Atazanavir, better known as Reyataz, (3eky)
Show: Asymmetric Unit Biological Assembly
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Better Known as: Reyataz
Marketed By: Bristol-Myers Squibb
Major Indication: Human Immunodeficiency Virus Infection
Drug Class: HIV Protease Inhibitor
Date of FDA Approval (Patent Expiration): 2003 (2018)
2009 Sales: $1.2 Billion
Importance: It is the first HIV Protease inhibitor approved for once-daily dosing and also appears to have a reduced side-effect profile.
See Pharmaceutical Drugs for more information about other drugs and disorders.
When HIV infects a host, it directs the synthesis of several polyproteins. The maturation of the virus to its infectious form requires that these polyproteins be cleaved to their component proteins by HIV Protease. The subunits of come together to form a catalytic tunnel capable of binding the nascent peptides and cleaving them into their mature form. Within this tunnel lies , which contain the . These catalytic Asp residues carry out the hydrolytic cleavage of the polyprotein. Atazanavir to these conserved sequences within the HIV Protease tunnel, preventing the nascent polyproteins from entering. Unable to actively cleave the nascent proteins into their appropriate form, HIV is unable to mature and proliferate, allowing the patients immune system to fight off the infection more easily.[1][2]
The biggest difficulty with treating HIV is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to HIV Protease, See: HIV Protease Inhibitor Resistance Profile
↑ Spinelli S, Liu QZ, Alzari PM, Hirel PH, Poljak RJ. The three-dimensional structure of the aspartyl protease from the HIV-1 isolate BRU. Biochimie. 1991 Nov;73(11):1391-6. PMID:1799632
↑ Klei HE, Kish K, Lin PF, Guo Q, Friborg J, Rose RE, Zhang Y, Goldfarb V, Langley DR, Wittekind M, Sheriff S. X-ray crystal structures of human immunodeficiency virus type 1 protease mutants complexed with atazanavir. J Virol. 2007 Sep;81(17):9525-35. Epub 2007 May 30. PMID:17537865 doi:10.1128/JVI.02503-05
David Canner, Michal Harel
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This page was last modified 10:16, 29 February 2016.