Target Information
| Target General Information | Top | |||||
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| Target ID |
T02591
(Former ID: TTDI01959)
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| Target Name |
Human immunodeficiency virus Envelope glycoprotein gp160 (HIV env)
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| Synonyms |
Envelope glycoprotein gp160; Env polyprotein
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| Gene Name |
HIV env
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Human immunodeficiency virus disease [ICD-11: 1C60-1C62] | |||||
| Function |
Envelope glycoprotein gp160: Oligomerizes in the host endoplasmic reticulum into predominantly trimers. In a second time, gp160 transits in the host Golgi, where glycosylation is completed. The precursor is then proteolytically cleaved in the trans-Golgi and thereby activated by cellular furin or furin-like proteases to produce gp120 and gp41.
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| UniProt ID | ||||||
| Sequence |
MRVKEKYQHLWRWGWRWGTMLLGMLMICSATEKLWVTVYYGVPVWKEATTTLFCASDAKA
YDTEVHNVWATHACVPTDPNPQEVVLVNVTENFNMWKNDMVEQMHEDIISLWDQSLKPCV KLTPLCVSLKCTDLKNDTNTNSSSGRMIMEKGEIKNCSFNISTSIRGKVQKEYAFFYKLD IIPIDNDTTSYKLTSCNTSVITQACPKVSFEPIPIHYCAPAGFAILKCNNKTFNGTGPCT NVSTVQCTHGIRPVVSTQLLLNGSLAEEEVVIRSVNFTDNAKTIIVQLNTSVEINCTRPN NNTRKRIRIQRGPGRAFVTIGKIGNMRQAHCNISRAKWNNTLKQIASKLREQFGNNKTII FKQSSGGDPEIVTHSFNCGGEFFYCNSTQLFNSTWFNSTWSTEGSNNTEGSDTITLPCRI KQIINMWQKVGKAMYAPPISGQIRCSSNITGLLLTRDGGNSNNESEIFRPGGGDMRDNWR SELYKYKVVKIEPLGVAPTKAKRRVVQREKRAVGIGALFLGFLGAAGSTMGAASMTLTVQ ARQLLSGIVQQQNNLLRAIEAQQHLLQLTVWGIKQLQARILAVERYLKDQQLLGIWGCSG KLICTTAVPWNASWSNKSLEQIWNHTTWMEWDREINNYTSLIHSLIEESQNQQEKNEQEL LELDKWASLWNWFNITNWLWYIKLFIMIVGGLVGLRIVFAVLSIVNRVRQGYSPLSFQTH LPTPRGPDRPEGIEEEGGERDRDRSIRLVNGSLALIWDDLRSLCLFSYHRLRDLLLIVTR IVELLGRRGWEALKYWWNLLQYWSQELKNSAVSLLNATAIAVAEGTDRVIEVVQGACRAI RHIPRRIRQGLERILL Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | Ad35-GRIN/ENV | Drug Info | Phase 1 | Human immunodeficiency virus infection | [2] | |
| 2 | Ad5-ENVA-48 | Drug Info | Phase 1 | Human immunodeficiency virus-1 infection | [1] | |
| 3 | MGD014 | Drug Info | Phase 1 | Human immunodeficiency virus-1 infection | [3] | |
| 4 | PENNVAX-6 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [4] | |
| 5 | TBC-M4 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [5] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | GPG | Drug Info | Discontinued in Phase 1/2 | Human immunodeficiency virus infection | [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | MGD014 | Drug Info | [8] | |||
| 2 | GPG | Drug Info | [11] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | PENNVAX-6 | Drug Info | [9] | |||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Pentane-1,5-diamine | Ligand Info | |||||
| Structure Description | Crystal structure of C14linkmid/IQN17: a cross-linked inhibitor of HIV-1 entry bound to the gp41 hydrophobic pocket | PDB:1GZL | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | Yes | [12] |
| PDB Sequence |
WEEWDREIEN
637 YT
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | ClinicalTrials.gov (NCT00695877) Safety and Immune Response to a Recombinant Adenovirus HIV-1 Vaccine in Healthy Adults. U.S. National Institutes of Health. | |||||
| REF 2 | ClinicalTrials.gov (NCT01496989) Safety and Immunogenicity Study of HIV-MAG Vaccine +/- IL-12 and Ad35-GRIN/ENV in HIV-uninfected Volunteers. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT03570918) MGD014 in HIV-Infected Individuals on Suppressive Antiretroviral Therapy. U.S. National Institutes of Health. | |||||
| REF 4 | Clinical pipeline report, company report or official report of Inovio Pharmaceuticals. | |||||
| REF 5 | ClinicalTrials.gov (NCT00902824) Safety and Immunogenicity of TBC-M4, a MVA HIV Vaccine Alone or in a Prime-Boost Regimen With ADVAX DNA HIV Vaccine. U.S. National Institutes of Health. | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021646) | |||||
| REF 7 | A phase I double blind, placebo-controlled, randomized study of a multigenic HIV-1 adenovirus subtype 35 vector vaccine in healthy uninfected adults. PLoS One. 2012;7(8):e41936. | |||||
| REF 8 | Clinical pipeline report, company report or official report of MacroGenics. | |||||
| REF 9 | Company report (Inovio) | |||||
| REF 10 | A Phase 1 study to evaluate the safety and immunogenicity of a recombinant HIV type 1 subtype C-modified vaccinia Ankara virus vaccine candidate in Indian volunteers. AIDS Res Hum Retroviruses. 2009 Nov;25(11):1107-16. | |||||
| REF 11 | GPG-NH2 acts via the metabolite alphaHGA to target HIV-1 Env to the ER-associated protein degradation pathway. Retrovirology 2010, 7:20. | |||||
| REF 12 | Short constrained peptides that inhibit HIV-1 entry. Proc Natl Acad Sci U S A. 2002 Nov 12;99(23):14664-9. | |||||
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