1gzl

From Proteopedia

Revision as of 08:50, 30 October 2007

CRYSTAL STRUCTURE OF C14LINKMID/IQN17: A CROSS-LINKED INHIBITOR OF HIV-1 ENTRY BOUND TO THE GP41 HYDROPHOBIC POCKET

Overview

Peptides corresponding to the C-terminal heptad repeat of HIV-1 gp41, (C-peptides) are potent inhibitors of HIV-1 entry into cells. Their, mechanism of inhibition involves binding in a helical conformation to the, central coiled coil of HIV-1 gp41 in a dominant-negative manner. Short, C-peptides, however, have low binding affinity for gp41 and poor, inhibitory activity, which creates an obstacle to the development of small, drug-like C-peptides. To improve the inhibitory potency of short, C-peptides that target the hydrophobic pocket region of gp41, we use two, strategies to stabilize the C-peptide helix: chemical crosslinking and, substitution with unnatural helix-favoring amino acids. In this study, the, short linear peptide shows no significant inhibitory activity, but a, constrained ... [(full description)]

About this Structure

1GZL is a [Single protein] structure of sequence from [[1]] with CL, ACE and N2P as [ligands]. Structure known Active Site: CLA. Full crystallographic information is available from [OCA].

Reference

Short constrained peptides that inhibit HIV-1 entry., Sia SK, Carr PA, Cochran AG, Malashkevich VN, Kim PS, Proc Natl Acad Sci U S A. 2002 Nov 12;99(23):14664-9. Epub 2002 Nov 4. PMID:12417739

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