Published in Chem Biol Drug Des on November 05, 2009
A combinatorial in silico and cellular approach to identify a new class of compounds that target VEGFR2 receptor tyrosine kinase activity and angiogenesis. Br J Pharmacol (2012) 0.86
Indolinones and anilinophthalazines differentially target VEGF-A- and basic fibroblast growth factor-mediated responses in primary human endothelial cells. Br J Pharmacol (2012) 0.82
Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src. ACS Chem Biol (2013) 0.80
Moving Beyond Active-Site Detection: MixMD Applied to Allosteric Systems. J Phys Chem B (2016) 0.75
Ponatinib in refractory Philadelphia chromosome-positive leukemias. N Engl J Med (2012) 6.99
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell (2009) 6.97
Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A (2011) 3.97
Characterization of susceptibility of inbred mouse strains to diabetic nephropathy. Diabetes (2005) 2.67
Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML. Blood (2004) 2.61
Phase II study of the mammalian target of rapamycin inhibitor ridaforolimus in patients with advanced bone and soft tissue sarcomas. J Clin Oncol (2011) 2.46
Stapled α-helical peptide drug development: a potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy. Proc Natl Acad Sci U S A (2013) 2.22
Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance. Chem Biol Drug Des (2010) 2.19
Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models. Mol Cancer Ther (2012) 2.05
Long-term pharmacologically regulated expression of erythropoietin in primates following AAV-mediated gene transfer. Blood (2004) 1.83
Catalytic asymmetric reductive coupling of alkynes and aldehydes: enantioselective synthesis of allylic alcohols and alpha-hydroxy ketones. J Am Chem Soc (2003) 1.81
Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen. Chem Biol Drug Des (2011) 1.68
Crystal structure of the T315I mutant of AbI kinase. Chem Biol Drug Des (2007) 1.60
Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD. Blood (2013) 1.52
Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol Cancer Ther (2011) 1.51
Crystal structure of an inactive Akt2 kinase domain. Structure (2003) 1.48
Identification of Src-specific phosphorylation site on focal adhesion kinase: dissection of the role of Src SH2 and catalytic functions and their consequences for tumor cell behavior. Cancer Res (2005) 1.45
Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma. Cancer Res (2006) 1.38
Targeting the BCR-ABL signaling pathway in therapy-resistant Philadelphia chromosome-positive leukemia. Clin Cancer Res (2010) 1.32
Dimerizer-regulated gene expression. Curr Opin Biotechnol (2002) 1.32
Probing the alpha-helical structural stability of stapled p53 peptides: molecular dynamics simulations and analysis. Chem Biol Drug Des (2010) 1.31
Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proc Natl Acad Sci U S A (2006) 1.30
Ridaforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens. Mol Cancer Ther (2011) 1.25
Distinct hsp70 domains mediate apoptosis-inducing factor release and nuclear accumulation. J Biol Chem (2006) 1.21
AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther (2005) 1.13
Pharmacologically regulated in vivo selection in a large animal. Blood (2002) 1.12
HSP72 attenuates renal tubular cell apoptosis and interstitial fibrosis in obstructive nephropathy. Am J Physiol Renal Physiol (2008) 1.10
9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. J Med Chem (2009) 1.10
Regulation of endogenous gene expression with a small-molecule dimerizer. Nat Biotechnol (2002) 1.08
Pharmacological regulation of protein expression from adeno-associated viral vectors in the eye. Mol Ther (2002) 1.07
Long-term inducible gene expression in the eye via adeno-associated virus gene transfer in nonhuman primates. Hum Gene Ther (2005) 1.07
Pharmacologically regulated Fas-mediated death of adoptively transferred T cells in a nonhuman primate model. Blood (2003) 1.06
Ponatinib in patients with refractory acute myeloid leukaemia: findings from a phase 1 study. Br J Haematol (2013) 1.04
Benzimidazole/amine-based compounds capable of ambipolar transport for application in single-layer blue-emitting OLEDs and as hosts for phosphorescent emitters. Angew Chem Int Ed Engl (2008) 1.04
Src activation of Stat3 is an independent requirement from NF-kappaB activation for constitutive IL-8 expression in human pancreatic adenocarcinoma cells. Angiogenesis (2006) 1.03
p53-dependent BRCA1 nuclear export controls cellular susceptibility to DNA damage. Cancer Res (2011) 1.03
HSP72 inhibits apoptosis-inducing factor release in ATP-depleted renal epithelial cells. Am J Physiol Cell Physiol (2003) 1.02
Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors. J Med Chem (2013) 1.01
Angiotensin type 1 receptor blocker restores podocyte potential to promote glomerular endothelial cell growth. J Am Soc Nephrol (2006) 1.01
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors. Bioorg Med Chem Lett (2008) 1.00
HSP72 inhibits Smad3 activation and nuclear translocation in renal epithelial-to-mesenchymal transition. J Am Soc Nephrol (2010) 0.99
SRC inhibitors in metastatic bone disease. Clin Cancer Res (2006) 0.99