Article
Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127.
Science (New York, N.Y.) - 2 Feb 2024
Montoya Skye, Bourcier Jessie, Noviski Mark, Lu Hao, Thompson Meghan C, Chirino Alexandra, Jahn Jacob, Sondhi Anya K, Gajewski Stefan, Tan Ying Siow May, Yung Stephanie, Urban Aleksandra, Wang Eric, Han Cuijuan, Mi Xiaoli, Kim Won Jun, Sievers Quinlan, Auger Paul, Bousquet Hugo, Brathaban Nivetha, Bravo Brandon, Gessner Melissa, Guiducci Cristiana, Iuliano James N, Kane Tim, Mukerji Ratul, Reddy Panga Jaipal, Powers Janine, Sanchez Garcia de Los Rios Mateo, Ye Jordan, Barrientos Risso Carla, Tsai Daniel, Pardo Gabriel, Notti Ryan Q, Pardo Alejandro, Affer Maurizio, Nawaratne Vindhya, Totiger Tulasigeri M, Pena-Velasquez Camila, Rhodes Joanna M, Zelenetz Andrew D, Alencar Alvaro, Roeker Lindsey E, Mehta Sanjoy, Garippa Ralph, Linley Adam, Soni Rajesh Kumar, Skånland Sigrid S, Brown Robert J, Mato Anthony R, Hansen Gwenn M, Abdel-Wahab Omar, Taylor Justin
Abstract excerpt
Increasing use of covalent and noncovalent inhibitors of Bruton's tyrosine kinase (BTK) has elucidated a series of acquired drug-resistant BTK mutations in patients with B cell malignancies. Here we identify inhibitor resistance mutations in BTK with distinct enzymatic activities, including some that impair BTK enzymatic activity while imparting novel protein-protein interactions that sustain B cell receptor...
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