Hirokazu Matsumoto , Tien-Cheng Wang , Haruka Taniguchi , Yu Nishioka , Mariko Hatakeyama , Takayoshi Kinoshita , Masaaki Sawa
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引用次数: 0
Abstract
Tyrosine kinase 2 (TYK2) plays a crucial role in both adaptive and innate immune responses. The catalytic activity of the TYK2 JH1 kinase domain is controlled by the TYK2 JH2 pseudokinase domain and stabilized to maintain its inactive state until the upstream receptor activations. Here, we report the discovery of aminopyridine analogs as novel TYK2 activators through structural modification of a known JH2 binder. Compound 16b demonstrated a dose-dependent increase in TYK2 enzymatic activity.
期刊介绍：
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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