Results 221 to 230 of about 37,007 (262)

GDC-0449—A potent inhibitor of the hedgehog pathway

Bioorganic and Medicinal Chemistry Letters, 2009
SAR for a wide variety of heterocyclic replacements for a benzimidazole led to the discovery of functionalized 2-pyridyl amides as novel inhibitors of the hedgehog pathway. The 2-pyridyl amides were optimized for potency, PK, and drug-like properties by modifications to the amide portion of the molecule resulting in 31 (GDC-0449).
Hank La, James C Marsters, Lee L Rubin
exaly   +3 more sources

Clinical Experience With Hedgehog Pathway Inhibitors

open access: yesJournal of Clinical Oncology, 2010
The Hedgehog (Hh) signaling pathway is critical for cell growth and differentiation during embryogenesis and early development. While it is mostly quiescent in adults, inappropriate reactivation of the Hh pathway has been shown to be involved in the development of cancer.
Jennifer A, Low, Frederic J, de Sauvage
openaire   +3 more sources

Sonic hedgehog pathway inhibitor mitigates mouse hepatocellular carcinoma

American Journal of Surgery, 2015
Hepatocellular carcinoma (HCC) is a leading cause of death in Asian countries. Sonic hedgehog (Shh) pathway plays a role in hepatocarcinogenesis. We investigated the treatment effect of mouse HCC with Shh inhibitor GDC-0449.Mouse hepatoma ML-1 cells were implanted in B6 mice. Fifteen days later, GDC-0449 (vismodegib), antagonist of smoothened, was used
Kuo-Shyang Jeng   +2 more
exaly   +3 more sources

Embryofetal Development Study of Vismodegib, a Hedgehog Pathway Inhibitor, in Rats

Birth Defects Research Part B: Developmental and Reproductive Toxicology, 2014
Vismodegib (Erivedge) is a first‐in‐class small‐molecule hedgehog pathway inhibitor for the treatment of adults with advanced basal‐cell carcinoma. Because this pathway is known to play key roles in patterning and growth during vertebrate development, vismodegib was anticipated to be embryotoxic.
Eric, Morinello   +4 more
exaly   +3 more sources

Potent Inhibitors of the Hedgehog Signaling Pathway

Journal of Medicinal Chemistry, 2008
A small family of phenyl quinazolinone ureas is reported as potent modulators of Hedgehog protein function. Preliminary SAR studies of the urea substituent led to a nanomolar Hedgehog antagonist.
Shirley A, Brunton   +6 more
openaire   +2 more sources

Hedgehog pathway and smoothened inhibitors in cancer therapies

Anti-Cancer Drugs, 2018
The hedgehog (Hh) pathway plays an important role in cancer development and maintenance, as ~25% of all cancers have aberrant Hh pathway activation. Targeted therapy for inhibition of the Hh pathway was thought to be promising for achieving clinical response in the Hh-dependent cancers.
Kirti K, Chahal   +2 more
openaire   +2 more sources

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