Dolutegravir, HIV integrase inhibitor
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(1 Publication)
MW 419.4 Da. Potent HIV integrase inhibitor (IC50 = 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro). Inhibits HIV-1 viral replication (EC50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs). Prevents replication of several HIV-1 strains (EC50 values of 0.36-2.1 nM) that are resistant to nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), and protease inhibitors.
View Alternative Names
1,8-cineole 2-exo-monooxygenase, AChR, AL024364, Aging-associated gene 8 protein, Albendazole monooxygenase, Albendazole sulfoxidase, BILIQTL1, Bilirubin-specific UDPGT isozyme 1, CP33, CP34, CP3A4_HUMAN, CYP3, CYP3A, CYP3A3, CYP3A4, CYPIIIA3, CYPIIIA4, Cytochrome P450 3A3, Cytochrome P450 3A4, Cytochrome P450 HLp, Cytochrome P450 NF-25, Cytochrome P450 family 3 subfamily A polypeptide 4, Cytochrome P450 subfamily IIIA polypeptide 4, Cytochrome P450-PCN1, EC 2.4.1.17, GNT1, Glucocorticoid inducible P450, HLP, HUG-BR1, MGC126680, MGC12716, NF 25, Nifedipine oxidase, P450 III steroid inducible, P450 PCN1, P450, family III, P450C3, PHENOL/BILIRUBIN UDP GLUCURONOSYLTRANSFERASE, Quinine 3-monooxygenase, RP23 167I12.6, SGMR1_HUMAN, SIG-1R, SR-BP, SR31747-binding protein, Sigma 1-type opioid receptor, Sigma non-opioid intracellular receptor 1, Sigma1-receptor, Sigma1R, Sigmar1, Slc18a3, Solute carrier family 18 (vesicular acetylcholine) member 3, Solute carrier family 18 (vesicular monoamine) member 3, Solute carrier family 18 member 3, Taurochenodeoxycholate 6-alpha-hydroxylase, UD11_HUMAN, UDP GLYCOSYLTRANSFERASE 1, UDP glucuronosyltransferase 1 1 [Precursor], UDP glucuronosyltransferase 1 family polypeptide A1, UDP-glucuronosyltransferase 1-1, UDP-glucuronosyltransferase 1-A, UDP-glucuronosyltransferase 1A1, UDPGT, UDPGT 1-1, UGT-1A, UGT1, UGT1*1, UGT1-01, UGT1.1, URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE, BILIRUBIN/PHENOL, URIDINE DIPHOSPHATE GLYCOSYLTRANSFERASE 1, URIDINE DIPHOSPHATE GLYCOSYLTRANSFERASE 1 FAMILY, POLYPEPTIDE A1, VACHT_HUMAN, Vesicular acetylcholine transporter, bilirubin UDP glucuronosyltransferase 1 1, bilirubin UDP glucuronosyltransferase isozyme 1, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, hSigmaR1, mSigmaR1, opioid receptor, sigma 1, opioid receptor, sigma 1 isoform 1, rVAT
- Chemical Structure
Lab
Chemical Structure - Dolutegravir, HIV integrase inhibitor (AB231511)
2D chemical structure image of ab231511, Dolutegravir, HIV integrase inhibitor
Properties and storage information
Shipped at conditions
Appropriate short-term storage conditions
Appropriate long-term storage conditions
Supplementary information
This supplementary information is collated from multiple sources and compiled automatically.
Biological function summary
CYP3A4 is important in metabolizing nearly 50% of all drugs including integrase inhibitors like dolutegravir used in HIV therapy. This enzyme mediates the oxidative metabolism impacting drug absorption and clearance rates. VAChT facilitates synaptic transmission by packaging acetylcholine while Sigma1-receptor is involved in cell signaling and stress response modulation. UGT1A1 is essential in bilirubin clearance and metabolizing various xenobiotics and endogenous substances. These targets are not part of a singular complex but exhibit essential roles individually within their respective pathways.
Pathways
These proteins perform integral roles in different biological functions. CYP3A4 is central in the drug metabolism pathway alongside other CYPs influencing the pharmacokinetics of many medications. VAChT is involved in cholinergic neurotransmission critical for nerve signal propagation. Similarly Sigma1-receptor is part of the neuroprotective and apoptotic pathways related to calcium signaling and lipid transport. UGT1A1 is prominently featured in the glucuronidation pathway a phase II drug metabolism process closely linked with heme and bilirubin metabolism. These proteins have specific yet interconnected pathways functioning with various related proteins.
Publications (1)
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The Journal of biological chemistry 295:13023-13030 PubMed32719008
2020
Applications
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Species
Unspecified reactive species
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