Results 201 to 210 of about 31,386 (239)

Clinical Experience With Hedgehog Pathway Inhibitors

Journal 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
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A novel hedgehog inhibitor for the treatment of hematological malignancies

Anti-Cancer Drugs, 2018
The hedgehog-smoothened (HH/SMO) pathway has been proposed as a potential therapeutic target for hematological malignancies. Our previous studies designed a series of HH inhibitors with novel scaffolds distinctive from vismodegib, the first Food and Drug Administration-approved HH inhibitor for the treatment of basal-cell carcinoma and medulloblastoma.
Peng, Lin, Yuanming, He, Guodong, Chen, Haikuo, Ma, Jiyue, Zheng, Zubin, Zhang, Biyin, Cao, Hongjian, Zhang, Xiaohu, Zhang, Xinliang, Mao   +9 more
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Current Status of Hedgehog Signaling Inhibitors

Current Topics in Medicinal Chemistry
Abstract: The Hedgehog (Hh) signaling pathway plays a crucial role in diverse biological pro-cesses such as cell differentiation, proliferation, senescence, tumorigenesis, malignant transfor-mation, and drug resistance. Aberrant Hh signaling, resulting from mutations and excessive acti-vation, can contribute to the development of various diseases ...
Xiaotang, Wang, Tian, Wang, Xiaona, Song, Jiping, Gao, Guoqiang, Xu, Yunhui, Ma, Guohua, Song   +6 more
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GDC-0449—A potent inhibitor of the hedgehog pathway

Bioorganic & 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).
Kirk D, Robarge, Shirley A, Brunton, Georgette M, Castanedo, Yong, Cui, Michael S, Dina, Richard, Goldsmith, Stephen E, Gould, Oivin, Guichert, Janet L, Gunzner, Jason, Halladay, Wei, Jia, Cyrus, Khojasteh, Michael F T, Koehler, Karen, Kotkow, Hank, La, Rebecca L, Lalonde, Kevin, Lau, Leslie, Lee, Derek, Marshall, James C, Marsters, Lesley J, Murray, Changgeng, Qian, Lee L, Rubin, Laurent, Salphati, Mark S, Stanley, John H A, Stibbard, Daniel P, Sutherlin, Savita, Ubhayaker, Shumei, Wang, Susan, Wong, Minli, Xie   +30 more
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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, Milind, Parle, Ruben, Abagyan   +2 more
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Targeting Hedgehog signaling and understanding refractory response to treatment with Hedgehog pathway inhibitors

Drug Resistance Updates, 2012
Hedgehog (Hh) signaling is a principal component of the morphogenetic code best known to direct pattern formation during embryogenesis. The Hh pathway remains active in adulthood however where it guides tissue regeneration and remodeling and Hh production in the niche plays an important role in maintaining stem cell compartment size.
Souza Queiroz, Karla, Spek, CA, Peppelenbosch, Maikel   +2 more
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Hedgehog inhibitors from Artocarpus communis and Hyptis suaveolens

Bioorganic & Medicinal Chemistry, 2015
The hedgehog (Hh) signaling pathway plays crucial roles in cell maintenance and proliferation during embryonic development. Naturally occurring Hh inhibitors were isolated from Artocarpus communis and Hyptis suaveolens using our previously constructed cell-based assay system.
Midori A, Arai, Kyoko, Uchida, Samir K, Sadhu, Firoj, Ahmed, Takashi, Koyano, Thaworn, Kowithayakorn, Masami, Ishibashi   +6 more
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Synthesis and Evaluation of Aminothiazole Derivatives as Hedgehog Pathway Inhibitors

Chemistry & Biodiversity, 2019
AbstractA series of aminothiazole derivatives bearing the benzimidazole moiety were synthesized and evaluated in Gli luciferase reporter assays. Lead optimization led to the discovery of potent hedgehog pathway antagonist 18 (2‐[3‐(1H‐benzimidazol‐2‐yl)‐4‐chloroanilino]‐N‐[4‐(trifluoromethyl)phenyl]‐1,3‐thiazole‐4‐carboxamide), with IC50 values in ...
Chiyu Sun, Ying Zhang, Lin Lin, Shuyuan Liu, Rui Wang, Wei Zang, Weijia Meng, Xiaofeng Chen   +7 more
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Synthesis and biological evaluation of desmethylveramiline, a micromolar Hedgehog inhibitor

Bioorganic & Medicinal Chemistry Letters, 2011
Desmethylveramiline (1), an aza steroid analogue of veramiline was designed as a surrogate for cyclopamine, a reference antagonist of the Sonic Hedgehog (Shh) pathway. Desmethyveramiline (1) was prepared in seven steps from commercially available Fernholtz acid using the hydroformylation of a terminal olefine as the key step for the construction of the
Guerlet, Guillaume, Spangenberg, Thomas, Mann, André, Faure, Hélène, Ruat, Martial   +4 more
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Hedgehog Pathway Inhibitors

2021
Shauna Higgins, Ashley Wysong
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