PDBsum entry 1zxc

Hydrolase

PDB id: 1zxc

Contents

Protein chains

259 a.a.

Ligands

IH6 ×2

Metals

_ZN ×2

Waters ×173

References listed in PDB file

Key reference

• Title: Acetylenic tace inhibitors. Part 2: sar of six-Membered cyclic sulfonamide hydroxamates.
• Authors: J.I.Levin, J.M.Chen, L.M.Laakso, M.Du, X.Du, A.M.Venkatesan, V.Sandanayaka, A.Zask, J.Xu, W.Xu, Y.Zhang, J.S.Skotnicki.
• Ref.: Bioorg Med Chem Lett, 2005, 15, 4345-4349. [DOI no: 10.1016/j.bmcl.2005.06.072]
• PubMed id: 16084720

Abstract

The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model.