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Structural Basis of Activin Receptor-Like Kinase 2 (R206H) Inhibition by Bis-heteroaryl Pyrazole-Based Inhibitors for the Treatment of Fibrodysplasia Ossificans Progressiva Identified by the Integration of Ligand-Based and Structure-Based Drug Design Approaches

[Image: see text] Fibrodysplasia ossificans progressiva (FOP) is a rare but severe genetic disorder in which acute inflammation elicits progressive heterotopic ossification in the muscles, tendons, and ligaments. Classic FOP is caused by the R206H mutation in ALK2/ACVR1. While several activin recept...

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Detalles Bibliográficos
Autores principales: Sato, Tomohiro, Sekimata, Katsuhiko, Sakai, Naoki, Watanabe, Hisami, Mishima-Tsumagari, Chiemi, Taguri, Tomonori, Matsumoto, Takehisa, Fujii, Yoshifumi, Handa, Noriko, Tanaka, Akiko, Shirouzu, Mikako, Yokoyama, Shigeyuki, Hashizume, Yoshinobu, Miyazono, Kohei, Koyama, Hiroo, Honma, Teruki
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7254505/
https://www.ncbi.nlm.nih.gov/pubmed/32478230
http://dx.doi.org/10.1021/acsomega.9b04245