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Entry inhibitor

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that binds to domain 2 of CD4 and interferes with post-attachment steps required for the entry of HIV-1 virus particles into host cells and prevents the viral transmission that occurs via cell-cell fusion.
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Other agents are under investigation for their ability to interact with the proteins involved in HIV entry and the possibility that they may serve as entry inhibitors.
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binds to CD4. b12 seems to serve as a natural entry inhibitor in some individuals. It is hoped that further study of b12 may lead to an effective HIV vaccine.
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that targets, among others sites, the GP41 transmembrane glycoprotein. The trials are being conducted by Virionyx, a New Zealand Company.
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was being developed to interfere with interaction between HIV and CXCR4, but showed little useful antiviral activity in recent trials.
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binds to gp41 and interferes with its ability to approximate the two membranes. It is also referred to as a "fusion inhibitor."
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Biswas P, Tambussi G, Lazzarin A (May 2007). "Access denied? The status of co-receptor inhibition to counter HIV entry".
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An HIV virion binds to a CD4+ human cell. The two bottom pictures depict two proposed models of HIV fusion with the cell.
430:) potently block viral entry of diverse strains and are being developed and studied as potential microbicide candidates 376:, an agent similar to maraviroc and vicriroc. Clinical trials were halted in 2005 over concerns about the drug's safety. 1639: 1195: 976: 946: 1992: 1649: 1533: 17: 1659: 1644: 1307: 1295: 825:"CD4-specific designed ankyrin repeat proteins are novel potent HIV entry inhibitors with unique characteristics" 1539: 776:"Direct inactivation of human immunodeficiency virus type 1 by a novel small-molecule entry inhibitor, DCM205" 969: 1744: 2031: 1816: 1726: 1707: 1594: 1555: 955: 384: 349: 447:
is a synthesized peptide which binds to gp41, preventing fusion of the virus with a cell membrane.
1980: 1576: 951: 86: 1654: 727:"Griffithsin, a potent HIV entry inhibitor, is an excellent candidate for anti-HIV microbicide" 1762: 823:
Schweizer A, Rusert P, Berlinger L, Ruprecht CR, Mann A, Corthésy S, et al. (July 2008).
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Sulkowski MS, Kang M, Matining R, Wyles D, Johnson VA, Morse GD, et al. (March 2014).
991: 415:, an integrase inhibitor. DCM205 has been reported to inactivate HIV-1 particles directly 8: 1669: 1528: 1400: 1318: 1117: 996: 307: 126: 110: 920: 895: 851: 824: 800: 775: 756: 647: 622: 592: 543: 516: 497: 725:
Emau P, Tian B, O'keefe BR, Mori T, McMahon JB, Palmer KE, et al. (August 2007).
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638: 583: 1986: 992: 702: 685: 438: 423: 82: 74: 2025: 1752: 1502: 1337: 1223: 485: 434: 412: 405:, a substance derived from algae, appears to have entry inhibitor properties. 260: 250: 209: 173: 911: 1806: 1796: 1377: 1367: 1185: 1142: 1137: 1132: 1094: 1074: 1004: 929: 860: 809: 752: 711: 669: 656: 601: 552: 493: 162: 142: 134: 774:
Duong YT, Meadows DC, Srivastava IK, Gervay-Hague J, North TW (May 2007).
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Entry inhibitors work by interfering with one aspect of this process.
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HIV entry into a human cell requires the following steps in sequence.
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Williamson MP, McCormick TG, Nance CL, Shearer WT (December 2006).
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Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
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Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
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Wilen, Craig B.; Tilton, John C.; Doms, Robert W. (2012).
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Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
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by gp41, which approximates the membrane of HIV and the
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Pugach P, Ketas TJ, Michael E, Moore JP (August 2008).
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and is thought to act primarily as an entry inhibitor.
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in the human immune system, also called CD4+ T cells
198:, another chemokine co-receptor found on CD4+ cells 133:infection. This class of drugs interferes with the 215: 2023: 1572:Dolutegravir/emtricitabine/tenofovir alafenamide 515:Xiao, Tianshu; Cai, Yongfei; Chen, Bing (2021). 1630:Emtricitabine/rilpivirine/tenofovir alafenamide 1550:Bictegravir/emtricitabine/tenofovir alafenamide 565: 1635:Emtricitabine/rilpivirine/tenofovir disoproxil 1121:(Integrase strand transfer inhibitors (INSTI)) 690:The Journal of Allergy and Clinical Immunology 113:(MOA) of two entry inhibitor, 5-Helix and C37. 1583:Dolutegravir/lamivudine/tenofovir alafenamide 977: 172:, a protein receptor found on the surface of 1605:Efavirenz/emtricitabine/tenofovir disoproxil 1589:Dolutegravir/lamivudine/tenofovir disoproxil 517:"HIV-1 entry and membrane fusion inhibitors" 614: 514: 465: 109:An illustration of HIV entry mechanism and 1600:Doravirine/lamivudine/tenofovir disoproxil 984: 970: 204:, an HIV protein, closely associated with 141:to a human cell. By blocking this step in 1610:Efavirenz/lamivudine/tenofovir disoproxil 954:at the U.S. National Library of Medicine 919: 850: 840: 799: 742: 701: 646: 591: 542: 532: 328: 270:The entry of the viral core into the cell 1877:Zinc finger protein transcription factor 116: 104: 340:, a monoclonal antibody that binds CCR5 14: 2024: 965: 780:Antimicrobial Agents and Chemotherapy 29: 1625:Emtricitabine/tenofovir alafenamide 224:The binding of HIV surface protein 24: 1640:Emtricitabine/tenofovir disoproxil 900:The Journal of Infectious Diseases 277: 25: 2043: 940: 663: 474:Expert Opinion on Pharmacotherapy 411:, is a small molecule based on L- 290:, preventing an interaction with 2013:. Formerly or rarely used agent. 1650:Lamivudine/nevirapine/zidovudine 1534:Abacavir/dolutegravir/lamivudine 947:Fusion Inhibitor Resource Center 744:10.1111/j.1600-0684.2007.00242.x 34: 1817:Epigallocatechin gallate (EGCG) 1660:Lamivudine/tenofovir disoproxil 1645:Lamivudine/nevirapine/stavudine 887: 867: 387:. It has been found to bind to 216:Binding, fusion, entry sequence 1540:Abacavir/lamivudine/zidovudine 816: 767: 731:Journal of Medical Primatology 718: 677: 559: 508: 437:antibody is in phase II human 13: 1: 572:Cold Spring Harb Perspect Med 568:"HIV: cell binding and entry" 458: 85:, for example, by blocking a 842:10.1371/journal.ppat.1000109 100: 7: 1415:Tenofovir alafenamide (TAF) 639:10.1016/j.virol.2008.04.032 584:10.1101/cshperspect.a006866 356:, appears to interact with 152: 10: 2048: 1410:Tenofovir disoproxil (TDF) 703:10.1016/j.jaci.2006.08.016 383:against HIV found in some 1970: 1885: 1779: 1761: 1743: 1725: 1706: 1699: 1678: 1519: 1466: 1440: 1431:Discovery and development 1423: 1306: 1294: 1257: 1211: 1202:Discovery and development 1194: 1166: 1116: 1038:Discovery and development 1030: 1012: 267:and promotes their fusion 135:binding, fusion and entry 43:This article needs to be 1727:Transcription inhibitors 1679:Pharmacokinetic boosters 1595:Dolutegravir/rilpivirine 1556:Cabotegravir/rilpivirine 1196:Protease Inhibitors (PI) 956:Medical Subject Headings 486:10.1517/14656566.8.7.923 391:at the exact region, or 385:long-term nonprogressors 350:Epigallocatechin gallate 2011:initial regimen options 1577:Dolutegravir/lamivudine 1054:Enfuvirtide (ENF, T-20) 1032:Entry/fusion inhibitors 352:, a substance found in 259:The penetration of the 143:HIV's replication cycle 1852:Portmanteau inhibitors 1745:Translation inhibitors 1655:Lamivudine/raltegravir 1425:Non-nucleoside (NNRTI) 1383:Islatravir (EFdA, ISL) 422:CD4 specific Designed 329:Investigational agents 208:, that penetrates the 157:There are several key 122: 114: 1867:Synergistic enhancers 1665:Lamivudine/zidovudine 1545:Atazanavir/cobicistat 1521:Combined formulations 1358:Zidovudine (AZT, ZDV) 1296:Reverse-transcriptase 1168:Maturation inhibitors 952:HIV+Fusion+Inhibitors 912:10.1093/infdis/jit503 233:conformational change 129:for the treatment of 120: 108: 1708:Uncoating inhibitors 1561:Darunavir/cobicistat 1401:Nucleotide analogues 1319:Nucleoside analogues 1118:Integrase inhibitors 997:antiretroviral drugs 792:10.1128/AAC.01001-06 360:as do several other 111:mechanisms of action 1700:Experimental agents 1670:Lopinavir/ritonavir 1529:Abacavir/lamivudine 1503:Elsulfavirine (ESV) 1338:Emtricitabine (FTC) 1224:Fosamprenavir (FPV) 308:monoclonal antibody 228:to the CD4 receptor 127:combination therapy 1997:Never to phase III 1143:Elvitegravir (EVG) 1138:Dolutegravir (DTG) 1133:Cabotegravir (CAB) 123: 115: 2019: 2018: 1966: 1965: 1812:Diarylpyrimidines 1515: 1514: 1511: 1510: 1491:Rilpivirine (RPV) 1475:diarylpyrimidines 1458:Delavirdine (DLV) 1353:Zalcitabine (ddC) 1310:nucleotide (NRTI) 1290: 1289: 1148:Raltegravir (RAL) 1128:Bictegravir (BIC) 1107:Fostemsavir (FTR) 1022:Lenacapavir (LEN) 1014:Capsid inhibitors 534:10.3390/v13050735 163:HIV entry process 125:They are used in 73:, are a class of 71:fusion inhibitors 64: 63: 16:(Redirected from 2039: 2032:Entry inhibitors 1837:Hydroxycarbamide 1704: 1703: 1498:Doravirine (DOR) 1486:Etravirine (ETR) 1481:Dapivirine (DPV) 1453:Nevirapine (NVP) 1438: 1437: 1343:Lamivudine (3TC) 1333:Didanosine (ddI) 1304: 1303: 1277:Tipranavir (TPV) 1265:Atazanavir (ATV) 1249:Saquinavir (SQV) 1239:Nelfinavir (NFV) 1219:Amprenavir (APV) 1209: 1208: 1091:Ibalizumab (IBA) 986: 979: 972: 963: 962: 934: 933: 923: 891: 885: 884: 882: 881: 871: 865: 864: 854: 844: 820: 814: 813: 803: 771: 765: 764: 746: 722: 716: 715: 705: 681: 675: 667: 661: 660: 650: 618: 612: 611: 609: 608: 595: 563: 557: 556: 546: 536: 512: 506: 505: 469: 320:by binding with 161:involved in the 81:from entering a 69:, also known as 67:Entry inhibitors 59: 56: 50: 38: 37: 30: 21: 18:Entry inhibitors 2047: 2046: 2042: 2041: 2040: 2038: 2037: 2036: 2022: 2021: 2020: 2015: 2014: 2002: 1987:Clinical trials 1962: 1913:Dexelvucitabine 1881: 1872:Tre recombinase 1775: 1757: 1739: 1735:Tat antagonists 1721: 1695: 1674: 1507: 1462: 1448:Efavirenz (EFV) 1427: 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Index

Entry inhibitors
antiviral drugs
virus
cell
receptor
HIV
hepatitis D

mechanisms of action

combination therapy
HIV
binding, fusion and entry
virion
HIV's replication cycle
AIDS
proteins
HIV entry process
CD4
helper T cells
gp120
CCR5
chemokine
CXCR4
gp41
gp120
cell membrane
gp120
conformational change
gp120

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