Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants.
Weisberg
Ellen
E
Department of Medical Oncology/Hematologic Neoplasia, Dana-Farber Cancer Institute, Boston, MA. Ellen_Weisberg@dfci.harvard.edu
Choi
Hwan Geun
HG
Ray
Arghya
A
Barrett
Rosemary
R
Zhang
Jianming
J
Sim
Taebo
T
Zhou
Wenjun
W
Seeliger
Markus
M
Cameron
Michael
M
Azam
Mohammed
M
Fletcher
Jonathan A
JA
Debiec-Rychter
Maria
M
Mayeda
Mark
M
Moreno
Daisy
D
Kung
Andrew L
AL
Janne
Pasi Antero
PA
Khosravi-Far
Roya
R
Melo
Junia V
JV
Manley
Paul W
PW
Adamia
Sophia
S
Wu
Catherine
C
Gray
Nathanael
N
Griffin
James D
JD
D019943:Amino Acid Substitution; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D001549:Benzamides; D045744:Cell Line, Tumor; D055808:Drug Discovery; D019008:Drug Resistance, Neoplasm / Q000235:genetics; D016044:Fusion Proteins, bcr-abl / Q000037:antagonists & inhibitors*; D006801:Humans; D000068877:Imatinib Mesylate; D066298:In Vitro Techniques; D015394:Molecular Structure; D050505:Mutant Proteins / Q000037:antagonists & inhibitors*; D020125:Mutation, Missense; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D019009:Proto-Oncogene Proteins c-kit / Q000037:antagonists & inhibitors*; D011743:Pyrimidines / Q000494:pharmacology; D020796:Receptor, Platelet-Derived Growth Factor alpha / Q000037:antagonists & inhibitors*; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*; D013912:Threonine / Q000235:genetics; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D001549:Benzamides; C552521:HG-7-85-01 compound; D050505:Mutant Proteins; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D013844:Thiazoles; D013912:Threonine; D000068877:Imatinib Mesylate; D019009:Proto-Oncogene Proteins c-kit; D020796:Receptor, Platelet-Derived Growth Factor alpha; D016044:Fusion Proteins, bcr-abl; D019061:src-Family Kinases