Publications

• High-throughput protein target mapping enables accelerated bioactivity discovery for ToxCast and PFAS compounds.
  bioRxiv
  03/25/2025 Authors: Yang D; Wang X; Liu J; Gong Y; Nair P; Sun J; Qian X; Cui C; Zeng H; Dong A
• Enantioselective Protein Affinity Selection Mass Spectrometry (EAS-MS).
  bioRxiv
  01/22/2025 Authors: Wang X; Sun J; Ahmad S; Yang D; Li F; Chan UH; Zeng H; Simoben CV; Houliston S; Dong A
• Tilting the Scales toward EGFR Mutant Selectivity: Expanding the Scope of Bivalent "Type V" Kinase Inhibitors.
  J Med Chem Volume: 67 Page(s): 21438 - 21469
  12/12/2024 Authors: Wittlinger F; Chitnis SP; Pham CD; Damghani T; Patel KB; Mllers M; Schaeffner IK; Abidakun OA; Deng MQ; Ogboo BC
• Biochemical analysis of EGFR exon20 insertion variants insASV and insSVD and their inhibitor sensitivity.
  Proc Natl Acad Sci U S A Volume: 121 Page(s): e2417144121
  11/05/2024 Authors: Zhao H; Beyett TS; Jiang J; Rana JK; Schaeffner IK; Santana J; Jnne PA; Eck MJ
• Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality.
  ACS Cent Sci Volume: 10 Page(s): 1156 - 1166
  06/26/2024 Authors: Li Z; Jiang J; Ficarro SB; Beyett TS; To C; Tavares I; Zhu Y; Li J; Eck MJ; Jnne PA
• Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase.
  ChemMedChem Volume: 19 Page(s): e202300343
  06/17/2024 Authors: Beyett TS; Rana JK; Schaeffner IK; Heppner DE; Eck MJ
• ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases.
  J Med Chem Volume: 67 Page(s): 2837 - 2848
  02/22/2024 Authors: Li Z; Lu W; Beyett TS; Ficarro SB; Jiang J; Tse J; Kim AY-J; Marto JA; Che J; Jnne PA
• Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors.
  Commun Chem Volume: 7 Page(s): 38
  02/20/2024 Authors: Wittlinger F; Ogboo BC; Shevchenko E; Damghani T; Pham CD; Schaeffner IK; Oligny BT; Chitnis SP; Beyett TS; Rasch A
• A Constitutive EGFR Kinase Dimer to Study Inhibitor Pharmacology.
  Mol Pharmacol Volume: 105 Page(s): 97 - 103
  01/10/2024 Authors: Kim JJ; Schaeffner IK; Heppner DE; To C; Jnne PA; Beyett TS; Eck MJ
• Oncogenic K-Ras suppresses global miRNA function.
  Mol Cell Volume: 83 Page(s): 2509 - 2523.e13
  07/20/2023 Authors: Shui B; Beyett TS; Chen Z; Li X; La Rocca G; Gazlay WM; Eck MJ; Lau KS; Ventura A; Haigis KM
• Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib.
  J Biol Chem Volume: 299 Page(s): 104634
  05/01/2023 Authors: Tkacik E; Li K; Gonzalez-Del Pino G; Ha BH; Vinals J; Park E; Beyett TS; Eck MJ
• Structural elements that enable specificity for mutant EGFR kinase domains with next-generation small-molecule inhibitors.
  Volume: 685 Page(s): 171 - 198
  01/01/2023 Authors: Damghani T; Wittlinger F; Beyett TS; Eck MJ; Laufer SA; Heppner DE
• Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
  J Med Chem Volume: 65 Page(s): 15679 - 15697
  12/08/2022 Authors: Amrhein JA; Beyett TS; Feng WW; Krmer A; Weckesser J; Schaeffner IK; Rana JK; Jnne PA; Eck MJ; Knapp S
• Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).
  ACS Med Chem Lett Volume: 13 Page(s): 1856 - 1863
  12/08/2022 Authors: Heppner DE; Wittlinger F; Beyett TS; Shaurova T; Urul DA; Buckley B; Pham CD; Schaeffner IK; Yang B; Ogboo BC
• Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC.
  Bioorg Med Chem Lett Volume: 68 Page(s): 128718
  07/15/2022 Authors: Gero TW; Heppner DE; Beyett TS; To C; Azevedo SC; Jang J; Bunnell T; Feru F; Li Z; Shin BH
• Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors.
  Nat Commun Volume: 13 Page(s): 2530
  05/09/2022 Authors: Beyett TS; To C; Heppner DE; Rana JK; Schmoker AM; Jang J; De Clercq DJH; Gomez G; Scott DA; Gray NS
• A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer.
  Cancer Res Volume: 82 Page(s): 1633 - 1645
  04/15/2022 Authors: Son J; Jang J; Beyett TS; Eum Y; Haikala HM; Verano A; Lin M; Hatcher JM; Kwiatkowski NP; Eser P
• An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer.
  Nat Cancer Volume: 3 Page(s): 402 - 417
  04/01/2022 Authors: To C; Beyett TS; Jang J; Feng WW; Bahcall M; Haikala HM; Shin BH; Heppner DE; Rana JK; Leeper BA
• Biochemical characterization of the interaction between KRAS and Argonaute 2.
  Biochem Biophys Rep Volume: 29 Page(s): 101191
  03/01/2022 Authors: Waninger JJ; Beyett TS; Gadkari VV; Siebenaler RF; Kenum C; Shankar S; Ruotolo BT; Chinnaiyan AM; Tesmer JJG
• Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
  J Med Chem Volume: 65 Page(s): 1370 - 1383
  01/27/2022 Authors: Wittlinger F; Heppner DE; To C; Gnther M; Shin BH; Rana JK; Schmoker AM; Beyett TS; Berger LM; Berger B-T
• Comprehensive functional evaluation of variants of fibroblast growth factor receptor genes in cancer.
  NPJ Precis Oncol Volume: 5 Page(s): 66
  07/16/2021 Authors: Nakamura IT; Kohsaka S; Ikegami M; Ikeuchi H; Ueno T; Li K; Beyett TS; Koyama T; Shimizu T; Yamamoto N
• Characterization of a hyperphosphorylated variant of G protein-coupled receptor kinase 5 expressed in E. coli.
  Protein Expr Purif Volume: 168 Page(s): 105547
  04/01/2020 Authors: Beyett TS; Chen Q; Labudde EJ; Krampen J; Sharma PV; Tesmer JJG
• Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe.
  Proc Natl Acad Sci U S A Volume: 116 Page(s): 15895 - 15900
  08/06/2019 Authors: Beyett TS; Fraley AE; Labudde E; Patra D; Coleman RC; Eguchi A; Glukhova A; Chen Q; Williams RM; Koch WJ
• A driving test for oncogenic mutations.
  J Biol Chem Volume: 294 Page(s): 9390 - 9391
  06/14/2019 Authors: Heppner DE; Beyett TS; Eck MJ
• Synthesis of deuterium-labelled amlexanox and its metabolic stability against mouse, rat, and human microsomes.
  J Labelled Comp Radiopharm Volume: 62 Page(s): 202 - 208
  05/15/2019 Authors: Gan X; Wilson MW; Beyett TS; Wen B; Sun D; Larsen SD; Tesmer JJG; Saltiel AR; Showalter HD
• Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKK for the treatment of obesity.
  Bioorg Med Chem Volume: 26 Page(s): 5443 - 5461
  11/01/2018 Authors: Beyett TS; Gan X; Reilly SM; Gomez AV; Chang L; Tesmer JJG; Saltiel AR; Showalter HD
• Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKK and Reveal Mechanisms for Selective Inhibition.
  Mol Pharmacol Volume: 94 Page(s): 1210 - 1219
  10/01/2018 Authors: Beyett TS; Gan X; Reilly SM; Chang L; Gomez AV; Saltiel AR; Showalter HD; Tesmer JJG
• Navigating the conformational landscape of G protein-coupled receptor kinases during allosteric activation.
  J Biol Chem Volume: 292 Page(s): 16032 - 16043
  09/29/2017 Authors: Yao X-Q; Cato MC; Labudde E; Beyett TS; Tesmer JJG; Grant BJ