Publications
Aza-SAHA Derivatives Are Selective Histone Deacetylase 10 Chemical Probes That Inhibit Polyamine Deacetylation and Phenocopy HDAC10 Knockout. J Am Chem Soc. 144, 18861-18875
(2022) Biochemical and structural basis for differential inhibitor sensitivity of EGFR with distinct exon 19 mutations. Nat Commun. 13, 6791
(2022) Crystal Structure of the RNA Lariat Debranching Enzyme Dbr1 with Hydrolyzed Phosphorothioate RNA Product. Biochemistry. 10.1021/acs.biochem.2c00590
(2022) Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 65, 9678-9690
(2022) Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CL covalent inhibitors.. Eur J Med Chem. 229, 114046
(2022) Development of optimized drug-like small molecule inhibitors of the SARS-CoV-2 3CL protease for treatment of COVID-19. Nat Commun. 13, 1891
(2022) Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor. J Med Chem. 65, 3173-3192
(2022) DHX15 is involved in SUGP1-mediated RNA missplicing by mutant SF3B1 in cancer. Proc Natl Acad Sci U S A. 119, e2216712119
(2022) Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4. J Med Chem. 10.1021/acs.jmedchem.2c00509
(2022) Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4. J Med Chem. 10.1021/acs.jmedchem.2c00509
(2022) Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4. J Med Chem. 10.1021/acs.jmedchem.2c00509
(2022) Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 10.1021/acs.jmedchem.2c00552
(2022) Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 10.1021/acs.jmedchem.2c00552
(2022) Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.. J Med Chem. 10.1021/acs.jmedchem.2c01422
(2022) (2022) (2022) Epstein-Barr virus gH/gL has multiple sites of vulnerability for virus neutralization and fusion inhibition. Immunity. 55, 2135-2148.e6
(2022) Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. RSC Med Chem. 13, 1549-1564
(2022) Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of -Deleted Cancers.. J Med Chem. 10.1021/acs.jmedchem.1c01900
(2022) (2022) Identification of a novel deFADding activity in human, yeast and bacterial 5' to 3' exoribonucleases. Nucleic Acids Res. 50, 8807-8817
(2022) Identification of , an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.. J Med Chem. 10.1021/acs.jmedchem.2c00998
(2022) Kinetic and Structural Characterization of a Flavin-Dependent Putrescine -Hydroxylase from . Biochemistry. 61, 2607-2620
(2022) Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors. Nat Commun. 13, 2530
(2022) A novel allosteric site employs a conserved inhibition mechanism in human kidney-type glutaminase. FEBS J. 10.1111/febs.16658
(2022)