Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T56915 Target Info
Target Name Human immunodeficiency virus Protease (HIV PR)
Synonyms
HIV Retropepsin; HIV PR
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Target Type Successful Target
Gene Name HIV PR
Biochemical Class Peptidase
UniProt ID
POL_HV1B1
Co-Targets of This Target  Top
Co-Target Name Hepatitis C virus Serine protease NS3/4A (HCV NS3/4A) Successful Target
UniProt ID POLG_HCV1
Gene Name HCV NS3/4A
Synonyms
HCV Hepacivirin/NS4A; HCV NS3P/NS4A; HCV p70/NS4A
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Representative Drug(s) BMS 650032 Drug Info IC50 = 1 nM [1]
Co-Target Name Hepatitis C virus NS3 helicase (HCV NS3) Successful Target
UniProt ID POLG_HCV1 (1027-1657)
Gene Name HCV NS3
Synonyms
HCV Hepacivirin; HCV NS3P; HCV p70
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Representative Drug(s) BMS 650032 Drug Info EC50 = 1.2 nM [2]
Co-Target Name Human immunodeficiency virus Reverse transcriptase (HIV RT) Successful Target
UniProt ID POL_HV1B1
Gene Name HIV RT
Synonyms
HIV p66 RT; HIV Exoribonuclease H
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Representative Drug(s) Atazanavir Drug Info IC50 = 26 nM [3]
Co-Target Name Solute carrier family 47 member 1 (SLC47A1) Successful Target
UniProt ID S47A1_HUMAN
Gene Name SLC47A1
Synonyms
hMATE-1; Multidrug and toxin extrusion protein 1; MATE1; MATE-1
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Representative Drug(s) Ritonavir Drug Info IC50 = 80 nM [4]
Co-Target Name Albendazole monooxygenase (CYP3A4) Clinical trial Target
UniProt ID CP3A4_HUMAN
Gene Name CYP3A4
Synonyms
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) Ritonavir Drug Info IC50 = 30 nM Click to Show More [5]
2 Indinavir Drug Info IC50 = 150 nM [6]
3 Saquinavir Drug Info Ki = 170 nM [7]
4 Amprenavir Drug Info Ki = 260 nM [7]
Co-Target Name Liver organic anion transporter 2 (SLCO1B3) Literature-reported Target
UniProt ID SO1B3_HUMAN
Gene Name SLCO1B3
Synonyms
Solute carrier organic anion transporter family member 1B3; Solute carrier family 21 member 8; SLC21A8; Organic anion-transporting polypeptide 8; Organic anion transporter 8; OATP8; OATP1B3; OATP-8; Liver-specific organic anion transporter 2; LST2; LST-2
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Representative Drug(s) Atazanavir Drug Info Ki = 370 nM [8]
Co-Target Name Liver organic anion transporter 1 (SLCO1B1) Literature-reported Target
UniProt ID SO1B1_HUMAN
Gene Name SLCO1B1
Synonyms
Solute carrier organic anion transporter family member 1B1; Solute carrier family 21 member 6; Sodium-independent organic anion-transporting polypeptide 2; SLC21A6; OATPC; OATP2; OATP-C; OATP-2; Liver-specific organic anion transporter 1; LST1; LST-1
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Representative Drug(s) Ritonavir Drug Info IC50 = 700 nM [9]
Co-Target Name Cytochrome P450 3A5 (CYP3A5) Co-Target
UniProt ID CP3A5_HUMAN
Gene Name CYP3A5
Synonyms
Cytochrome P450-PCN3; CYPIIIA5
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Representative Drug(s) Ritonavir Drug Info Ki = 120 nM Click to Show More [7]
2 Amprenavir Drug Info Ki = 200 nM [7]
Co-Target Name UDP-glucuronosyltransferase 1A1 (UGT1A1) Co-Target
UniProt ID UD11_HUMAN
Gene Name UGT1A1
Synonyms
UGT1A1; Bilirubin-specific UDPGT isozyme 1; hUG-BR1; UDP-glucuronosyltransferase 1-1; UDPGT 1-1; UGT1*1; UGT1-01; UGT1.1; UDP-glucuronosyltransferase 1A isoform 1
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Representative Drug(s) Atazanavir Drug Info IC50 = 300 nM [10]
References  Top
REF 1 Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor. ACS Med Chem Lett. 2018 Jan 19;9(2):143-148.
REF 2 The discovery and optimization of naphthalene-linked P2-P4 Macrocycles as inhibitors of HCV NS3 protease. Bioorg Med Chem Lett. 2018 Jan 1;28(1):43-48.
REF 3 New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development. J Med Chem. 1998 Aug 27;41(18):3387-401.
REF 4 Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J Med Chem. 2013 Feb 14;56(3):781-795.
REF 5 Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25.
REF 6 Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2423-6.
REF 7 Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. Curr Drug Metab. 2005 Oct;6(5):413-54.
REF 8 Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63.
REF 9 The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery. Drug Metab Dispos. 2012 Aug;40(8):1641-8.
REF 10 Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir. J Med Chem. 2019 Apr 11;62(7):3553-3574.

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