Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.

PubWeight™: 0.77‹?›

🔗 View Article (PMID 16678413)

Published in Bioorg Med Chem Lett on May 05, 2006

Authors

Sheela A Thomas1, Tongmei Li, Keith W Woods, Xiaohong Song, Garrick Packard, John P Fischer, Robert B Diebold, Xuesong Liu, Yan Shi, Vered Klinghofer, Eric F Johnson, Jennifer J Bouska, Amanda Olson, Ran Guan, Shayna R Magnone, Kennan Marsh, Yan Luo, Saul H Rosenberg, Vincent L Giranda, Qun Li

Author Affiliations

1: Cancer Research, Department R47S, AP10 Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064, USA. sheela.thomas@abbott.com

Articles by these authors

Human infection with a novel avian-origin influenza A (H7N9) virus. N Engl J Med (2013) 24.88

An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature (2005) 22.40

Fever with thrombocytopenia associated with a novel bunyavirus in China. N Engl J Med (2011) 13.18

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res (2008) 9.65

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med (2013) 8.89

Standardizing global gene expression analysis between laboratories and across platforms. Nat Methods (2005) 6.23

A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Cell Stem Cell (2008) 5.90

ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res (2007) 5.75

Nosocomial transmission of human granulocytic anaplasmosis in China. JAMA (2008) 5.01

ABT-450/r-ombitasvir and dasabuvir with or without ribavirin for HCV. N Engl J Med (2014) 4.90

Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab (2006) 4.64

Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell (2008) 4.63

Probable limited person-to-person transmission of highly pathogenic avian influenza A (H5N1) virus in China. Lancet (2008) 4.17

Phase 0 clinical trial of the poly (ADP-ribose) polymerase inhibitor ABT-888 in patients with advanced malignancies. J Clin Oncol (2009) 4.14

S phase activation of the histone H2B promoter by OCA-S, a coactivator complex that contains GAPDH as a key component. Cell (2003) 4.03

Human infection with avian influenza A H7N9 virus: an assessment of clinical severity. Lancet (2013) 3.90

An emerging recombinant human enterovirus 71 responsible for the 2008 outbreak of hand foot and mouth disease in Fuyang city of China. Virol J (2010) 3.90

Comparative epidemiology of human infections with avian influenza A H7N9 and H5N1 viruses in China: a population-based study of laboratory-confirmed cases. Lancet (2013) 3.77

Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity. Lancet Oncol (2010) 3.76

Person-to-person transmission of severe fever with thrombocytopenia syndrome virus. Vector Borne Zoonotic Dis (2011) 3.73

Highly efficient differentiation of human ES cells and iPS cells into mature pancreatic insulin-producing cells. Cell Res (2009) 3.44

Should we standardize the 1,700-year-old fecal microbiota transplantation? Am J Gastroenterol (2012) 3.38

Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737. Cancer Res (2007) 3.24

MyD88-dependent IL-1 receptor signaling is essential for gouty inflammation stimulated by monosodium urate crystals. J Clin Invest (2006) 3.21

The structure of human microsomal cytochrome P450 3A4 determined by X-ray crystallography to 2.05-A resolution. J Biol Chem (2004) 3.18

Control of rice grain-filling and yield by a gene with a potential signature of domestication. Nat Genet (2008) 3.09

Comprehensive Molecular Characterization of Papillary Renal-Cell Carcinoma. N Engl J Med (2015) 3.00

Alum interaction with dendritic cell membrane lipids is essential for its adjuvanticity. Nat Med (2011) 2.82

An open conformation of mammalian cytochrome P450 2B4 at 1.6-A resolution. Proc Natl Acad Sci U S A (2003) 2.74

Antigen retrieval immunohistochemistry: review and future prospects in research and diagnosis over two decades. J Histochem Cytochem (2011) 2.70

Induction of pluripotency in mouse somatic cells with lineage specifiers. Cell (2013) 2.69

Receptor-independent, direct membrane binding leads to cell-surface lipid sorting and Syk kinase activation in dendritic cells. Immunity (2008) 2.67

Structure of mammalian cytochrome P450 2B4 complexed with 4-(4-chlorophenyl)imidazole at 1.9-A resolution: insight into the range of P450 conformations and the coordination of redox partner binding. J Biol Chem (2004) 2.66

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A (2007) 2.60

Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen. Nat Struct Mol Biol (2005) 2.54

Epidemiologic features of severe fever with thrombocytopenia syndrome in China, 2011-2012. Clin Infect Dis (2013) 2.46

TIN2 binds TRF1 and TRF2 simultaneously and stabilizes the TRF2 complex on telomeres. J Biol Chem (2004) 2.36

Plant hormone jasmonate prioritizes defense over growth by interfering with gibberellin signaling cascade. Proc Natl Acad Sci U S A (2012) 2.34

In vitro derivation of functional insulin-producing cells from human embryonic stem cells. Cell Res (2007) 2.28

Clinical characteristics of 26 human cases of highly pathogenic avian influenza A (H5N1) virus infection in China. PLoS One (2008) 2.28

A chemical approach to stem-cell biology and regenerative medicine. Nature (2008) 2.25

The structure of human cytochrome P450 2C9 complexed with flurbiprofen at 2.0-A resolution. J Biol Chem (2004) 2.24

Chk1 mediates S and G2 arrests through Cdc25A degradation in response to DNA-damaging agents. J Biol Chem (2003) 2.18

DNA extraction from archival formalin-fixed, paraffin-embedded tissue sections based on the antigen retrieval principle: heating under the influence of pH. J Histochem Cytochem (2002) 2.16

Colon-specific delivery of a probiotic-derived soluble protein ameliorates intestinal inflammation in mice through an EGFR-dependent mechanism. J Clin Invest (2011) 2.16

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther (2005) 2.15

Generation of oligodendrocyte precursor cells from mouse dorsal spinal cord independent of Nkx6 regulation and Shh signaling. Neuron (2005) 2.12

Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res (2008) 2.10

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J Med Chem (2007) 2.09

Structure of human microsomal cytochrome P450 2C8. Evidence for a peripheral fatty acid binding site. J Biol Chem (2003) 2.09

Bioavailability of generic ritonavir and lopinavir/ritonavir tablet products in a dog model. J Pharm Sci (2010) 2.06

A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J Pharmacol Exp Ther (2006) 2.06

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J Med Chem (2004) 2.05

Generation of iPSCs from mouse fibroblasts with a single gene, Oct4, and small molecules. Cell Res (2010) 2.04

Hepatocellular carcinoma: stiffness value and ratio to discriminate malignant from benign focal liver lesions. Radiology (2015) 2.03

Venous thromboembolism in body contouring: an analysis of 17,774 patients from the National Surgical Quality Improvement databases. Plast Reconstr Surg (2015) 2.03

Lethal pulmonary infection with Francisella novicida is associated with severe sepsis. J Leukoc Biol (2009) 2.01

Segmental hair analysis after a single dose of zolpidem: comparison with a previous study. J Anal Toxicol (2013) 1.98

A Propensity-Matched Analysis of the Influence of Breast Reconstruction on Subsequent Development of Lymphedema. Plast Reconstr Surg (2015) 1.97

Adaptations for the oxidation of polycyclic aromatic hydrocarbons exhibited by the structure of human P450 1A2. J Biol Chem (2007) 1.96

Is Single-Stage Prosthetic Reconstruction Cost Effective? A Cost-Utility Analysis for the Use of Direct-to-Implant Breast Reconstruction Relative to Expander-Implant Reconstruction in Postmastectomy Patients. Plast Reconstr Surg (2016) 1.95

Calcium oxalate crystals induce renal inflammation by NLRP3-mediated IL-1β secretion. J Clin Invest (2012) 1.91

Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor. Clin Cancer Res (2011) 1.91

Navigating the kinome. Nat Chem Biol (2011) 1.88

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J Med Chem (2008) 1.85

Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia. Pain (2009) 1.84

Breaking tolerance to the natural human liver autoantigen cytochrome P450 2D6 by virus infection. J Exp Med (2008) 1.76

On the evolutionary history, population genetics and diversity among isolates of Salmonella Enteritidis PFGE pattern JEGX01.0004. PLoS One (2013) 1.69

Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer. J Med Chem (2009) 1.68

High resolution clustering of Salmonella enterica serovar Montevideo strains using a next-generation sequencing approach. BMC Genomics (2012) 1.68

A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo. Cancer Res (2006) 1.67