Target General Infomation
Target ID
T56915 (Former ID: TTDS00320)
Target Name
Human immunodeficiency virus Protease (HIV PR)
Synonyms
HIV Retropepsin; HIV PR
Gene Name
HIV PR
Target Type
Successful target
[1]
Disease [+] 1 Target-related Diseases +
1 Human immunodeficiency virus disease [ICD-11: 1C60-1C62]
Function
Gag-Pol polyprotein: Mediates, with Gag polyprotein, the essential events in virion assembly, including binding the plasma membrane, making the protein-protein interactions necessary to create spherical particles, recruiting the viral Env proteins, and packaging the genomic RNA via direct interactions with the RNA packaging sequence (Psi). Gag-Pol polyprotein may regulate its own translation, by the binding genomic RNA in the 5'-UTR. At low concentration, the polyprotein would promote translation, whereas at high concentration, the polyprotein would encapsidate genomic RNA and then shut off translation.
BioChemical Class
Peptidase
UniProt ID
POL_HV1B1
EC Number
EC 3.4.23.16
Sequence
PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMSLPGRWKPKMIGGIGGFIKVRQYD
QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF
Drugs and Modes of Action
Approved Drug(s) [+] 8 Approved Drugs +
1 Amprenavir Drug Info Approved Human immunodeficiency virus infection [2]
2 Atazanavir Drug Info Approved Human immunodeficiency virus infection [2]
3 Darunavir Drug Info Approved Human immunodeficiency virus infection [2]
4 Fosamprenavir Drug Info Approved Human immunodeficiency virus infection [3]
5 Indinavir Drug Info Approved Human immunodeficiency virus infection [3]
6 Ritonavir Drug Info Approved Human immunodeficiency virus infection [2]
7 Saquinavir Drug Info Approved Human immunodeficiency virus infection [3], [4]
8 Tipranavir Drug Info Approved Human immunodeficiency virus infection [2]
Clinical Trial Drug(s) [+] 16 Clinical Trial Drugs +
1 BI 201335 Drug Info Phase 3 Hepatitis C virus infection [5]
2 ABT-450 Drug Info Phase 2 Hepatitis C virus infection [6]
3 ACH-1625 Drug Info Phase 2 Hepatitis C virus infection [7]
4 BMS 650032 Drug Info Phase 2 Hepatitis C virus infection [8]
5 Danoprevir Drug Info Phase 2 Hepatitis C virus infection [9]
6 DG-17 Drug Info Phase 2 Human immunodeficiency virus infection [10]
7 GS-9256 Drug Info Phase 2 Hepatitis C virus infection [11]
8 KNI-272 Drug Info Phase 2 Human immunodeficiency virus infection [12]
9 MK-5172 Drug Info Phase 2 Hepatitis C virus infection [13]
10 TMC-310911 Drug Info Phase 2 Human immunodeficiency virus infection [14]
11 Vaniprevir Drug Info Phase 2 Hepatitis C virus infection [13]
12 BIT225 Drug Info Phase 1 Hepatitis C virus infection [15]
13 CTP-298 Drug Info Phase 1 Human immunodeficiency virus infection [16]
14 PF-04776548 Drug Info Phase 1 Human immunodeficiency virus infection [17]
15 TMB-607 Drug Info Phase 1 Human immunodeficiency virus infection [18]
16 VX-500 Drug Info Phase 1 Hepatitis C virus infection [19]
Discontinued Drug(s) [+] 33 Discontinued Drugs +
1 A-75925 Drug Info Discontinued in Phase 2 Virus infection [20]
2 BRECANAVIR Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [21]
3 MK-944a Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [22]
4 MOZENAVIR MESILATE Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [23]
5 R-87366 Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [24]
6 Telinavir Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [25]
7 GS-9005 Drug Info Discontinued in Phase 1/2 Human immunodeficiency virus infection [26]
8 A-80987 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [27]
9 CGP-53437 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [28]
10 DMP-851 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [29]
11 DPC-681 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [30]
12 DPC-684 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [31]
13 KNI-764 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [32]
14 LASINAVIR Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [33]
15 R-944 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [34]
16 SPI-256 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [35]
17 U-103017 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [36]
18 U-96988 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [37]
19 XM-323 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [38]
20 AG-1284 Drug Info Terminated Human immunodeficiency virus infection [40]
21 AG-1350 Drug Info Terminated Human immunodeficiency virus infection [41]
22 BAY-793 Drug Info Terminated Human immunodeficiency virus infection [42]
23 BMS-182193 Drug Info Terminated Human immunodeficiency virus infection [43]
24 BMS-186318 Drug Info Terminated Human immunodeficiency virus-1 infection [44]
25 CGP-70726 Drug Info Terminated Human immunodeficiency virus-1 infection [45]
26 Droxinavir hydrochloride Drug Info Terminated Human immunodeficiency virus infection [46]
27 GE-20372A Drug Info Terminated Human immunodeficiency virus infection [47]
28 GS-2992 Drug Info Terminated Human immunodeficiency virus infection [48]
29 KNI-102 Drug Info Terminated Human immunodeficiency virus infection [49]
30 Palinavir Drug Info Terminated Human immunodeficiency virus infection [50]
31 PD-153103 Drug Info Terminated Human immunodeficiency virus-1 infection [51]
32 SB-206343 Drug Info Terminated Human immunodeficiency virus-1 infection [52]
33 U-75875 Drug Info Terminated Human immunodeficiency virus infection [53]
Preclinical Drug(s) [+] 1 Preclinical Drugs +
1 PPL-100 Drug Info Preclinical Human immunodeficiency virus infection [39]
Mode of Action [+] 2 Modes of Action +
Inhibitor [+] 39 Inhibitor drugs +
1 Amprenavir Drug Info [54]
2 Fosamprenavir Drug Info [58]
3 Indinavir Drug Info [1]
4 Ritonavir Drug Info [59], [60]
5 Saquinavir Drug Info [61]
6 BI 201335 Drug Info [5]
7 BMS 650032 Drug Info [8]
8 ABT-450 Drug Info [6]
9 ACH-1625 Drug Info [7]
10 Danoprevir Drug Info [9]
11 DG-17 Drug Info [62]
12 GS-9256 Drug Info [11]
13 MK-5172 Drug Info [13]
14 TMC-310911 Drug Info [64]
15 Vaniprevir Drug Info [13]
16 BIT225 Drug Info [15]
17 CTP-298 Drug Info [65]
18 TMB-607 Drug Info [18]
19 VX-500 Drug Info [19]
20 A-75925 Drug Info [66]
21 MK-944a Drug Info [68]
22 MOZENAVIR MESILATE Drug Info [69]
23 R-87366 Drug Info [70], [71]
24 Telinavir Drug Info [72]
25 GS-9005 Drug Info [73]
26 A-80987 Drug Info [74]
27 CGP-53437 Drug Info [75]
28 DMP-851 Drug Info [71], [76]
29 DPC-681 Drug Info [71], [77]
30 DPC-684 Drug Info [71], [77]
31 LASINAVIR Drug Info [71], [79]
32 R-944 Drug Info [80]
33 SPI-256 Drug Info [81]
34 U-103017 Drug Info [82]
35 U-96988 Drug Info [83]
36 XM-323 Drug Info [84]
37 PPL-100 Drug Info [85]
38 AG-1350 Drug Info [71], [87]
39 GE-20372A Drug Info [93]
Modulator [+] 21 Modulator drugs +
1 Atazanavir Drug Info [55], [56]
2 Darunavir Drug Info [57]
3 Tipranavir Drug Info [56]
4 KNI-272 Drug Info [63]
5 PF-04776548 Drug Info [17]
6 BRECANAVIR Drug Info [67]
7 KNI-764 Drug Info [78]
8 AG-1284 Drug Info [86]
9 BAY-793 Drug Info [88]
10 BMS-182193 Drug Info [89]
11 BMS-186318 Drug Info [90]
12 CGP-70726 Drug Info [91]
13 Droxinavir hydrochloride Drug Info [92]
14 GS-2992 Drug Info [93]
15 KNI-102 Drug Info [94]
16 Palinavir Drug Info [95]
17 PD-153103 Drug Info [93]
18 SB-206343 Drug Info [96]
19 U-75875 Drug Info [97]
20 JG-365 Drug Info [98]
21 KH-164 Drug Info [99]
Target Profiles in Patients
Drug Resistance
 Mutation (DRM)
Target-Related Models and Studies
Target Validation
Target QSAR Model
References
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REF 15 2011 Pipeline of Biotron.
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REF 17 ClinicalTrials.gov (NCT01045317) A Study To Investigate The Clearance Of PF-04776548 From The Body Following A Very Low (Micro) Dose Of The Compound Using A Low Level Of Radiotracer To Help Quantify Expected Low Concentrations Of PF-04776548 In The Body. U.S. National Institutes of Health.
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REF 60 Peptide mimetic HIV protease inhibitors are ligands for the orphan receptor SXR. J Biol Chem. 2001 Sep 7;276(36):33309-12.
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REF 68 Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. J Med Chem. 2000 Sep 7;43(18):3386-99.
REF 69 Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450. Chem Biol. 1996 Apr;3(4):301-14.
REF 70 In vitro and ex vivo anti-human immunodeficiency virus (HIV) activities of a new water-soluble HIV protease inhibitor, R-87366, containing (2S,3S)-3-amino-2-hydroxy-4-phenylbutanoic acid. Biol Pharm Bull. 1997 Feb;20(2):175-80.
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REF 73 WO patent application no. 2003,0906,90, Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such.
REF 74 Human serum alpha 1 acid glycoprotein reduces uptake, intracellular concentration, and antiviral activity of A-80987, an inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1996 Jun;40(6):1491-7.
REF 75 CGP 53437, an orally bioavailable inhibitor of human immunodeficiency virus type 1 protease with potent antiviral activity. Antimicrob Agents Chemother. 1993 Oct;37(10):2087-92.
REF 76 Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors. Chem Biol. 1998 Oct;5(10):597-608.
REF 77 DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. Antimicrob Agents Chemother. 2001 Nov;45(11):3021-8.
REF 78 JE-2147: a dipeptide protease inhibitor (PI) that potently inhibits multi-PI-resistant HIV-1. Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8675-80.
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