Disabling Uncompetitive Inhibition of Oncogenic IDH Mutations Drives Acquired Resistance.
Cancer Discovery
Lyu, Junhua J; Liu, Yuxuan Y; Gong, Lihu L; Chen, Mingyi M; Madanat, Yazan F YF; Zhang, Yuannyu Y; Cai, Feng F; Gu, Zhimin Z; Cao, Hui H; Kaphle, Pranita P; Kim, Yoon Jung YJ; Kalkan, Fatma N FN; Stephens, Helen H; Dickerson, Kathryn E KE; Ni, Min M; Chen, Weina W; Patel, Prapti P; Mims, Alice S AS; Borate, Uma U; Burd, Amy A; Cai, Sheng F SF; Yin, C Cameron CC; You, M James MJ; Chung, Stephen S SS; Collins, Robert H RH; DeBerardinis, Ralph J RJ; Liu, Xin X; Xu, Jian J
Secondary IDH1 resistance mutations and oncogenic IDH2 mutations cause acquired resistance to ivosidenib in cholangiocarcinoma.
Npj Precision Oncology
Cleary, James M JM; Rouaisnel, Betty B; Daina, Antoine A; Raghavan, Srivatsan S; Roller, Lauren A LA; Huffman, Brandon M BM; Singh, Harshabad H; Wen, Patrick Y PY; Bardeesy, Nabeel N; Zoete, Vincent V; Wolpin, Brian M BM; Losman, Julie-Aurore JA
Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors.
Nature Communications
Reinbold, Raphael R; Hvinden, Ingvild C IC; Rabe, Patrick P; Herold, Ryan A RA; Finch, Alina A; Wood, James J; Morgan, Melissa M; Staudt, Maximillian M; Clifton, Ian J IJ; Armstrong, Fraser A FA; McCullagh, James S O JSO; Redmond, Jo J; Bardella, Chiara C; Abboud, Martine I MI; Schofield, Christopher J CJ
Molecular mechanisms mediating relapse following ivosidenib monotherapy in IDH1-mutant relapsed or refractory AML.
Blood Advances
Choe, Sung S; Wang, Hongfang H; DiNardo, Courtney D CD; Stein, Eytan M EM; de Botton, Stéphane S; Roboz, Gail J GJ; Altman, Jessica K JK; Mims, Alice S AS; Watts, Justin M JM; Pollyea, Daniel A DA; Fathi, Amir T AT; Tallman, Martin S MS; Kantarjian, Hagop M HM; Stone, Richard M RM; Quek, Lynn L; Konteatis, Zenon Z; Dang, Lenny L; Nicolay, Brandon B; Nejad, Parham P; Liu, Guowen G; Zhang, Vickie V; Liu, Hua H; Goldwasser, Meredith M; Liu, Wei W; Marks, Kevin K; Bowden, Chris C; Biller, Scott A SA; Attar, Eyal C EC; Wu, Bin B
Acquired resistance to IDH inhibition through trans or cis dimer-interface mutations.
Nature
Intlekofer, Andrew M AM; Shih, Alan H AH; Wang, Bo B; Nazir, Abbas A; Rustenburg, Ariën S AS; Albanese, Steven K SK; Patel, Minal M; Famulare, Christopher C; Correa, Fabian M FM; Takemoto, Naofumi N; Durani, Vidushi V; Liu, Hui H; Taylor, Justin J; Farnoud, Noushin N; Papaemmanuil, Elli E; Cross, Justin R JR; Tallman, Martin S MS; Arcila, Maria E ME; Roshal, Mikhail M; Petsko, Gregory A GA; Wu, Bin B; Choe, Sung S; Konteatis, Zenon D ZD; Biller, Scott A SA; Chodera, John D JD; Thompson, Craig B CB; Levine, Ross L RL; Stein, Eytan M EM