Navigation Links
Scripps Research scientists find two compounds that lay the foundation for a new class of AIDS drug
Date:2/3/2010

>

That's what the Scripps Research team set out to learn in the new study, which was funded by a grant to the Olson lab from the National Institutes of Health to seek ways to combat drug-resistance in HIV.

To accomplish this goal, the team procured a "library" of 384 compound fragments that had been compiled by a company called Active Sight. Screening fragments rather than larger compounds has become more popular over the last several years, Perryman explained, since using these smaller pieces is a more efficient way to find promising structures than using libraries of large compounds. In addition, fragments can be extended, combined, and modified using "structure-based drug design" in a way that makes them fit tightly into the right binding sites, without displaying the unwanted interactions that sometimes come with larger molecules. Using libraries of much larger, "lead-like" compounds is less efficient, and those large compounds are less extendable.

Since the HIV protease molecule is in constant motion, the team of scientists, which included members of Scripps Research Professor John Elder's lab, first crystallized the molecule in various different conformations. The scientists then screened a library of fragments against these crystals to see if any of them bound and characterized the structural features of the results using the Stanford Synchrotron Radiation Lightsource (SSRL). Stout notes that, in total, the project conducted a massive screen of more than 800 crystals producing more than 400 data sets, a feat made possible by SSRL's robotic capabilities.

In their initial experiments, the scientists met with partial successenough to establish a proof-of-conceptas one fragment attached to the "eye site" between the tip of a flap and the top of the active site's wall. However, the large active site of the molecule tended to be problematic, interfering with the scientists' goal of searching for fragments that bind to alternate
'/>"/>

Contact: Keith McKeown
kmckeown@scripps.edu
858-784-8134
Scripps Research Institute
Source:Eurekalert

Page: 1 2 3 4 5

Related biology news :

1. Scripps scientists discover fluorescence in key marine creature
2. Scripps research team blocks bacterial communication system to prevent deadly staph infections
3. Scripps scientists develop new tests that identify lethal prion strains quickly and accurately
4. Scripps Research discovery leads to broad potential applications in CovX-Pfizer deal
5. Scripps expedition provides new baseline for coral reef conservation
6. Bright lights: Mystery of glowing antibody solved by Scripps research scientists
7. Fishing throws targeted species off balance, Scripps study shows
8. Scripps Oceanography Research pegs ID of red tide killer
9. Scripps Research Institute awarded patent for remarkable chemical technology
10. Scripps research scientists reveal key structure from ebola virus
11. Scripps study sets high economic value on threatened Mexican mangroves
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:10/15/2014)... The Ebola virus is spreading rapidly and to an ... experienced in the past and the virus shows a ... been recorded before. For this reason, the German National ... of Science and Engineering, and the Union of the ... statement on the Ebola epidemic today. , In the ...
(Date:10/15/2014)... 44th Rosenstiel Award for Distinguished Work in Biomedical Science ... mechanisms of genomic instability and its implications for the ... alumnus to win the Rosenstiel Award; the first, Rod ... is the Charles A. Janeway Professor of Pediatrics and ... investigator at the Howard Hughes Medical Institute at Boston ...
(Date:10/14/2014)... Cancer Research shows SIRT6—a protein known to inhibit ... development of skin cancers by turning on an enzyme ... cells. , Previously considered protective, SIRT6 is part of ... regulate genomic stability and prevent some of the genetic ... which can lead to cancer. This study, in the ...
Breaking Biology News(10 mins):Academies call for consequences from the Ebola virus epidemic 2Academies call for consequences from the Ebola virus epidemic 3Academies call for consequences from the Ebola virus epidemic 4Academies call for consequences from the Ebola virus epidemic 5Brandeis awards 44th Rosenstiel Award to pioneering geneticist Fred Alt 2Two-faced gene: SIRT6 prevents some cancers but promotes sun-induced skin cancer 2
... World leaders have made pitiful progress on their guarantee to ... a paper published today (Friday 15th June) in Science ... researchers have reviewed commitments made by governments to protect the ... over the past 20 years. At the World ...
... found a surprising connection between a key DNA-repair process and ... and other chronic conditions. The discovery promises to open up ... could ultimately yield novel treatments for a wide variety of ... it goes against current dogma about the role of DNA ...
... the Instituto Andaluz de Ciencias de la Tierra and other ... published in the prestigious journal Reviews of Modern Physics ... different countries has published the most comprehensive study ever done ... important contemporary issues in a field of research that is ...
Cached Biology News:A sea of broken promises 2Scientists tie DNA repair to key cell signaling network 2Spanish scientist participate in the most comprehensive study ever done on ice 2
(Date:10/22/2014)... Involution Studios , a healthcare ... new infographic, Understanding Ebola . The goal ... easy to follow informative tool for anyone wanting to ... and prevention. , "As the news has spread in ... outbreak represents not only a healthcare crisis with global ...
(Date:10/22/2014)... Currently offering a comprehensive portfolio ... Weighing, Rice Lake, and Ohaus, Pipette.com has added ... Sartorius CPA Semi-Micro Balance is ideal for lab ... user-friendly laboratory balance. , Sartorius is a global ... balances are well known for their high performance, ...
(Date:10/22/2014)... 2014 Physicians Choice Laboratory Services ... menu, which enables healthcare providers to individualize therapeutic ... evidence-based results, healthcare providers are better able to ... while minimizing risks for adverse drug reactions and ... the FDA [1] more than 2.2 million adverse ...
(Date:10/22/2014)... --  Synthetic Biologics, Inc. (NYSE MKT: SYN), a ... and diseases, announced today that the U.S. Patent and ... a composition of matter patent application that covers the ... This is Synthetic Biologics, first allowed patent application directly ... the Company,s extensive C. difficile patent estate. ...
Breaking Biology Technology:Involution Studios' Ebola Infographic Provides Key Disease Information and Statistics at a Glance 2Pipette.com Launches the Addition of Sartorius CPA Semi-Micro Balance to Their Product Portfolio with Special Promotional Pricing 2Pipette.com Launches the Addition of Sartorius CPA Semi-Micro Balance to Their Product Portfolio with Special Promotional Pricing 3PCLS Announces Expansion of Cardiovascular Pharmacogenetic Testing Menu 2PCLS Announces Expansion of Cardiovascular Pharmacogenetic Testing Menu 3Synthetic Biologics Announces Allowance of Key U.S. Composition of Matter Patent for C. difficile Program 2Synthetic Biologics Announces Allowance of Key U.S. Composition of Matter Patent for C. difficile Program 3Synthetic Biologics Announces Allowance of Key U.S. Composition of Matter Patent for C. difficile Program 4
... On June 19 and 20 at the Drake Hotel ... real estate, legal, engineering and due diligence providers gathered ... on the small and middle markets ($10 million to ... such as "maximizing the value of your brand and ...
... Madison, Wis . - In a merging of complementary companies, ... new Vitamin D products, has acquired Proventiv Therapeutics, LLC, of ... $25 million in venture capital from Canadian and American investors. ... of Bone Care International , which was acquired last ...
... and natural gas have sparked a race to make transportation ... and gasoline containing ethanol are starting to make an impact ... has also fueled a race to find new sources for ... many modern plastics, drugs, and fuels. Behind the scenes, American ...
Cached Biology Technology:Some great insights into the current Mergers & Acquisitions Market 2Some great insights into the current Mergers & Acquisitions Market 3Some great insights into the current Mergers & Acquisitions Market 4Some great insights into the current Mergers & Acquisitions Market 5Canadian firm buys Proventiv Therapeutics, makes ex-Bone Care exec CEO 2Canadian firm buys Proventiv Therapeutics, makes ex-Bone Care exec CEO 3UW prof turns sugar into diesel fuel, chemicals 2UW prof turns sugar into diesel fuel, chemicals 3
... Thermo Savant SpeedVac Concentrators set the standard ... SC110A SpeedVac uses a combination of centrifugal force, ... a single run., SC110A comes equipped with:, , ... chemical compatibility , ...
... Savant SpeedVac™ Concentrators set the standard for sample ... SpeedVac with large chamber uses a combination of ... samples in a single run. , SC210A comes ... for long lasting chemical compatibility ...
... (for aqueous, other low volatility and noxious ... to specific applications of molecular biology and ... heat-labile samples. The RC systems can be ... and a wide selection of rotors (eliminating ...
... Jouan RC Standard Bio for vacuum ... of molecular biology and biochemistry for rapid ... RC systems can be expanded with pumps, ... selection of rotors (eliminating sample loss by ...
Biology Products: