Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- PA-1050040
- DrugBank Accession Number
- DB06039
- Background
PA1050040, a second generation HIV-1 maturation inhibitor, is a chemical analog of Bevirimat (BVM). It inhibits virus replication by the same mechanism of action as BVM.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in HIV infection.
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Not Available
- Mechanism of action
Like protease inhibitors, PA-1050040 and other maturation inhibitors interfere with protease processing of newly translated HIV polyprotein precursor, called gag. This molecule contains a number of HIV proteins in a single polypeptide which is then cleaved by the enzyme protease to produce functional structural proteins. However, unlike the protease inhibitors, PA-1050040 binds the gag protein, not protease. Once bound to gag, PA-1050040 prevents a critical cleavage at a site called the capsid-SP1 junction. The resulting virus particles lack functional capsid protein and have structural defects, rendering them incapable of infecting other cells. For reasons not entirely understood, protease inhibitor-resistant HIV-1 was hypersensitive to PA-1050040 in vitro.
Target Actions Organism UGag polyprotein Not Available HIV-1 - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Not Available
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Not Available
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Not Available
- External Links
- PubChem Substance
- 347910320
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- HIV-1
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Gag polyprotein: Mediates, with Gag-Pol polyrotein, the essential events in virion assembly, including binding the plasma membrane, making the protein-protein interactions necessary to create spher...
- Gene Name
- gag
- Uniprot ID
- O93182
- Uniprot Name
- Gag polyprotein
- Molecular Weight
- 55673.715 Da
Drug created at November 18, 2007 18:29 / Updated at June 12, 2020 16:52