Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT5FNQT)

• DTT Name: Human immunodeficiency virus Protease (HIV PR)
• Synonyms: HIV Retropepsin; HIV PR
• Gene Name: HIV PR
• DTT Type: Successful target; [1]
• BioChemical Class: Peptidase
• UniProt ID: POL_HV1B1
• TTD ID: T56915
• EC Number: EC 3.4.23.16
• Sequence:
  PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMSLPGRWKPKMIGGIGGFIKVRQYD
  QILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF
• 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.

Molecular Interaction Atlas (MIA) of This DTT

8 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amprenavir	DMLMXE0	Human immunodeficiency virus infection	1C62	Approved	[2]
Atazanavir	DMSYRBX	Human immunodeficiency virus infection	1C62	Approved	[3]
Darunavir	DMN3GCH	Human immunodeficiency virus infection	1C62	Approved	[4]
Fosamprenavir	DM4W9B3	Human immunodeficiency virus infection	1C62	Approved	[5]
Indinavir	DM0T3YH	Human immunodeficiency virus infection	1C62	Approved	[1]
Ritonavir	DMU764S	Human immunodeficiency virus infection	1C62	Approved	[6]
Saquinavir	DMG814N	Human immunodeficiency virus infection	1C62	Approved	[7]
Tipranavir	DM8HJX6	Human immunodeficiency virus infection	1C62	Approved	[8]

16 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BI 201335	DM3MXT8	Hepatitis C virus infection	1E51.1	Phase 3	[9]
ABT-450	DMFW860	Hepatitis C virus infection	1E51.1	Phase 2	[10]
ACH-1625	DMIVUFL	Hepatitis C virus infection	1E51.1	Phase 2	[11]
BMS 650032	DMQI43G	Hepatitis C virus infection	1E51.1	Phase 2	[12]
Danoprevir	DM20MDU	Hepatitis C virus infection	1E51.1	Phase 2	[13]
DG-17	DMS9Y1T	Human immunodeficiency virus infection	1C62	Phase 2	[14]
GS-9256	DMCZH5B	Hepatitis C virus infection	1E51.1	Phase 2	[15]
KNI-272	DMQZ5HF	Human immunodeficiency virus infection	1C62	Phase 2	[16]
MK-5172	DMSPWX6	Hepatitis C virus infection	1E51.1	Phase 2	[17]
TMC-310911	DMW145U	Human immunodeficiency virus infection	1C62	Phase 2	[18]
Vaniprevir	DMCF5E0	Hepatitis C virus infection	1E51.1	Phase 2	[17]
BIT225	DMGAR9Y	Hepatitis C virus infection	1E51.1	Phase 1	[19]
CTP-298	DMIKX01	Human immunodeficiency virus infection	1C62	Phase 1	[20]
PF-04776548	DMLGD0V	Human immunodeficiency virus infection	1C62	Phase 1	[21]
PPL-100	DMOYUPM	Human immunodeficiency virus infection	1C62	Phase 1	[22]
VX-500	DM8UTPJ	Hepatitis C virus infection	1E51.1	Phase 1	[23]

33 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
A-75925	DMF4MRD	Virus infection	1A24-1D9Z	Discontinued in Phase 2	[24]
BRECANAVIR	DMRVH2S	Human immunodeficiency virus infection	1C62	Discontinued in Phase 2	[25]
MK-944a	DMOZUPB	Human immunodeficiency virus infection	1C62	Discontinued in Phase 2	[26]
Mozenavir	DMLG7QB	Human immunodeficiency virus infection	1C62	Discontinued in Phase 2	[27]
R-87366	DMRZI3C	Human immunodeficiency virus infection	1C62	Discontinued in Phase 2	[28]
Telinavir	DM8OWID	Human immunodeficiency virus infection	1C62	Discontinued in Phase 2	[29]
GS-9005	DM7R126	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1/2	[30]
A-80987	DMGEWQ7	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[31]
CGP-53437	DMF0O2H	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[32]
DMP-851	DM412S9	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[33]
DPC-681	DM5HAG0	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[34]
DPC-684	DMS19VG	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[34]
KNI-764	DM6LTRC	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[35]
LASINAVIR	DMHEKIN	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[36]
R-944	DMJ2ZVW	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[37]
SPI-256	DMKGL2I	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[38]
U-103017	DMTVC3W	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[39]
U-96988	DML73BR	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[40]
XM-323	DMQKH07	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[41]
AG-1284	DMRI7YB	Human immunodeficiency virus infection	1C62	Terminated	[42]
AG-1350	DMALV1W	Human immunodeficiency virus infection	1C62	Terminated	[43]
BAY-793	DM69EHF	Human immunodeficiency virus infection	1C62	Terminated	[44]
BMS-182193	DMEDLHG	Human immunodeficiency virus infection	1C62	Terminated	[45]
BMS-186318	DMKZ3PW	Human immunodeficiency virus-1 infection	1C62	Terminated	[46]
CGP-70726	DMRLXC3	Human immunodeficiency virus-1 infection	1C62	Terminated	[47]
Droxinavir hydrochloride	DM6EJVF	Human immunodeficiency virus infection	1C62	Terminated	[48]
GE-20372A	DMGM3VP	Human immunodeficiency virus infection	1C62	Terminated	[49]
GS-2992	DMPSZR0	Human immunodeficiency virus infection	1C62	Terminated	[49]
KNI-102	DMXZNB2	Human immunodeficiency virus infection	1C62	Terminated	[50]
Palinavir	DMLKQUR	Human immunodeficiency virus infection	1C62	Terminated	[51]
PD-153103	DMVEXID	Human immunodeficiency virus-1 infection	1C62	Terminated	[49]
SB-206343	DMYFE23	Human immunodeficiency virus-1 infection	1C62	Terminated	[52]
U-75875	DMRBXEA	Human immunodeficiency virus infection	1C62	Terminated	[53]

2 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
JG-365	DMQP4VG	Discovery agent	N.A.	Investigative	[54]
KH-164	DMCE8Q9	Discovery agent	N.A.	Investigative	[55]

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