Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain:phosphotyrosine mimetics exploiting multifunctional group replacement chemistry.

Src inhibitors in the treatment of metastatic bone disease: rationale and clinical data. Clin Investig (Lond) (2011) 0.86

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

Genetic screens for Caenorhabditis elegans mutants defective in left/right asymmetric neuronal fate specification. Genetics (2007) 2.48

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

Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant. J Med Chem (2010) 1.82

Analysis of multiple ethyl methanesulfonate-mutagenized Caenorhabditis elegans strains by whole-genome sequencing. Genetics (2010) 1.76

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

Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol Cancer Ther (2011) 1.51

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

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

Distinct hsp70 domains mediate apoptosis-inducing factor release and nuclear accumulation. J Biol Chem (2006) 1.21

The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression. J Biol Chem (2008) 1.20

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

9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. J Med Chem (2009) 1.10

HSP72 attenuates renal tubular cell apoptosis and interstitial fibrosis in obstructive nephropathy. Am J Physiol Renal Physiol (2008) 1.10

Pharmacologically regulated Fas-mediated death of adoptively transferred T cells in a nonhuman primate model. Blood (2003) 1.06

Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: broad-spectrum antibacterial agents with reduced hERG activity. J Med Chem (2011) 1.05

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

Effects of asymptomatic proximal and distal gastroesophageal reflux on asthma severity. Am J Respir Crit Care Med (2009) 1.01

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

Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds. Chem Biol Drug Des (2006) 0.98

Identification of 4-substituted 1,2,3-triazoles as novel oxazolidinone antibacterial agents with reduced activity against monoamine oxidase A. J Med Chem (2005) 0.95

Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility. J Med Chem (2007) 0.93

Heat shock protein 72 enhances autophagy as a protective mechanism in lipopolysaccharide-induced peritonitis in rats. Am J Pathol (2011) 0.92

hsp72 inhibits focal adhesion kinase degradation in ATP-depleted renal epithelial cells. J Biol Chem (2003) 0.90

Inhibitors of hepatitis C virus polymerase: synthesis and characterization of novel 2-oxy-6-fluoro-N-((S)-1-hydroxy-3-phenylpropan-2-yl)-benzamides. Bioorg Med Chem Lett (2010) 0.90

Non-steroidal anti-inflammatory drugs-associated acute interstitial nephritis with granular tubular basement membrane deposits. Pediatr Nephrol (2007) 0.90

Regulation of bone remodeling and emerging breakthrough drugs for osteoporosis and osteolytic bone metastases. Kidney Int Suppl (2003) 0.90

gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists. Bioorg Med Chem Lett (2010) 0.88

Hsp72 interacts with paxillin and facilitates the reassembly of focal adhesions during recovery from ATP depletion. J Biol Chem (2004) 0.88

SRC homology-2 inhibitors: peptidomimetic and nonpeptide. Mini Rev Med Chem (2002) 0.87

Discovery and optimization of antibacterial AccC inhibitors. Bioorg Med Chem Lett (2009) 0.85

Exploring 8-benzyl pteridine-6,7-diones as inhibitors of glutamate racemase (MurI) in gram-positive bacteria. Bioorg Med Chem Lett (2008) 0.85

Hydrogen exchange-mass spectrometry measures stapled peptide conformational dynamics and predicts pharmacokinetic properties. Anal Chem (2013) 0.85

Targeting protein kinases for bone disease: discovery and development of Src inhibitors. Curr Pharm Des (2002) 0.85

Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template. Chem Biol Drug Des (2009) 0.82

SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity. Chem Biol Drug Des (2008) 0.82