About: Rational improvement of gp41-targeting HIV-1 fusion inhibitors: an innovatively designed Ile-Asp-Leu tail with alternative conformations

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About: Rational improvement of gp41-targeting HIV-1 fusion inhibitors: an innovatively designed Ile-Asp-Leu tail with alternative conformations Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Rational improvement of gp41-targeting HIV-1 fusion inhibitors: an innovatively designed Ile-Asp-Leu tail with alternative conformations
Creator	Jiang, Shibo Shi, Lei Lu, Lu Zhu, Yun Ma, Zhenxuan Qin, Lili Su, Shan Tang, Jianchao Wang, Qian Ye, Sheng Zhang, Rongguang
Source	Medline; PMC
abstract	Peptides derived from the C-terminal heptad repeat (CHR) of HIV gp41 have been developed as effective fusion inhibitors against HIV-1, but facing the challenges of enhancing potency and stability. Here, we report a rationally designed novel HIV-1 fusion inhibitor derived from CHR-derived peptide (Trp628~Gln653, named CP), but with an innovative Ile-Asp-Leu tail (IDL) that dramatically increased the inhibitory activity by up to 100 folds. We also determined the crystal structures of artificial fusion peptides N36- and N43-L6-CP-IDL. Although the overall structures of both fusion peptides share the canonical six-helix bundle (6-HB) configuration, their IDL tails adopt two different conformations: a one-turn helix with the N36, and a hook-like structure with the longer N43. Structural comparison showed that the hook-like IDL tail possesses a larger interaction interface with NHR than the helical one. Further molecular dynamics simulations of the two 6-HBs and isolated CP-IDL peptides suggested that hook-like form of IDL tail can be stabilized by its binding to NHR trimer. Therefore, CP-IDL has potential for further development as a new HIV fusion inhibitor, and this strategy could be widely used in developing artificial fusion inhibitors against HIV and other enveloped viruses.
has issue date	2016-09-26(xsd:dateTime)
bibo:doi	10.1038/srep31983
bibo:pmid	27666394
has license	cc-by
sha1sum (hex)	bba54a43464e4fda9280139894c5467524ef2faf
schema:url	https://doi.org/10.1038/srep31983
resource representing a document's title	Rational improvement of gp41-targeting HIV-1 fusion inhibitors: an innovatively designed Ile-Asp-Leu tail with alternative conformations
has PubMed Central identifier	PMC5036048
has PubMed identifier	27666394
schema:publication	Sci Rep
resource representing a document's body	covid:bba54a43464e4fda9280139894c5467524ef2faf#body_text
is schema:about of	named entity 'TARGETING' named entity 'structure' named entity 'tail' named entity 'inhibitors' named entity 'IMPROVEMENT' named entity 'ADOPT' named entity 'SHARE' named entity 'BINDING' named entity 'COULD BE' named entity 'FUSION' named entity 'DEVELOPING' named entity 'PEPTIDES' named entity 'DERIVED' named entity 'NEW' named entity 'TRIMER' named entity 'HIV FUSION INHIBITOR' named entity '100' named entity 'FORM' named entity 'TAILS' named entity 'STRUCTURE' named entity 'POSSESSES' named entity 'ITS' named entity 'HOOK' named entity 'COMPARISON' named entity 'STRUCTURES' named entity 'HIV' named entity 'REPORT' named entity 'N43' named entity 'DIFFERENT' named entity 'ISOLATED' named entity 'ILE-ASP' named entity 'ARTIFICIAL' named entity 'HERE' named entity 'CONFIGURATION' named entity 'VIRUSES' named entity 'STRUCTURAL' named entity 'INHIBITORY ACTIVITY' named entity 'CRYSTAL' named entity 'INTERFACE' named entity 'DEVELOPMENT' named entity 'HBS' named entity 'LIKE' named entity 'USED' named entity 'CHR' named entity 'ALTERNATIVE' named entity 'TAIL' named entity 'TAIL' named entity 'GP41' named entity 'HIV-1' named entity 'ILE-ASP' named entity 'FOLDS' named entity 'NOVEL' named entity 'BUNDLE' named entity 'STABILIZED' named entity 'INTERACTION' named entity 'LARGER' named entity 'MOLECULAR DYNAMICS SIMULATIONS' named entity 'THEIR' named entity 'IDL' named entity 'OVERALL' named entity 'FUSION INHIBITORS' named entity 'FUSION INHIBITOR' named entity 'INCREASED' named entity 'BUT' named entity 'PEPTIDE' named entity 'HIV-1' named entity 'DETERMINED' named entity 'POTENTIAL' named entity 'N36' named entity 'TURN' named entity 'NAMED'

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