Published in Bioorg Med Chem Lett on August 05, 2002
Molecular dynamics analysis of a series of 22 potential farnesyltransferase substrates containing a CaaX-motif. J Mol Model (2012) 0.77
How to Target Activated Ras Proteins: Direct Inhibition vs. Induced Mislocalization. Mini Rev Med Chem (2016) 0.76
Breast tumor cells with PI3K mutation or HER2 amplification are selectively addicted to Akt signaling. PLoS One (2008) 4.12
Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. Biochem J (2005) 3.58
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A proprotein convertase subtilisin/kexin type 9 neutralizing antibody reduces serum cholesterol in mice and nonhuman primates. Proc Natl Acad Sci U S A (2009) 3.39
Lung cancer cell lines harboring MET gene amplification are dependent on Met for growth and survival. Cancer Res (2007) 3.20
Comparative genomics of Vibrio cholerae from Haiti, Asia, and Africa. Emerg Infect Dis (2011) 2.50
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. J Med Chem (2004) 2.46
Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. Mol Cancer Ther (2005) 2.23
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorg Med Chem Lett (2006) 2.17
Induction of apoptosis by an inhibitor of the mitotic kinesin KSP requires both activation of the spindle assembly checkpoint and mitotic slippage. Cancer Cell (2005) 2.16
Novel mechanism of resistance to oxazolidinones, macrolides, and chloramphenicol in ribosomal protein L4 of the pneumococcus. Antimicrob Agents Chemother (2005) 2.14
An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo. Cancer Biol Ther (2010) 1.77
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. J Med Chem (2010) 1.76
MK-1775, a novel Wee1 kinase inhibitor, radiosensitizes p53-defective human tumor cells. Clin Cancer Res (2011) 1.59
Inhibition of a mitotic motor protein: where, how, and conformational consequences. J Mol Biol (2004) 1.58
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett (2008) 1.44
Characterization of Notch1 antibodies that inhibit signaling of both normal and mutated Notch1 receptors. PLoS One (2010) 1.41
Comparison of bacterial community structure and dynamics during the thermophilic composting of different types of solid wastes: anaerobic digestion residue, pig manure and chicken manure. Microb Biotechnol (2014) 1.40
DLK1-DIO3 genomic imprinted microRNA cluster at 14q32.2 defines a stemlike subtype of hepatocellular carcinoma associated with poor survival. J Biol Chem (2011) 1.40
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A biochemical rationale for the anticancer effects of Hsp90 inhibitors: slow, tight binding inhibition by geldanamycin and its analogues. Proc Natl Acad Sci U S A (2006) 1.38
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Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist. J Med Chem (2008) 1.28
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. Bioorg Med Chem Lett (2005) 1.27
Evaluation of efficacy, biodistribution, and inflammation for a potent siRNA nanoparticle: effect of dexamethasone co-treatment. Mol Ther (2009) 1.25
RNA interference-mediated silencing of mitotic kinesin KIF14 disrupts cell cycle progression and induces cytokinesis failure. Mol Cell Biol (2006) 1.23
Cotreatment with vorinostat enhances activity of MK-0457 (VX-680) against acute and chronic myelogenous leukemia cells. Clin Cancer Res (2008) 1.23
Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators. Bioorg Med Chem Lett (2009) 1.22
MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res (2010) 1.20
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett (2005) 1.19
microRNA-203 suppresses bladder cancer development by repressing bcl-w expression. FEBS J (2011) 1.17
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates. J Pharmacol Exp Ther (2008) 1.16
In vitro evaluation of the antimicrobial activity of ceftaroline against cephalosporin-resistant isolates of Streptococcus pneumoniae. Antimicrob Agents Chemother (2008) 1.16
Glycoengineered Pichia produced anti-HER2 is comparable to trastuzumab in preclinical study. MAbs (2011) 1.08
An inhibitor of the kinesin spindle protein activates the intrinsic apoptotic pathway independently of p53 and de novo protein synthesis. Mol Cell Biol (2006) 1.08
Genotypic and demographic characterization of invasive isolates of Salmonella Typhimurium in HIV co-infected patients in South Africa. J Infect Dev Ctries (2009) 1.06
An outbreak of foodborne salmonellosis in rural KwaZulu-Natal, South Africa. Foodborne Pathog Dis (2011) 1.04
Fluoroquinolone-resistant typhoid, South Africa. Emerg Infect Dis (2010) 1.04
Quantitative evaluation of siRNA delivery in vivo. RNA (2010) 1.03
Ductal adenocarcinoma of the prostate: immunohistochemical findings and clinical significance. Onco Targets Ther (2013) 1.03
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. J Med Chem (2008) 1.03
Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators. Bioorg Med Chem Lett (2010) 0.99
Discovery and biochemical characterization of selective ATP competitive inhibitors of the human mitotic kinesin KSP. Arch Biochem Biophys (2007) 0.99
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity. Bioorg Med Chem Lett (2007) 0.98
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand. Bioorg Med Chem Lett (2006) 0.97
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine. Bioorg Med Chem Lett (2006) 0.96
Noninvasive imaging of lipid nanoparticle-mediated systemic delivery of small-interfering RNA to the liver. Mol Ther (2010) 0.96
Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series. Bioorg Med Chem Lett (2011) 0.96
Mechanistically probing lipid-siRNA nanoparticle-associated toxicities identifies Jak inhibitors effective in mitigating multifaceted toxic responses. Mol Ther (2010) 0.95
Meningococcal disease in South Africa, 1999-2002. Emerg Infect Dis (2007) 0.95
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors. Bioorg Med Chem Lett (2008) 0.95
Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding. Bioorg Med Chem Lett (2009) 0.94
Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. ChemMedChem (2012) 0.94
Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther (2002) 0.94
Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold. J Med Chem (2011) 0.93
Germline mutations in the von Hippel-Lindau disease (VHL) gene in mainland Chinese families. J Cancer Res Clin Oncol (2008) 0.93
EGFR-dependent downregulation of Bim in epithelial cells requires MAPK and PKC-delta activities. Cancer Biol Ther (2006) 0.93
Hypoxia-induced downregulation of miR-30c promotes epithelial-mesenchymal transition in human renal cell carcinoma. Cancer Sci (2013) 0.92
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther (2010) 0.92
Protease inhibitors as potential disease-modifying therapeutics for Alzheimer's disease. Expert Opin Investig Drugs (2005) 0.92
Knowledge of human papillomavirus (HPV) and the HPV vaccine in a national sample of Australian men and women. Sex Health (2010) 0.92
Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3). Bioorg Med Chem Lett (2009) 0.91
Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR. Bioorg Med Chem Lett (2004) 0.91
Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides. ChemMedChem (2006) 0.91
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model. J Med Chem (2006) 0.90
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs). Bioorg Med Chem Lett (2007) 0.90
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats. ChemMedChem (2009) 0.90
Biochemical and cell-based assays for characterization of BACE-1 inhibitors. Anal Biochem (2005) 0.90
N-heterocyclic derived M1 positive allosteric modulators. Bioorg Med Chem Lett (2010) 0.90