Target Information
Target General Infomation | |||||
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Target ID |
T56915
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Former ID |
TTDS00320
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Target Name |
HIV protease
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Gene Name |
gag-pol
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Synonyms |
HIV-1 Retropepsin; HIV-1 peptidase; Retropepsin; gag-pol
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Target Type |
Successful
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Disease | HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | ||||
HIV-1 infection [ICD9: 001-139, 042; ICD10: B20-B24] | |||||
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26] | |||||
Viral infections [ICD9: 054.0, 054.1, 054.2, 054.3, 075, 771.2, 052, 053; ICD10: B01, B02, A60, B00, B27, G05.1, P35.2] | |||||
Unspecified [ICD code not available] | |||||
Function |
Integrase: Catalyzes viral DNA integration into the host chromosome, by performing a series of DNA cutting and joining reactions. This enzyme activity takes place after virion entry into a cell and reverse transcription of the RNA genome in dsDNA. The first step in the integration process is 3' processing. This step requires a complex comprising the viral genome, matrix protein, Vpr and integrase. This complex is called the pre- integration complex (PIC). The integrase protein removes 2 nucleotides from each 3' end of the viral DNA, leaving recessed CA OH's at the 3' ends. In the second step, the PIC enters cell nucleus. This process is mediated through integrase and Vpr proteins, and allows the virus to infect a non dividing cell. This ability to enter the nucleus is specific of lentiviruses, other retroviruses cannot and rely on cell division to access cell chromosomes. In the third step, termed strand transfer, the integrase protein joins the previously processed 3' ends to the 5' ends of strands of target cellular DNA at the site of integration. The 5'-ends are produced by integrase-catalyzed staggered cuts, 5 bp apart. A Y-shaped, gapped, recombination intermediate results, with the 5'-ends of the viral DNA strands and the 3' ends of target DNA strands remaining unjoined, flanking a gap of 5 bp. The last step is viral DNA integration into host chromosome. This involves host DNA repair synthesis in which the 5 bp gaps between the unjoined strands are filled in and then ligated. Since this process occurs at both cuts flanking the HIV genome, a 5 bpduplication of host DNA is produced at the ends of HIV-1 integration. Alternatively, Integrase may catalyze the excision of viral DNA just after strand transfer, this is termed disintegration.
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BioChemical Class |
Peptidase
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Target Validation |
T56915
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UniProt ID | |||||
EC Number |
EC 3.4.23.16
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Sequence |
PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMSLPGRWKPKMIGGIGGFIKVRQYD
QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF |
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Structure |
1A9M; 1AJV; 1AJX; 1AXA; 1BQM; 1BQN; 1D4H; 1D4I; 1D4J; 1DLO; 1DW6; 1EBK; 1EBW; 1EBY; 1EBZ; 1EC0; 1EC1; 1EC2; 1EC3; 1EET; 1G35; 1GNM; 1GNN; 1GNO; 1HAR; 1HBV; 1HEF; 1HEG; 1HIH; 1HMV; 1HNI; 1HNV; 1HOS; 1HPS; 1HPZ; 1HQE; 1HQU; 1HRH; 1HTE; 1HTF; 1HTG; 1HVI; 1HVK; 1HVP; 1HVU; 1HYS; 1IKV; 1IKW; 1IKX; 1IKY; 1J5O; 1KJH; 1MER; 1MES; 1MET; 1MEU; 1N5Y; 1N6Q; 1NPA; 1NPV; 1NPW; 1QE1; 1QMC;1R0A; 1RDH; 1RTD; 1RVL; 1RVM; 1RVN; 1RVO; 1RVP; 1RVQ; 1RVR; 1S6P; 1S6Q; 1S9E; 1S9G; 1SBG; 1SUQ; 1SV5; 1T03; 1T05; 1T7K; 1TV6; 1TVR; 1UWB; 1W5V; 1W5W; 1W5X; 1W5Y; 1YT9; 1ZP8; 1ZPA; 1ZSF; 1ZSR; 2AQU; 2B5J; 2B6A; 2BAN; 2BBB; 2BE2; 2EXF; 2G69; 2HB3; 2HMI; 2HNZ; 2HS1; 2HS2; 2I4D; 2I4U; 2I4V; 2I4W; 2I4X; 2I5J; 2IAJ; 2IC3; 2IDW; 2IEO; 2JZW; 2L45; 2L46; 2L4L; 2UXZ; 2UY0; 2VG5; 2VG6; 2VG7; 2X4U; 2YKM; 2YKN; 2ZD1; 2ZE2; 3AVI; 3BGR; 3DLK; 3GGA; 3GGV; 3GGX; 3HVT; 3IG1; 3IRX; 3IS9; 3ISN; 3ITH; 3JSM; 3JYT; 3K2P; 3K4V; 3KLE; 3KLF; 3KLG; 3KLH; 3KLI; 3NDT; 3NU3; 3NU4; 3NU5; 3NU6; 3NU9; 3NUJ; 3NUO; 3OK9; 3PSU;3QAA; 3QLH; 3QO9; 3TKG; 3TKW; 3TL9; 3TLH; 3V4I; 3V6D; 3V81; 3ZPS; 3ZPT; 3ZPU; 4COE; 4CP7; 4CPQ; 4CPR; 4CPS; 4CPT; 4CPU; 4CPW; 4CPX; 4DG1; 4G1Q; 4G8G; 4G8I; 4G9D; 4G9F; 4H4M; 4H4O; 4I2P; 4I2Q; 4ICL; 4ID5; 4IDK; 4IFV; 4IFY; 4IG0; 4IG3; 4KFB; 4KKO; 4KO0; 4LSL; 4LSN; 4MFB; 4O44; 4O4G; 4OJR; 4PQU; 4PUO; 4PWD; 4Q0B; 4QAG; 4U8W; 4WE1
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Drugs and Mode of Action | |||||
Drug(s) | Amprenavir | Drug Info | Approved | Human immunodeficiency virus infection | [536361] |
Atazanavir | Drug Info | Approved | Human immunodeficiency virus infection | [536361] | |
Darunavir | Drug Info | Approved | Human immunodeficiency virus infection | [536361] | |
Fosamprenavir | Drug Info | Approved | Human immunodeficiency virus infection | [550326] | |
Indinavir | Drug Info | Approved | Human immunodeficiency virus infection | [550326] | |
Ritonavir | Drug Info | Approved | Human immunodeficiency virus infection | [536361] | |
Saquinavir | Drug Info | Approved | Human immunodeficiency virus infection | [468045], [550326] | |
Tipranavir | Drug Info | Approved | Human immunodeficiency virus infection | [536361] | |
BI 201335 | Drug Info | Phase 3 | HCV infection | [550385] | |
ABT-450 | Drug Info | Phase 2 | HCV infection | [550189] | |
ACH-1625 | Drug Info | Phase 2 | HCV infection | [550195] | |
BMS 650032 | Drug Info | Phase 2 | HCV infection | [550384] | |
Danoprevir | Drug Info | Phase 2 | HCV infection | [551039] | |
DG-17 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [550282] | |
GS-9256 | Drug Info | Phase 2 | HCV infection | [550812] | |
KNI-272 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [544490] | |
MK-5172 | Drug Info | Phase 2 | HCV infection | [551141] | |
TMC-310911 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [522572] | |
Vaniprevir | Drug Info | Phase 2 | HCV infection | [551141] | |
BIT225 | Drug Info | Phase 1 | HCV infection | [550378] | |
CTP-298 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [523670] | |
PF-04776548 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [522912] | |
VX-500 | Drug Info | Phase 1 | HCV infection | [551770] | |
PPL-100 | Drug Info | Preclinical | Human immunodeficiency virus infection | [547190] | |
A-75925 | Drug Info | Discontinued in Phase 2 | Viral infections | [545458] | |
BRECANAVIR | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [547500] | |
MK-944a | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [547117] | |
MOZENAVIR MESILATE | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [545709] | |
R-87366 | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [546555] | |
Telinavir | Drug Info | Discontinued in Phase 2 | Human immunodeficiency virus infection | [545455] | |
GS-9005 | Drug Info | Discontinued in Phase 1/2 | Human immunodeficiency virus infection | [547700] | |
A-80987 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [545217] | |
CGP-53437 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [545200] | |
DMP-851 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [546493] | |
DPC-681 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [547252] | |
DPC-684 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [547253] | |
KNI-764 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [546821] | |
LASINAVIR | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [546180] | |
R-944 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [547553] | |
SPI-256 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [548265] | |
U-103017 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [546040] | |
U-96988 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [545725] | |
XM-323 | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [545218] | |
AG-1284 | Drug Info | Terminated | Human immunodeficiency virus infection | [545853] | |
AG-1350 | Drug Info | Terminated | Human immunodeficiency virus infection | [545680] | |
BAY-793 | Drug Info | Terminated | Human immunodeficiency virus infection | [545325] | |
BMS-182193 | Drug Info | Terminated | Human immunodeficiency virus infection | [545338] | |
BMS-186318 | Drug Info | Terminated | HIV-1 infection | [545817] | |
CGP-70726 | Drug Info | Terminated | HIV-1 infection | [546368] | |
Droxinavir hydrochloride | Drug Info | Terminated | Human immunodeficiency virus infection | [545796] | |
GE-20372A | Drug Info | Terminated | Human immunodeficiency virus infection | [545909] | |
GS-2992 | Drug Info | Terminated | Human immunodeficiency virus infection | [545882] | |
KNI-102 | Drug Info | Terminated | Human immunodeficiency virus infection | [545221] | |
Palinavir | Drug Info | Terminated | Human immunodeficiency virus infection | [545948] | |
PD-153103 | Drug Info | Terminated | HIV-1 infection | [545855] | |
SB-206343 | Drug Info | Terminated | HIV-1 infection | [545968] | |
U-75875 | Drug Info | Terminated | Human immunodeficiency virus infection | [545091] | |
Inhibitor | A-75925 | Drug Info | [534596] | ||
A-80987 | Drug Info | [534168] | |||
ABT-450 | Drug Info | [550189] | |||
ACH-1625 | Drug Info | [550195] | |||
AG-1350 | Drug Info | [551632], [551871] | |||
Amprenavir | Drug Info | [537180] | |||
BI 201335 | Drug Info | [550385] | |||
BIT225 | Drug Info | [550378] | |||
BMS 650032 | Drug Info | [550384] | |||
BMS-232632 | Drug Info | [535120] | |||
CGP-53437 | Drug Info | [533961] | |||
CTP-298 | Drug Info | [550016] | |||
Danoprevir | Drug Info | [551039] | |||
DG-17 | Drug Info | [544059] | |||
DMP-851 | Drug Info | [534751], [551871] | |||
DPC-681 | Drug Info | [526167], [551871] | |||
DPC-684 | Drug Info | [526167], [551871] | |||
Fosamprenavir | Drug Info | [537453] | |||
GE-20372A | Drug Info | [550896] | |||
GS-9005 | Drug Info | [550938] | |||
GS-9256 | Drug Info | [550812] | |||
Indinavir | Drug Info | [537031] | |||
LASINAVIR | Drug Info | [534465], [551871] | |||
MK-5172 | Drug Info | [551141] | |||
MK-944a | Drug Info | [525865] | |||
MOZENAVIR MESILATE | Drug Info | [534206] | |||
PPL-100 | Drug Info | [528026] | |||
R-87366 | Drug Info | [534336], [551871] | |||
R-944 | Drug Info | [550855] | |||
Ritonavir | Drug Info | [535213], [536999] | |||
Saquinavir | Drug Info | [536954] | |||
SPI-256 | Drug Info | [544193] | |||
Telinavir | Drug Info | [534397] | |||
TMC-310911 | Drug Info | [551655] | |||
U-103017 | Drug Info | [534077] | |||
U-96988 | Drug Info | [533813] | |||
Vaniprevir | Drug Info | [551141] | |||
VX-500 | Drug Info | [551770] | |||
XM-323 | Drug Info | [533902] | |||
Modulator | AG-1284 | Drug Info | [534231] | ||
Atazanavir | Drug Info | [556264] | |||
BAY-793 | Drug Info | [533674] | |||
BMS-182193 | Drug Info | [533713] | |||
BMS-186318 | Drug Info | [534225] | |||
BRECANAVIR | Drug Info | ||||
CGP-70726 | Drug Info | [525842] | |||
Darunavir | Drug Info | [528715] | |||
Droxinavir hydrochloride | Drug Info | [534332] | |||
GS-2992 | Drug Info | [550896] | |||
JG-365 | Drug Info | ||||
KH-164 | Drug Info | ||||
KNI-102 | Drug Info | [529151] | |||
KNI-272 | Drug Info | ||||
KNI-764 | Drug Info | ||||
Palinavir | Drug Info | [534383] | |||
PD-153103 | Drug Info | [550896] | |||
PF-04776548 | Drug Info | [522912] | |||
SB-206343 | Drug Info | [533812] | |||
Tipranavir | Drug Info | [556264] | |||
U-75875 | Drug Info | [533613] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
DRM | DRM Info | ||||
References | |||||
Ref 468045 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4813). | ||||
Ref 522572 | ClinicalTrials.gov (NCT00838162) A Study to Determine the Antiviral Activity of TMC310911 When Administered With Ritonavir in Treatment-Naive Human Immunodeficiency Virus - Type 1 (HIV-1) Infected Patients. U.S. National Institutes of Health. | ||||
Ref 522912 | 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. | ||||
Ref 523670 | ClinicalTrials.gov (NCT01458769) Pharmacokinetics, Safety & Tolerability of Isotopologs of Atazanavir (ATV), With Pharmacokinetic Comparison to Reyataz. U.S. National Institutes of Health. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 544490 | Metabolic Characterization of a Tripeptide Human Immunodeficiency Virus Type 1 Protease Inhibitor, KNI-272, in Rat Liver Microsomes. Antimicrob Agents Chemother. 1999 March; 43(3): 549-556. | ||||
Ref 545091 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002095) | ||||
Ref 545200 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002438) | ||||
Ref 545217 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002482) | ||||
Ref 545218 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002483) | ||||
Ref 545221 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002506) | ||||
Ref 545325 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002843) | ||||
Ref 545338 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002890) | ||||
Ref 545455 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003330) | ||||
Ref 545458 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003337) | ||||
Ref 545680 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004154) | ||||
Ref 545709 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004305) | ||||
Ref 545725 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004387) | ||||
Ref 545796 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004768) | ||||
Ref 545817 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004898) | ||||
Ref 545853 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005055) | ||||
Ref 545855 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005066) | ||||
Ref 545882 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005194) | ||||
Ref 545909 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005311) | ||||
Ref 545948 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005466) | ||||
Ref 545968 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005565) | ||||
Ref 546040 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006008) | ||||
Ref 546180 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006772) | ||||
Ref 546368 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007747) | ||||
Ref 546493 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008536) | ||||
Ref 546555 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008914) | ||||
Ref 546821 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010459) | ||||
Ref 547117 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013179) | ||||
Ref 547190 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013779) | ||||
Ref 547252 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014480) | ||||
Ref 547253 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014481) | ||||
Ref 547500 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016864) | ||||
Ref 547553 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017230) | ||||
Ref 547700 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018518) | ||||
Ref 548265 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023938) | ||||
Ref 522912 | 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. | ||||
Ref 525842 | Oral bioavailability of a poorly water soluble HIV-1 protease inhibitor incorporated into pH-sensitive particles: effect of the particle size and nutritional state. J Control Release. 2000 Aug 10;68(2):291-8. | ||||
Ref 525865 | 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 526167 | 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 528026 | Antiviral activity and cross-resistance profile of P-1946, a novel human immunodeficiency virus type 1 protease inhibitor. Antiviral Res. 2006 Jun;70(2):17-20. Epub 2006 Jan 20. | ||||
Ref 529151 | KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic. Chem Pharm Bull (Tokyo). 1991 Nov;39(11):3088-90. | ||||
Ref 533613 | Effects of U-75875, a peptidomimetic inhibitor of retroviral proteases, on simian immunodeficiency virus infection in rhesus monkeys. Antimicrob Agents Chemother. 1994 Jun;38(6):1277-83. | ||||
Ref 533674 | HIV protease inhibitor HOE/BAY 793, structure-activity relationships in a series of C2-symmetric diols. Bioorg Med Chem. 1995 May;3(5):559-71. | ||||
Ref 533713 | Antiviral properties of aminodiol inhibitors against human immunodeficiency virus and protease. Antimicrob Agents Chemother. 1995 Feb;39(2):374-9. | ||||
Ref 533812 | Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere. J Med Chem. 1994 Sep 16;37(19):3100-7. | ||||
Ref 533813 | Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors. J Med Chem. 1994 Sep 30;37(20):3200-4. | ||||
Ref 533902 | In vitro anti-human immunodeficiency virus (HIV) activity of XM323, a novel HIV protease inhibitor. Antimicrob Agents Chemother. 1993 Dec;37(12):2606-11. | ||||
Ref 533961 | 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 534077 | Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors. J Med Chem. 1995 Dec 22;38(26):4968-71. | ||||
Ref 534168 | 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 534206 | 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 534225 | Determination of BMS-186318 in dog, rat and monkey plasma by liquid chromatography-ionspray mass spectrometry. J Pharm Biomed Anal. 1995 Dec;14(1-2):43-8. | ||||
Ref 534231 | Exploring the energy landscapes of molecular recognition by a genetic algorithm: analysis of the requirements for robust docking of HIV-1 protease and FKBP-12 complexes. Proteins. 1996 Jul;25(3):342-53. | ||||
Ref 534332 | A mutation in human immunodeficiency virus type 1 protease at position 88, located outside the active site, confers resistance to the hydroxyethylurea inhibitor SC-55389A. Antimicrob Agents Chemother. 1997 Mar;41(3):515-22. | ||||
Ref 534336 | 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. | ||||
Ref 534383 | Antiviral properties of palinavir, a potent inhibitor of the human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1997 May;41(5):965-71. | ||||
Ref 534397 | Improvement of bioavailability of the HIV protease inhibitor SC-52151 in the beagle dog by coadministration of the CYP3A4 inhibitor, ketoconazole. Xenobiotica. 1997 May;27(5):489-97. | ||||
Ref 534465 | Quantitative determination of CGP 61755, a protease inhibitor, in plasma and urine by high-performance liquid chromatography and fluorescence detection. J Chromatogr B Biomed Sci Appl. 1997 Aug 15;696(1):123-30. | ||||
Ref 534596 | Solvation studies of DMP323 and A76928 bound to HIV protease: analysis of water sites using grand canonical Monte Carlo simulations. Protein Sci. 1998 Mar;7(3):573-9. | ||||
Ref 534751 | 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 535120 | Hollow-fiber unit evaluation of a new human immunodeficiency virus type 1 protease inhibitor, BMS-232632, for determination of the linked pharmacodynamic variable. J Infect Dis. 2001 Apr 1;183(7):1126-9. Epub 2001 Mar 1. | ||||
Ref 535213 | Peptide mimetic HIV protease inhibitors are ligands for the orphan receptor SXR. J Biol Chem. 2001 Sep 7;276(36):33309-12. Epub 2001 Jul 20. | ||||
Ref 536954 | PL-100, a novel HIV-1 protease inhibitor displaying a high genetic barrier to resistance: an in vitro selection study. J Med Virol. 2008 Dec;80(12):2053-63. | ||||
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