Navigation Links
Potent peptides inhibit HIV entry into cells
Date:10/10/2007

UPTON, NY -- Based in part on protein structures determined at the National Synchrotron Light Source (NSLS) at the U.S. Department of Energy's Brookhaven National Laboratory, scientists at the University of Utah have developed new peptides that appear to be significantly more effective at blocking HIV's entry into cells than other drugs in their class. In a paper being published online by the Proceedings of the National Academy of Sciences the week of October 8, 2007, the researchers say these peptides are sufficiently potent to begin pre-clinical studies as a new class of agents for the prevention and treatment of HIV/AIDS.

"Our 'D-peptides' offer several potential therapeutic advantages over existing peptide entry inhibitors, which are costly, require high dose injections, and suffer from the emergence of drug-resistance," said University of Utah biochemist Michael S. Kay, lead author on the paper. "In contrast, our D-peptides resist degradation, so they have the potential to be administered by mouth and last longer in the bloodstream. Since these inhibitors have a unique inhibitory mechanism, they should work well in combination with existing HIV inhibitors."

The researchers were particularly interested in developing drugs to bind to an essential "pocket" structure found in all HIV strains that was previously identified as a promising drug target using structures determined at Brookhaven's NSLS. Numerous previous attempts to target this pocket failed to produce potent and non-toxic pocket-specific entry inhibitors.

In the current work, the researchers used a high-throughput technique to screen a "library" containing hundreds of millions of peptides to identify the rare peptides that would bind to the pocket structure and inhibit HIV entry.

After identifying the most promising candidate peptides, the researchers analyzed the structure of these peptides bound to the target protein using x-ray crystallography at the NSLS. In this technique, researchers analyze how an extremely bright beam of x-rays, available only at synchrotron sources, bounces off and is refracted by the sample to determine the positions of individual atoms.

"These structures reveal details of how the peptides bind and guide the development of future inhibitors," said paper co-author Annie Heroux, a biologist and crystallography specialist at Brookhaven Lab.

This structure-assisted design led to the discovery of D-peptides with up to a 40,000-fold improved antiviral potency over previously reported D-peptides. The structures also suggest ways to engineer the peptides to reduce the chance of drug resistance.


'/>"/>

Contact: Karen McNulty Walsh
kmcnulty@bnl.gov
631-344-8350
DOE/Brookhaven National Laboratory
Source:Eurekalert

Related medicine news :

1. Potential New Cancer Gene Identified
2. Hepatitis E virus made impotent
3. Lack of Smell And Its Potential Risks
4. New Blood Thinner Pill - First Potential Alternative to Warfarin in 50 years
5. The Potential Of Cadaver Transplantation Programme In India
6. Unwed mothers find it difficult to attract potential life partner
7. Dermaseptins: Potent vaginal contraceptives
8. The potent anti-leukemia activity of Berbamine
9. Another Potential Of Stem Cells Discovered: Used For Growing Cartilage
10. Unpasteurised juices found to be potential health hazards
11. The many facets of milk and its health potential
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:5/26/2017)... ... May 26, 2017 , ... Rob Lowe acts as ... production of the series is on hiking in American. Viewers can reconnect with America ... great benefits of hiking. , Many consumers have looked for an inventive new place ...
(Date:5/26/2017)... ... May 26, 2017 , ... “THE FLINTHILLS FAMILY-Our Journey to the Cross”: the personal journey of ... Cross” is the creation of published authors, Bob and Margaret Massey. Bob Massey is ... is "panther quick and leather tough." His love for others is apparent in all ...
(Date:5/26/2017)... ... ... Jack: Against All Odds”: the story of Coach Cactus Jack and the impact he ... creation of published author, Walter Hubbard, a retired wildlife and fisheries biologist and pharmacy ... Walter and Jane have three adult children and a granddaughter. Walter and ...
(Date:5/24/2017)... ... May 24, 2017 , ... In ... choosing the most appropriate instruments for research and understanding the basic principles that ... webinar will focus on innovations in stereo microscopy for brightfield and fluorescence typically ...
(Date:5/24/2017)... California (PRWEB) , ... May 24, 2017 , ... ... through innovative medical image management and interpretation, has received U.S. Food and Drug ... , Nucleus.io is a web-based, scalable and secure cloud platform for medical image ...
Breaking Medicine News(10 mins):
(Date:5/15/2017)... Inc., a privately-held CNS pharmaceutical company based in ... disease (PD), has enrolled the first patient in the RASMET ... study involving patients with PD and taking place at 12 ... period. The first stage is open label and involves single ... Denver , Boca Raton ...
(Date:5/10/2017)... Global Health Intelligence (GHI), the leading healthcare data analytics ... 2017 ranking of the Best-Equipped Hospitals in Latin America ... GHI,s hospitals database for Latin America , which is ... database covers 86% of the hospitals in Latin ... each institution in key areas such as beds, medical specialties, ...
(Date:5/9/2017)... -- Zimmer Biomet Holdings, Inc. (NYSE and SIX: ZBH), ... has earned a spot on Forbes, "America,s ... ranked among 500 U.S. employers as well as in ... Services. The annual Forbes rankings ... of over 30,000 employees across 25 industries. The survey ...
Breaking Medicine Technology: