Discovery of highly potent and ALK2/ALK1 selective kinase inhibitors using DNA-encoded chemistry technology

Activin receptor type 1 (ACVR1; ALK2) and activin receptor like type 1 (ACVRL1; ALK1) are transforming growth factor beta family receptors that integrate extracellular signals of bone morphogenic proteins (BMPs) and activins into Mothers Against Decapentaplegic homolog 1/5 (SMAD1/SMAD5) signaling co...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 2024-11, Vol.121 (47), p.e2413108121
Hauptverfasser:	Jimmidi, Ravikumar, Monsivais, Diana, Ta, Hai Minh, Sharma, Kiran L, Bohren, Kurt M, Chamakuri, Srinivas, Liao, Zian, Li, Feng, Hakenjos, John M, Li, Jian-Yuan, Mishina, Yuji, Pan, Haichun, Qin, Xuan, Robers, Matthew B, Sankaran, Banumathi, Tan, Zhi, Tang, Suni, Vasquez, Yasmin M, Wilkinson, Jennifer, Young, Damian W, Palmer, Stephen S, MacKenzie, Kevin R, Kim, Choel, Matzuk, Martin M
Format:	Artikel
Sprache:	eng
Schlagworte:	Activin Activin Receptors, Type I - antagonists & inhibitors Activin Receptors, Type I - genetics Activin Receptors, Type I - metabolism Activin Receptors, Type II - genetics Activin Receptors, Type II - metabolism Bone growth Bone morphogenetic proteins Brain tumors Cancer Chemical compounds Chemical synthesis Deoxyribonucleic acid DNA DNA - metabolism DNA biosynthesis DNA structure Drug Discovery - methods Enzyme inhibitors Gene expression Growth factors Humans Hydrogen bonding Hydrogen bonds Inhibitors Kinases Lung cancer Mutation Myositis ossificans Pancreatic cancer Pharmacology Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Receptors Signal Transduction - drug effects Smad5 protein Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology
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