic Scholar
Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors.
Ivana Yen, Frances Shanahan, M. Merchant, C. Orr +16 more
2018Cancer Cell71 citations Open access
Semantic Scholar
Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90.
Joerg Bussenius, Charles M. Blazey, N. Aay, N. Anand +33 more
2012Bioorganic & Medicinal Chemistry Letters69 citations Open access
Semantic Scholar
Targeting the MAPK Pathway in RAS Mutant Cancers.
S. Hymowitz, S. Malek
2018Cold Spring Harbor Perspectives in Medicine65 citations Open access
Semantic Scholar
Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase.
Ben Fauber, P. Dragovich, Jinhua Chen, L. Corson +17 more
2013Bioorganic & Medicinal Chemistry Letters60 citations Open access
Semantic Scholar
Identification of Preferred Chemotherapeutics for Combining with a CHK1 Inhibitor
Yang Xiao, J. Ramiscal, Katarzyna Kowanetz, Chris DelNagro +5 more
2013Molecular Cancer Therapeutics57 citations
Semantic Scholar
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.
Hans E. Purkey, K. Robarge, Jinhua Chen, Zhongguo Chen +29 more
2016ACS Medicinal Chemistry Letters54 citations Open access
Semantic Scholar
Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation
Emily J. Hanan, C. Eigenbrot, M. Bryan, D. Burdick +21 more
2014Journal of Medicinal Chemistry54 citations Open access
Semantic Scholar
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
R. Heald, K. Bowman, M. Bryan, D. Burdick +27 more
2015Journal of Medicinal Chemistry52 citations Open access
Semantic Scholar
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
P. Dragovich, Ben Fauber, J. Boggs, Jinhua Chen +28 more
2014Bioorganic & Medicinal Chemistry Letters45 citations Open access
Semantic Scholar
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.
Z. Pei, E. Blackwood, Li-Chuan Liu, S. Malek +26 more
2013ACS Medicinal Chemistry Letters45 citations Open access
Semantic Scholar
Identifying transcriptional programs underlying cancer drug response with TraCe-seq
Matthew T. Chang, Frances Shanahan, Thi Thu Thao Nguyen, S. Staben +11 more
2021Nature Biotechnology41 citations
Semantic Scholar
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Emily J. Hanan, M. Baumgardner, M. Bryan, Yuan Chen +12 more
2016Bioorganic & Medicinal Chemistry Letters41 citations Open access
Semantic Scholar
CRAF dimerization with ARAF regulates KRAS-driven tumor growth.
Avinashnarayan Venkatanarayan, Jason Liang, Ivana Yen, Frances Shanahan +19 more
2022Cell Reports38 citations Open access
Semantic Scholar
Mechanism of kappa B DNA binding by Rel/NF-kappa B dimers.
C. Phelps, L. L. Sengchanthalangsy, S. Malek, G. Ghosh
2000Journal of Biological Chemistry37 citations
Semantic Scholar
Combination Drug Scheduling Defines a “Window of Opportunity” for Chemopotentiation of Gemcitabine by an Orally Bioavailable, Selective ChK1 Inhibitor, GNE-900
E. Blackwood, J. Epler, Ivana Yen, Michael Flagella +16 more
2013Molecular Cancer Therapeutics34 citations
Semantic Scholar
Emerging Trends in Cancer Drug Discovery-From Drugging the "Undruggable" to Overcoming Resistance.
J. Rudolph, J. Settleman, S. Malek
2021Cancer Discovery31 citations Open access
Semantic Scholar
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
M. Bryan, D. Burdick, Bryan K. Chan, Yuan Chen +20 more
2016ACS Medicinal Chemistry Letters31 citations Open access
Semantic Scholar
A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.
Wendy B. K. Lee, D. Ortwine, Philippe Bergeron, K. Lau +8 more
2013Bioorganic & Medicinal Chemistry Letters30 citations Open access
Semantic Scholar
Dimerization induced by C-terminal 14-3-3 binding is sufficient for BRAF kinase activation.
Nicholas P. D. Liau, Avinashnarayan Venkatanarayan, J. Quinn, Wilson Phung +3 more
2020Biochemistry29 citations
Semantic Scholar
Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).
Anthony A. Estrada, D. Shore, E. Blackwood, Yung-Hsiang Chen +16 more
2013Journal of Medicinal Chemistry29 citations Open access
Semantic Scholar
Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.
Michael F. T. Koehler, Philippe Bergeron, E. Blackwood, K. Bowman +19 more
2012Journal of Medicinal Chemistry26 citations Open access
Semantic Scholar
Machine learning and chemico-genomics approach defines and predicts cross-talk of Hippo and MAPK pathways.
Trang Pham, Thijs J. Hagenbeek, Ho-June Lee, Jason Li +14 more
2020Cancer Discovery25 citations
Semantic Scholar
Author Correction: RAS-targeted therapies: is the undruggable drugged?
Amanda R. Moore, S. Rosenberg, F. McCormick, S. Malek
2020Nature reviews. Drug discovery24 citations Open access
Semantic Scholar
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.
Bryan K. Chan, Emily J. Hanan, K. Bowman, M. Bryan +25 more
2016Journal of Medicinal Chemistry24 citations Open access
Semantic Scholar
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
Malcolm P. Huestis, Darlene Dela Cruz, A. DiPasquale, M. Durk +20 more
2021Journal of Medicinal Chemistry23 citations Open access
Semantic Scholar
RAS-targeted therapies.
Amanda R. Moore, S. Rosenberg, F. McCormick, S. Malek
2021Nature reviews. Drug discovery23 citations
Semantic Scholar
Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.
F. Cohen, Philippe Bergeron, E. Blackwood, K. Bowman +19 more
2011Journal of Medicinal Chemistry23 citations Open access
Semantic Scholar
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
S. Labadie, P. Dragovich, Jinhua Chen, Ben Fauber +23 more
2015Bioorganic & Medicinal Chemistry Letters21 citations Open access
Semantic Scholar
Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.
Ben Fauber, P. Dragovich, Jinhua Chen, L. Corson +13 more
2014Bioorganic & Medicinal Chemistry Letters21 citations Open access
Semantic Scholar
Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.
Lewis Gazzard, B. Appleton, K. Chapman, Hui-Fen Chen +12 more
2014Bioorganic & Medicinal Chemistry Letters18 citations Open access
Semantic Scholar
Preparation and Crystallization of Dynamic NF-κB·IκB Complexes*
T. Huxford, S. Malek, G. Ghosh
2000Journal of Biological Chemistry18 citations Open access
Semantic Scholar
Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
Lewis Gazzard, Karen Williams, Hui-Fen Chen, Lorraine C. Axford +28 more
2015Journal of Medicinal Chemistry16 citations Open access
Semantic Scholar
Ternary complex dissociation kinetics contribute to mutant-selective EGFR degradation.
S. Rosenberg, Frances Shanahan, Sayumi Yamazoe, M. Kschonsak +12 more
2023Cell Chemical Biology15 citations Open access
Semantic Scholar
The promise and peril of KRAS G12C inhibitors.
Amanda R. Moore, S. Malek
2021Cancer Cell12 citations Open access
Semantic Scholar

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M. Merchant — researcher profile on SciRah

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S. Labadie — researcher profile on SciRah