Detalhe da pesquisa
1.
Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation.
Nature
; 519(7541): 102-5, 2015 Mar 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-25686603
2.
Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation.
J Biol Chem
; 294(23): 9029-9036, 2019 06 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-31018963
3.
Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.
N Engl J Med
; 374(1): 54-61, 2016 Jan 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-26698910
4.
PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Proc Natl Acad Sci U S A
; 112(11): 3493-8, 2015 Mar 17.
Artigo
em Inglês
| MEDLINE | ID: mdl-25733882
5.
Acquired resistance to crizotinib from a mutation in CD74-ROS1.
N Engl J Med
; 368(25): 2395-401, 2013 Jun 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-23724914
6.
Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors.
Proc Natl Acad Sci U S A
; 109(45): 18281-9, 2012 Nov 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-22988103
7.
Design and Synthesis of Functionally Active 5-Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1.
J Med Chem
; 66(7): 4888-4909, 2023 04 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-36940470
8.
KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.
Proc Natl Acad Sci U S A
; 106(5): 1542-7, 2009 Feb 03.
Artigo
em Inglês
| MEDLINE | ID: mdl-19164557
9.
Analysis of lorlatinib analogs reveals a roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer.
Nat Cancer
; 3(6): 710-722, 2022 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-35726063
10.
SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance.
Mol Cancer Ther
; 21(1): 3-15, 2022 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-34737197
11.
Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.
J Med Chem
; 64(13): 9056-9077, 2021 07 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-34110834
12.
Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor.
Cancer Cell
; 39(10): 1404-1421.e11, 2021 10 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-34520734
13.
Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors.
Biochemistry
; 48(23): 5339-49, 2009 Jun 16.
Artigo
em Inglês
| MEDLINE | ID: mdl-19459657
14.
Characterizing the effects of the juxtamembrane domain on vascular endothelial growth factor receptor-2 enzymatic activity, autophosphorylation, and inhibition by axitinib.
Biochemistry
; 48(29): 7019-31, 2009 Jul 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-19526984
15.
Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3.
Clin Cancer Res
; 14(22): 7272-83, 2008 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19010843
16.
Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib.
ACS Med Chem Lett
; 9(9): 878-883, 2018 Sep 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-30258534
17.
Reviving B-Factors: Activating ALK Mutations Increase Protein Dynamics of the Unphosphorylated Kinase.
ACS Med Chem Lett
; 9(9): 872-877, 2018 Sep 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-30258533
18.
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
J Med Chem
; 57(11): 4720-44, 2014 Jun 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-24819116
19.
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
J Med Chem
; 57(4): 1170-87, 2014 Feb 27.
Artigo
em Inglês
| MEDLINE | ID: mdl-24432909
20.
Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats.
J Med Chem
; 56(17): 6651-65, 2013 Sep 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-23944843