Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß [PDF]
Angewandte Chemie - International Edition, 2019 AbstractThe Hedgehog (Hh) signaling pathway is crucial for vertebrate embryonic development, tissue homeostasis and regeneration. Hh signaling is upregulated in basal cell carcinoma and medulloblastoma and Hh pathway inhibitors targeting the Smoothened (SMO) protein are in clinical use.
Hideaki T Matsubayashi +2 more
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Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors [PDF]
Beilstein Journal of Organic Chemistry, 2012 Sant-75 is a newly identified potent inhibitor of the hedgehog pathway. We designed a diversity-oriented synthesis program, and synthesized a series of Sant-75 analogues, which lays the foundation for further investigation of the structure–activity ...
Chao Che +8 more
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Targeted protein degradation reveals BET bromodomains as the cellular target of Hedgehog pathway inhibitor-1 [PDF]
Nature Communications, 2023 Target deconvolution of small molecule hits from phenotypic screens presents a major challenge. Many screens have been conducted to find inhibitors for the Hedgehog signaling pathway – a developmental pathway with many implications in health and disease –
Meropi Bagka +8 more
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Update on Hedgehog Pathway Inhibitor Therapy for Patients with Basal Cell Naevus Syndrome or High-frequency Basal Cell Carcinoma [PDF]
Acta Dermato-Venereologica, 2022 Some patients with basal cell carcinoma develop a large number of basal cell carcinomas during their lives. The most common underlying genetic disease that causes multiple basal cell carcinomas is basal cell naevus syndrome. Basal cell naevus syndrome is
Babette J.A. Verkouteren +4 more
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Treatment of Medulloblastoma with Hedgehog Pathway Inhibitor GDC-0449 [PDF]
New England Journal of Medicine, 2009 Medulloblastoma is the most common malignant brain tumor in children. Aberrant activation of the hedgehog signaling pathway is strongly implicated in the development of some cases of medulloblastoma. A 26-year-old man with metastatic medulloblastoma that was refractory to multiple therapies was treated with a novel hedgehog pathway inhibitor, GDC-0449;
Charles M Rüdin +2 more
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Hedgehog Pathway Inhibitor HhAntag691 Is a Potent Inhibitor of ABCG2/BCRP and ABCB1/Pgp
Neoplasia: An International Journal for Oncology Research, 2009 HhAntag691 (GDC-0449), a low-molecular weight inhibitor of the tumor-promoting hedgehog (Hh) signaling pathway, has been used to treat medulloblastoma in animal models and has recently entered clinical trials for a variety of solid tumors.
Yimao Zhang +2 more
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Effective treatment of locally advanced periocular basal cell carcinoma with oral hedgehog pathway inhibitor? [PDF]
Graefe's Archive for Clinical and Experimental Ophthalmology, 2020 Xiaoyi Hou +2 more
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Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61 [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2018 Andrea Calcaterra +2 more
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Hedgehog Pathway Inhibitors against Tumor Microenvironment [PDF]
Cells, 2021 Targeting the hedgehog (HH) pathway to treat aggressive cancers of the brain, breast, pancreas, and prostate has been ongoing for decades. Gli gene amplifications have been long discovered within malignant glioma patients, and since then, inhibitors against HH pathway-associated molecules have successfully reached the clinical stage where several of ...
Gampala, Silpa, Yang, Jer-Yen
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Radiation Sensitization of Basal Cell and Head and Neck Squamous Cell Carcinoma by the Hedgehog Pathway Inhibitor Vismodegib [PDF]
International Journal of Molecular Sciences, 2018 Stephanie Hehlgans +2 more
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