GLIS3 drives epithelial-mesenchymal transition and cancer stem-like traits in stomach adenocarcinoma via TGFBR3-Hedgehog signaling. [PDF]
Xiao Q, Deng H, Li J, Zheng Y, Zhang Y.
europepmc +1 more source
Dual Hedgehog/GLI1 and PI3K/Akt/mTOR Targeting Possesses Higher Efficacy to Inhibit T-Cell Acute Lymphoblastic Leukemia Growth. [PDF]
De Chiara M +4 more
europepmc +1 more source
Transition from acute kidney injury to chronic kidney disease: molecular mechanisms and therapeutic interventions. [PDF]
Huang X +7 more
europepmc +1 more source
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GDC-0449—A potent inhibitor of the hedgehog pathway
Bioorganic and Medicinal Chemistry Letters, 2009SAR 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
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, 2015Hepatocellular 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, 2014Vismodegib (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, 2008A 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, 2018The 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

