106:
36:
118:
1430:
310:
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.
673:
1614:
1619:
1565:
1037:
2004:
1201:
333:
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.
1571:
1629:
1549:
1634:
1582:
983:
399:
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.
1604:
1588:
1599:
1609:
896:"Safety and antiviral activity of the HCV entry inhibitor ITX5061 in treatment-naive HCV-infected adults: a randomized, double-blind, phase 1b study"
1876:
1520:
1975:
1866:
441:
that targets, among others sites, the GP41 transmembrane glycoprotein. The trials are being conducted by
Virionyx, a New Zealand Company.
1624:
1639:
346:
was being developed to interfere with interaction between HIV and CXCR4, but showed little useful antiviral activity in recent trials.
1195:
976:
1649:
1533:
1659:
1644:
1424:
1404:
1322:
1307:
1295:
300:
binds to gp41 and interferes with its ability to approximate the two membranes. It is also referred to as a "fusion inhibitor."
1539:
686:"Epigallocatechin gallate, the main polyphenol in green tea, binds to the T-cell receptor, CD4: Potential for HIV-1 therapy"
623:"Neutralizing antibody and anti-retroviral drug sensitivities of HIV-1 isolates resistant to small molecule CCR5 inhibitors"
961:
472:
Biswas P, Tambussi G, Lazzarin A (May 2007). "Access denied? The status of co-receptor inhibition to counter HIV entry".
121:
An HIV virion binds to a CD4+ human cell. The two bottom pictures depict two proposed models of HIV fusion with the cell.
969:
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.
1992:
946:
2031:
825:"CD4-specific designed ankyrin repeat proteins are novel potent HIV entry inhibitors with unique characteristics"
1816:
1726:
1594:
1555:
955:
384:
349:
776:"Direct inactivation of human immunodeficiency virus type 1 by a novel small-molecule entry inhibitor, DCM205"
1980:
1576:
86:
1654:
1851:
1664:
1544:
1414:
1013:
232:
105:
1560:
1409:
1167:
1669:
1528:
1400:
1318:
1117:
996:
307:
126:
117:
110:
447:
is a synthesized peptide which binds to gp41, preventing fusion of the virus with a cell membrane.
951:
756:
497:
1957:
1952:
727:"Griffithsin, a potent HIV entry inhibitor, is an excellent candidate for anti-HIV microbicide"
1811:
1474:
925:
856:
823:
Schweizer A, Rusert P, Berlinger L, Ruprecht CR, Mann A, Corthésy S, et al. (July 2008).
805:
748:
707:
652:
597:
567:
548:
489:
1836:
915:
907:
846:
836:
795:
787:
738:
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642:
634:
587:
579:
538:
528:
481:
408:
894:
Sulkowski MS, Kang M, Matining R, Wyles D, Johnson VA, Morse GD, et al. (March 2014).
1912:
1871:
415:, an integrase inhibitor. DCM205 has been reported to inactivate HIV-1 particles directly
1986:
1762:
1744:
1707:
992:
920:
895:
851:
824:
800:
775:
647:
622:
592:
543:
516:
438:
423:
82:
74:
725:
Emau P, Tian B, O'keefe BR, Mori T, McMahon JB, Palmer KE, et al. (August 2007).
2025:
1752:
1502:
1337:
1223:
743:
726:
434:
412:
260:
209:
173:
17:
760:
501:
294:. It is also referred to as a "chemokine receptor antagonist" or a "CCR5 inhibitor."
1806:
1796:
1377:
1367:
1185:
1142:
1137:
1132:
1094:
1074:
1004:
669:
841:
370:, similar to maraviroc, is currently undergoing clinical trials for FDA approval.
188:, a second receptor found on the surface of CD4+ cells and macrophages, called a
49:
Please help update this to reflect recent events or newly available information.
1932:
1907:
1846:
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1021:
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94:
702:
685:
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1357:
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1218:
1180:
1090:
1078:
1070:
367:
361:
343:
337:
303:
485:
405:, a substance derived from algae, appears to have entry inhibitor properties.
1947:
1927:
1922:
1892:
1821:
1801:
1734:
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1347:
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656:
601:
552:
493:
774:
Duong YT, Meadows DC, Srivastava IK, Gervay-Hague J, North TW (May 2007).
316:, an attachment inhibitor that interferes with the interaction of CD4 and
1942:
1327:
791:
380:
2010:
1841:
1387:
1157:
444:
392:
158:
533:
274:
Entry inhibitors work by interfering with one aspect of this process.
220:
HIV entry into a human cell requires the following steps in sequence.
1791:
1786:
427:
264:
138:
684:
Williamson MP, McCormick TG, Nance CL, Shearer WT (December 2006).
1101:
396:
388:
357:
321:
317:
291:
246:
239:, which both increases its affinity for a co-receptor and exposes
236:
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205:
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116:
104:
78:
1060:
1048:
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185:
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965:
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1000:
169:
162:
142:
134:
130:
90:
29:
1615:
Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
1620:
Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil
874:
672:.com Human Immunodeficiency Virus (HIV) Infection Table 4
566:
Wilen, Craig B.; Tilton, John C.; Doms, Robert W. (2012).
182:, a protein on HIV surface that binds to the CD4 receptor
145:, such agents slow the progression from HIV infection to
1566:
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide
263:
by gp41, which approximates the membrane of HIV and the
89:. Entry inhibitors are used to treat conditions such as
621:
Pugach P, Ketas TJ, Michael E, Moore JP (August 2008).
419:
and is thought to act primarily as an entry inhibitor.
176:
in the human immune system, also called CD4+ T cells
1885:
1779:
1761:
1743:
1725:
1706:
1699:
1678:
1519:
1466:
1440:
1423:
1306:
1294:
1257:
1211:
1194:
1166:
1116:
1030:
1012:
198:, another chemokine co-receptor found on CD4+ cells
133:infection. This class of drugs interferes with the
1572:Dolutegravir/emtricitabine/tenofovir alafenamide
515:Xiao, Tianshu; Cai, Yongfei; Chen, Bing (2021).
1630:Emtricitabine/rilpivirine/tenofovir alafenamide
1550:Bictegravir/emtricitabine/tenofovir alafenamide
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
8:
1605:Efavirenz/emtricitabine/tenofovir disoproxil
1589:Dolutegravir/lamivudine/tenofovir disoproxil
517:"HIV-1 entry and membrane fusion inhibitors"
109:An illustration of HIV entry mechanism and
1703:
1600:Doravirine/lamivudine/tenofovir disoproxil
1437:
1303:
1208:
984:
970:
962:
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:
270:The entry of the viral core into the cell
1877:Zinc finger protein transcription factor
464:
340:, a monoclonal antibody that binds CCR5
780:Antimicrobial Agents and Chemotherapy
7:
1625:Emtricitabine/tenofovir alafenamide
224:The binding of HIV surface protein
1640:Emtricitabine/tenofovir disoproxil
900:The Journal of Infectious Diseases
25:
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
387:. It has been found to bind to
216:Binding, fusion, entry sequence
1540:Abacavir/lamivudine/zidovudine
731:Journal of Medical Primatology
437:antibody is in phase II human
1:
572:Cold Spring Harb Perspect Med
568:"HIV: cell binding and entry"
85:, for example, by blocking a
842:10.1371/journal.ppat.1000109
1415:Tenofovir alafenamide (TAF)
639:10.1016/j.virol.2008.04.032
584:10.1101/cshperspect.a006866
356:, appears to interact with
2048:
1410:Tenofovir disoproxil (TDF)
703:10.1016/j.jaci.2006.08.016
383:against HIV found in some
1970:
1431:Discovery and development
1202:Discovery and development
1038:Discovery and development
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:
18:Hiv fusion inhibitors
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:
1498:Doravirine (DOR)
1486:Etravirine (ETR)
1481:Dapivirine (DPV)
1453:Nevirapine (NVP)
1438:
1343:Lamivudine (3TC)
1333:Didanosine (ddI)
1304:
1277:Tipranavir (TPV)
1265:Atazanavir (ATV)
1249:Saquinavir (SQV)
1239:Nelfinavir (NFV)
1219:Amprenavir (APV)
1209:
1091:Ibalizumab (IBA)
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320:by binding with
161:involved in the
81:from entering a
69:, also known as
67:Entry inhibitors
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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:
1419:
1348:Stavudine (d4T)
1309:
1297:
1286:
1271:Darunavir (DRV)
1253:
1244:Ritonavir (RTV)
1234:Lopinavir (LPV)
1229:Indinavir (IDV)
1198:
1190:
1162:
1120:
1112:
1066:Maraviroc (MVC)
1034:
1026:
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993:Antiviral drugs
990:
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835:(7): e1000109.
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737:(4–5): 244–53.
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439:clinical trials
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278:Approved agents
245:The binding of
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77:that prevent a
75:antiviral drugs
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1328:Abacavir (ABC)
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1308:Nucleoside and
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941:External links
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875:"virionyx.com"
866:
829:PLOS Pathogens
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696:(6): 1369–74.
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578:(8): a006866.
558:
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174:helper T cells
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27:Antiviral drug
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1538:
1535:
1532:
1530:
1527:
1526:
1524:
1522:
1518:
1504:
1501:
1499:
1496:
1492:
1489:
1487:
1484:
1482:
1479:
1478:
1477:
1476:
1472:
1471:
1469:
1465:
1459:
1456:
1454:
1451:
1449:
1446:
1445:
1443:
1439:
1436:
1434:
1432:
1426:
1422:
1416:
1413:
1411:
1408:
1406:
1402:
1398:
1397:
1394:
1391:
1389:
1386:
1384:
1381:
1379:
1376:
1374:
1371:
1369:
1366:
1364:
1361:
1359:
1356:
1354:
1351:
1349:
1346:
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1341:
1339:
1336:
1334:
1331:
1329:
1326:
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1320:
1316:
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1313:
1311:
1305:
1302:
1299:
1293:
1283:
1280:
1278:
1275:
1272:
1269:
1266:
1263:
1262:
1260:
1256:
1250:
1247:
1245:
1242:
1240:
1237:
1235:
1232:
1230:
1227:
1225:
1222:
1220:
1217:
1216:
1214:
1210:
1207:
1205:
1203:
1197:
1193:
1187:
1184:
1182:
1179:
1177:
1174:
1173:
1171:
1169:
1165:
1159:
1156:
1154:
1151:
1149:
1146:
1144:
1141:
1139:
1136:
1134:
1131:
1129:
1126:
1125:
1123:
1119:
1115:
1108:
1104:
1103:
1099:
1096:
1092:
1088:
1087:
1083:
1080:
1076:
1072:
1069:
1067:
1063:
1062:
1058:
1055:
1051:
1050:
1046:
1045:
1043:
1041:
1039:
1033:
1029:
1023:
1020:
1019:
1017:
1015:
1011:
1006:
1002:
999:used against
998:
994:
987:
982:
980:
975:
973:
968:
967:
964:
957:
953:
950:
948:
945:
944:
940:
931:
927:
922:
917:
913:
909:
906:(5): 658–67.
905:
901:
897:
890:
887:
876:
870:
867:
862:
858:
853:
848:
843:
838:
834:
830:
826:
819:
816:
811:
807:
802:
797:
793:
789:
786:(5): 1780–6.
785:
781:
777:
770:
767:
762:
758:
754:
750:
745:
740:
736:
732:
728:
721:
718:
713:
709:
704:
699:
695:
691:
687:
680:
677:
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671:
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663:
658:
654:
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644:
640:
636:
632:
628:
624:
617:
614:
603:
599:
594:
589:
585:
581:
577:
573:
569:
562:
559:
554:
550:
545:
540:
535:
530:
526:
522:
518:
511:
508:
503:
499:
495:
491:
487:
483:
480:(7): 923–33.
479:
475:
468:
465:
458:
453:
449:
446:
443:
440:
436:
433:A polyclonal
432:
429:
425:
421:
418:
414:
413:chicoric acid
410:
407:
404:
401:
398:
394:
390:
386:
382:
378:
375:
372:
369:
366:
363:
359:
355:
351:
348:
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342:
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336:
335:
334:
328:
323:
319:
315:
312:
309:
305:
302:
299:
296:
293:
289:
285:
282:
281:
277:
275:
269:
266:
262:
261:cell membrane
258:
256:CCR5 or CXCR4
255:
252:
248:
244:
242:
238:
234:
230:
227:
223:
222:
221:
215:
211:
210:cell membrane
207:
203:
200:
197:
194:
191:
187:
184:
181:
178:
175:
171:
168:
167:
166:
164:
160:
152:
150:
148:
144:
140:
136:
132:
128:
119:
112:
107:
100:
98:
96:
92:
88:
84:
80:
76:
72:
68:
58:
46:
41:
32:
31:
19:
2007:
1807:Cyanovirin-N
1797:Calanolide A
1473:
1467:2 generation
1441:1 generation
1428:
1399:
1378:Elvucitabine
1368:Apricitabine
1317:
1258:2 generation
1212:1 generation
1199:
1186:Fipravirimat
1100:
1095:Semzuvolimab
1084:
1075:Cenicriviroc
1059:
1047:
1035:
1031:
903:
899:
889:
878:. Retrieved
869:
832:
828:
818:
783:
779:
769:
734:
730:
720:
693:
689:
679:
670:Merck Manual
665:
633:(2): 401–7.
630:
626:
616:
605:. Retrieved
575:
571:
561:
524:
520:
510:
477:
473:
467:
450:ITX5061 for
416:
332:
273:
253:
219:
156:
124:
70:
66:
65:
52:
44:
2008:recommended
1983:from market
1933:Lersivirine
1908:Capravirine
1847:Miltefosine
1832:Griffithsin
1827:Fosdevirine
1373:Censavudine
1003:(primarily
452:hepatitis C
403:Griffithsin
362:theaflavins
314:Fostemsavir
298:Enfuvirtide
251:co-receptor
192:co-receptor
95:hepatitis D
1938:Lodenosine
1918:Droxinavir
1903:Brecanavir
1898:Atevirdine
1862:Seliciclib
1857:Scytovirin
1771:Elipovimab
1716:TRIM5alpha
1393:Stampidine
1298:inhibitors
1282:TMC-310911
1181:BMS-955176
1079:Leronlimab
1071:Vicriviroc
880:2007-08-26
607:2021-08-11
527:(5): 735.
459:References
426:Proteins (
379:b12 is an
368:Vicriviroc
344:Plerixafor
338:Leronlimab
304:Ibalizumab
137:of an HIV
1993:Phase III
1981:Withdrawn
1958:Telinavir
1953:Palinavir
1948:Mozenavir
1928:Emivirine
1923:Lasinavir
1893:Aplaviroc
1822:Foscarnet
1802:Ceragenin
1363:Amdoxovir
1176:Bevirimat
1153:BI 224436
374:Aplaviroc
354:green tea
286:binds to
284:Maraviroc
190:chemokine
101:HIV entry
2026:Category
1943:Loviride
930:24041792
861:18654624
810:17307982
761:22539115
753:17669213
712:17157668
657:18519143
627:Virology
602:22908191
553:33922579
502:32675897
494:17472538
417:in vitro
395:, where
381:antibody
159:proteins
153:Proteins
87:receptor
55:May 2020
1842:KP-1461
1388:Racivir
1158:MK-2048
921:3923538
852:2453315
801:1855571
648:2528836
593:3405824
544:8146413
521:Viruses
445:VIR-576
435:caprine
428:DARPins
393:epitope
45:updated
1976:WHO-EM
1792:BIT225
1787:Abzyme
1718:(gene)
1405:NtRTIs
1300:(RTIs)
958:(MeSH)
928:
918:
859:
849:
808:
798:
759:
751:
710:
655:
645:
600:
590:
551:
541:
500:
492:
409:DCM205
265:T cell
254:either
139:virion
1780:Other
1763:BNAbs
1323:NRTIs
1102:gp120
757:S2CID
498:S2CID
397:gp120
389:gp120
358:gp120
322:gp120
318:gp120
292:gp120
249:to a
247:gp120
237:gp120
226:gp120
206:gp120
196:CXCR4
180:gp120
79:virus
2005:DHHS
1061:CCR5
1049:gp41
926:PMID
857:PMID
806:PMID
749:PMID
708:PMID
653:PMID
598:PMID
549:PMID
490:PMID
306:, a
288:CCR5
241:gp41
202:gp41
186:CCR5
147:AIDS
93:and
83:cell
1086:CD4
1005:J05
1001:HIV
916:PMC
908:doi
904:209
847:PMC
837:doi
796:PMC
788:doi
739:doi
698:doi
694:118
643:PMC
635:doi
631:377
588:PMC
580:doi
539:PMC
529:doi
482:doi
235:in
170:CD4
131:HIV
91:HIV
2028::
1989::
1093:,
1077:,
1073:,
995::
924:.
914:.
902:.
898:.
855:.
845:.
831:.
827:.
804:.
794:.
784:51
782:.
778:.
755:.
747:.
735:36
733:.
729:.
706:.
692:.
688:.
651:.
641:.
629:.
625:.
596:.
586:.
574:.
570:.
547:.
537:.
525:13
523:.
519:.
496:.
488:.
476:.
231:A
165:.
149:.
97:.
2003:°
1591:°
1585:°
1579:°
1568:°
1552:°
1536:°
1433:)
1429:(
1407::
1403:/
1325::
1321:/
1273:°
1267:°
1204:)
1200:(
1109:)
1105:(
1097:)
1089:(
1081:)
1064:(
1056:)
1052:(
1040:)
1036:(
1007:)
985:e
978:t
971:v
932:.
910::
883:.
863:.
839::
833:4
812:.
790::
763:.
741::
714:.
700::
659:.
637::
610:.
582::
576:2
555:.
531::
504:.
484::
478:8
454:.
364:.
324:.
57:)
53:(
47:.
20:)
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