PDBsum entry 2c0t

Transferase

PDB id: 2c0t

Contents

Protein chains

428 a.a.

Ligands

L3G ×2

Metals

_CA ×4

Waters ×200

References listed in PDB file

Key reference

• Title: Discovery of a-770041, A src-Family selective orally active lck inhibitor that prevents organ allograft rejection.
• Authors: A.Burchat, D.W.Borhani, D.J.Calderwood, G.C.Hirst, B.Li, R.F.Stachlewitz.
• Ref.: Bioorg Med Chem Lett, 2006, 16, 118-122. [DOI no: 10.1016/j.bmcl.2005.09.039]
• PubMed id: 16216497

Abstract

We describe the identification, SAR, and pharmacology of the src-family selective lck inhibitor A-770041 that prolongs the survival of major histocompatibility mismatched allografts in models of solid organ transplant rejection for greater than 65 days.

Secondary reference #1

• Title: A-420983: a potent, Orally active inhibitor of lck with efficacy in a model of transplant rejection.
• Authors: D.W.Borhani, D.J.Calderwood, M.M.Friedman, G.C.Hirst, B.Li, A.K.Leung, B.Mcrae, S.Ratnofsky, K.Ritter, W.Waegell.
• Ref.: Bioorg Med Chem Lett, 2004, 14, 2613-2616. [DOI no: 10.1016/j.bmcl.2004.02.101]
• PubMed id: 15109663