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2w3l

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2w3l, resolution 2.10Å ()
Sites: and
Ligands:
Related: 1ysw, 1g5m, 1gjh


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



CRYSTAL STRUCTURE OF CHIMAERIC BCL2-XL AND PHENYL TETRAHYDROISOQUINOLINE AMIDE COMPLEX

Publication Abstract from PubMed

Anti-apoptotic Bcl-2 protects cells from apoptosis by binding to pro-apoptotic members of the Bcl-2 family thereby playing a role in tumour survival in response to chemo- or radiation therapy. We describe a series of phenyl pyrazoles that have high affinity for Bcl-2 and rationalise the observed SAR by means of an X-ray crystal structure.

Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors., Porter J, Payne A, de Candole B, Ford D, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Whitcombe I, Davis J, Stubberfield C, Bioorg Med Chem Lett. 2008 Oct 31. PMID:19027294

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

2W3L is a 2 chains structure with sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  • Porter J, Payne A, de Candole B, Ford D, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Whitcombe I, Davis J, Stubberfield C. Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors. Bioorg Med Chem Lett. 2008 Oct 31. PMID:19027294 doi:S0960-894X(08)01331-0

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