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Evaluation of sequence variability in HIV-1 gp41 C-peptide helix-grafted proteins.

Abstract：

:Many therapeutically-relevant protein-protein interactions (PPIs) have been reported that feature a helix and helix-binding cleft at the interface. Given this, different approaches to disrupting such PPIs have been developed. While short peptides (<15 amino acids) typically do not fold into a stable helix, researchers have reported chemical approaches to constraining helix structure. However, these approaches rely on laborious, and often expensive, chemical synthesis and purification. Our premise is that protein-based solutions that stabilize a therapeutically-relevant helix offer a number of advantages. In contrast to chemically constrained helical peptides, or minimal/miniature proteins, which must be synthesized (at great expense and labor), a protein can be expressed in a cellular system (like all current protein therapeutics). If selected properly, the protein scaffold can stabilize the therapeutically-relevant helix. We recently reported a protein engineering strategy, which we call "helix-grafted display", and applied it to the challenge of suppressing HIV entry. We have reported helix-grafted display proteins that inhibit formation of an intramolecular PPI involving HIV gp41 C-peptide helix, and HIV gp41 N-peptide trimer, which contain C-peptide helix-binding clefts. Here, we used yeast display to screen a library of grafted C-peptide helices for N-peptide trimer recognition. Using 'hits' from yeast display library screening, we evaluated the effect helix mutations have on structure, expression, stability, function (target recognition), and suppression of HIV entry.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tennyson RL,Walker SN,Ikeda T,Harris RS,McNaughton BR

doi

10.1016/j.bmc.2017.07.064

subject

Has Abstract

pub_date

2018-03-15 00:00:00

pages

1220-1224

issue

6

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(17)31259-2

journal_volume

26

pub_type

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