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Pyrophosphate Analog HIV-1 Reverse Transcriptase Inhibitors

20:00 EDT 22 Aug 2017 | NIH

The invention relates to compounds that inhibit HIV-1 DNA synthesis mediated by reverse transcriptase (RT). HIV-1 DNA synthesis by RT utilizes deoxynucleoside 5’-triphosphate (dNTP) as substrate and like many other enzymes, the reaction is reversible. Pyrophosphate analogs like imidodiphosphate strongly promote reverse reaction dNTP products containing the imidodiphosphate group instead of the naturally occurring pyrophosphate group. This imidodiphosphate-containing dNTP was found to be a potent inhibitor of the forward RT reaction. Whereas pyrophosphorolysis is limited by a nonchemical step, replacing the bridging oxygen of pyrophosphate with an imido group resulted in a change in the rate-limiting step, so that the imidodiphosphate-dependent reverse reaction was limited by chemistry. There exists, then, the potential to use pyrophosphate analogs therapeutically.

IC: 
NIEHS
NIH Ref. No.: 
E-210-2017/0
Applications: 
  • Anti-microbial
  • HIV therapeutic
Provider Technology ID: 
3156
Updated On: 
Aug 23, 2017
Date Published: 
Wednesday, August 23, 2017
Provider Classifications: 
Publications: 
Patent Application: 
62/542,600
Patent Authority: 
US
Licensing Contacts: 
Lead Inventor: 
Inventor IC: 
NIEHS
NIEHS
NIEHS
Inventor Lab URL: 
http://irp.nih.gov/pi/samuel-wilson
LPM FIrst Name: 
Michael
LPM Last Name: 
Shmilovich
LPM Address: 
31 Center Drive, Room 4A29 (MSC 2479)
LPM City: 
Bethesda
Inv Is lead: 
LPM Zip: 
20892-2479
LPM State: 
MD
LPM Phone: 
301-435-5019
LPM Suffix: 
J.D.
LPM Organization: 
NIH Office of Technology Transfer
LPM Fax: 
301-594-3080
DTDT Classification: 
AIDS (only)
Infectious Diseases (viral)
In vitro data available
DTDT Description: 
Infectious Diseases - Therapeutics - Anti-virals: AIDS
Infectious Diseases (viral)
In vitro data available
Pat Filing Date: 
2017-08-08
Development Stage Term: 
Collaboration Sought: 
Yes
Institute or Center: 
Collaboration Opportunity: 

The National Institute of Environmental Health Sciences seeks statements of capability or interest from parties interested in collaborative research to further develop and evaluate this technology. Please contact Sally E. Tilotta, PhD, Director, Office of Technology Transfer, National Institute of Environmental Health Sciences; Phone: (919) 316-4526; Email: sally.tilotta@nih.gov.

E Number Only: 
E-210-2017
Inventor First Name: 
Samuel
William
David
Inventor Last Name: 
Wilson
Beard
Shock

Original Article: Pyrophosphate Analog HIV-1 Reverse Transcriptase Inhibitors

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