1zml
From Proteopedia
Crystal Structure of the Catalytic Domain of Factor XI in complex with (R)-1-(4-(4-(hydroxymethyl)-1,3,2-dioxaborolan-2-yl)phenethyl)guanidine
Contents |
Overview
A series of functionalized aryl boronic acids were synthesized and evaluated as potential inhibitors of factor XIa. Crystal structures of the protein-inhibitor complexes led to the design and synthesis of second generation compounds showing single digit micromolar inhibition against FXIa and selectivity against thrombin, trypsin, and FXa.
Disease
Known disease associated with this structure: Factor XI deficiency, autosomal dominant OMIM:[264900], Factor XI deficiency, autosomal recessive OMIM:[264900]
About this Structure
1ZML is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa., Lazarova TI, Jin L, Rynkiewicz M, Gorga JC, Bibbins F, Meyers HV, Babine R, Strickler J, Bioorg Med Chem Lett. 2006 Oct 1;16(19):5022-7. Epub 2006 Jul 28. PMID:16876411 Page seeded by OCA on Sat May 3 17:48:50 2008
