1BIW

DESIGN AND SYNTHESIS OF CONFORMATIONALLY-CONSTRAINED MMP INHIBITORS

1BIW の概要

• エントリーDOI: 10.2210/pdb1biw/pdb
• 分子名称: PROTEIN (STROMELYSIN-1 COMPLEX), ZINC ION, CALCIUM ION, ... (5 entities in total)
• 機能のキーワード: stromelysin, matrix metalloprotease, osteoarthritis, structure-based drug design, protein crystal structure, hydrolase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Secreted, extracellular space, extracellular matrix (Probable): P08254
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 39750.69

構造登録者

Natchus, M.G.,Cheng, M.,Wahl, C.T.,Pikul, S.,Almstead, N.G.,Bradley, R.S.,Taiwo, Y.O.,Mieling, G.E.,Dunaway, C.M.,Snider, C.E.,McIver, J.M.,Barnett, B.L.,McPhail, S.J.,Anastasio, M.B.,De, B. (登録日: 1998-06-19, 公開日: 1999-07-16, 最終更新日: 2023-12-27)

主引用文献

Natchus, M.G.,Cheng, M.,Wahl, C.T.,Pikul, S.,Almstead, N.G.,Bradley, R.S.,Taiwo, Y.O.,Mieling, G.E.,Dunaway, C.M.,Snider, C.E.,McIver, J.M.,Barnett, B.L.,McPhail, S.J.,Anastasio, M.B.,De, B.
Design and synthesis of conformationally-constrained MMP inhibitors.
Bioorg.Med.Chem.Lett., 8:2077-2080, 1998

PubMed Abstract: A novel series of conformationally constrained matrix metalloprotease inhibitors was identified. The potencies observed for these inhibitors were highly dependent upon the substitution pattern on the caprolactam ring as well as the succinate moiety.

PubMed: 9873489
DOI: 10.1016/S0960-894X(98)00370-9

実験手法

X-RAY DIFFRACTION (2.5 Å)