Patent Update Anti-infectives: Emerging anti-HIV agents and targets

References to Primary Literature

• RANE DF: Recent advances in anti-HIV agents. Exp. Opin. 7her. Patents (1995) 5:913–921.
   Google Scholar
• DECLERCQ E: Toward improved anti-HIV chemother-apy: therapeutic strategies for intervention with HIV Infections. J. Med. Chem. (1995) 38:2491–2517.
   PubMed Web of Science ®Google Scholar
• DECLERQ E: Antiviral therapy for human immunodefi-ciency virus infections. Clin. Microbiol. Rev. (1995) 8:200–239.
   PubMedGoogle Scholar
• Antiviral Agents Bulletin (1995) 8:321–324.
   Google Scholar
• Antiviral Agents Bulletin (1995) 8:289–292.
   Google Scholar
• MANSOUR TS, TSE A, CHARRON M, HOOKER EU, ASHMAN C, CAMMACK N, CAMERON JM: Anti-HIV and anti-HBV activities of L-2',3'-dicleoxynucleoside analogues: ddC, 5FddC, 5-azaddC and ddG. Med. Chem. Res. (1995) 5:417–425.
   Web of Science ®Google Scholar
• MANSOUR TS, JIN H, WANG W, HOOKER EU, ASHMAN C, CAMMACK N, SALOMON H, BELMONTE AR, Co7AINBERGMA: Anti-human immunodeficiency virus and anti-hepatitis B virus activities and toxidties of the enan-tiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. J. Med. Chem. (1995) 38:1–4.
   PubMed Web of Science ®Google Scholar
• LOAKES D, BROWN DM, MAHMOOD N, BALZARINI J,DECLERCQ E: Antiviral activity of N-4-aminocytidine derivatives related to AZT. Antiviral Chem. Chemother. (1995) 6:9–16.
   Google Scholar
• JONES BCNM, SILVERTON JV, SIMONS C, MEGATI S, NISHIMURA H, MAEDA Y, MITSUYA H, ZEMLICKA J: Syn-thesis, absolute configuration, and enantioselectivity of antiretroviral effect of (R)-(-)- and (S)-(+)-cytallene-li-pase-catalyzed enantioselective acylations of (±)N-4-acylcytallenes. J. Med. Chem. (1995) 38:1397–1405.
   PubMedGoogle Scholar
• TSAI C-C, FOLLIS KE, SABO A, BECK TW, GRANT RF, BISCHOFBERGER N, BENVENISTE RE, BLACK R: Preven-tion of SW infection in macaques by (R)-9-(2-phos-phony! methoxypropyl) adenine. Science (1995) 270:1197–1199.
   PubMedGoogle Scholar
• CHERRINGTON JM, ALLEN sjw, BISCHOFBERGER N, CHENMS: Kinetic interaction of the diphosphates of 942-phosphonylmethoxyethyl) adenine and other anti-HIV active purine congeners with HIV reverse transcriptase and human DNA polymerases a,13 and y. Antiviral Chem. Chemother. (1995) 6:217–221.
   Web of Science ®Google Scholar
• HAKIMELAHI GH, MOOSAVI-MOVAHEDI AA, SADEGHI MM, TSAY S-C, HWN JR: Design, synthesis and structure-activity relationship of novel dinucleotide analogs as agents against herpes and human immunodeficiency viruses. J. Med. Chem. (1995) 38:4648–4659.
   PubMed Web of Science ®Google Scholar
• saiarr H, HAUSSLER MP, GOWLAND P, BENDER A, VON BRIESEN H, SCHWENDENER RA: Synthesis and in vitro antiviral properties of amphillic &nucleoside phos-phate derivatives of 2',3'-dideoxycytidine (ddC). Antivi-ral Chem. Chemother. (1995) 6:320–326.
   Google Scholar
• MAYERS DL, MIKOVITS JA, JOSHI B, HEWLETT IK, ES-TRADA JS, WOLFE AD, GARCIA GE, DOCTOR BP, BURKE DS, GORDON RK: Anti-human imuumnodeficiency virus 1 (HIV-1) activities of 3-deazaadenosine analogs: in-creased potency agAinst 3'-azido-3'-deox-ythymidine-re-sistant HIV-1 strains. Proc. Natl. Acad. Sci. USA (1995) 92:215–219.
   PubMed Web of Science ®Google Scholar
• FORD H, SIDDIQUI MA, DRISCOLL JS, MARQUEZ YE, KELLEY JA, MITSUYA H, SHIRASAKA T: Liphophilic, add stable, adenosine dearninase-activated anti-HIV pro-drugs for central nervous system delivery. 2.6-halo and 6-alkoxy prodrugs of 2'-fluoro-2',3'-dideox-yinosine. J. Med. Chem. (1995) 38:1189–1195.
   Google Scholar
• XIE H, VORONKOV M, LiarrA DC, KORBA BA, SCHINAZI RF, RICHMAN DD, HOSTETLER KY: Phosphatidy1-2',3'-dideoxy-3'-thiacytidine: synthesis and antiviral activity In hepatitis B and HIV-1-infected cells. Antiviral Res. (1995) 28:113–120.
   PubMedGoogle Scholar
• SHIMIZU NS, HANDA A, SHIMIZU NG, IKEDA R, UCHI-YAMA T, ACHIWAK, HOSHINO H: Inhibition of infection of T-cells with human immunodeficinecy 'virus type 1 by dideoxynucleosides conjugated with oligopeptides. Antiviral Chem. Chemother. (1995) 6:17–24.
   Google Scholar
• CALOGEROPOULOU T, KOUFAKI M, TSOTINIS A, BALZARINI J, DECLERCQ E, MAKRIYANNIS A: Synthesis and anti-HIV evaluation of alkyl and alkoxyethyl phos-phodiester AZT derivatives. Antiviral Chem. Chemother. (1995) 6:43–49.
   Google Scholar
• NILLROTH U, VRANG L, AHLSEN G, BESIDSKY Y, CHAT-TOPADHYAYA J, UGI I, DANIELSON UH: The use of 5'-phosphate derivatives of nucleoside analogues as inhibitors ofreplication. Antiviral Chem.Chemother. (1995) 6:50–64.
   Web of Science ®Google Scholar
• LEFEBVRE I, PERIGAUD C, POMPON A, AUBERTIN A-M, GIRARDET J-L, KIRN A, GOSSELIN G, IMBACH J-L:Mononu-cleoside phosphotriester derivatives with S-acy1-2-thkoethyl bioreversible phosphate-protecting groups: Intracellular delivery of 3'-azido-2',3'-dideoxythymid-ine 5'-monophosphate. J. Med. Chem. (1995) 38:3941–3950.
   PubMed Web of Science ®Google Scholar
• PERIGAUD C, GOSSELIN G, BENZARIA 5, GIRARDET J-L, MAURY G, PELICAN° H, AUBERTIN A-M, KIRN A, IMBACH J-L:Bis(S-acy1-2-thioethybesters of 2',3'-dideoxyadenos-ine 5'-monophosphate are potent anti-HIV agents in cell culture. Nucleosides Nucleotides (1995) 14:789–791.
   Google Scholar
• SPENCE RA, KATI WM, ANDERSON KS, JOHNSON KA: Mechanism of inhibition of HIV-1 reverse transcriptaseby non-nucleoside inhibitors. Science(1995) 267:988–993.
   PubMed Web of Science ®Google Scholar
• WYATT PG, BETHELL RC, CAMMACK N, CHARON D, DODIC N, DUMAITRE B, EVANS DN, GREEN DVS, HOPEW-ELL PL, HUMBER DC, LAMONT RB, ORE DC, PLESTED 5J, RYAN DM, SOLI IS SL, STORER R, WEINGARTEN GG: Ben-zophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase. J. Med. Chem. (1995) 38:1657–1665.
   PubMed Web of Science ®Google Scholar
• HANASAKI Y, WATANABE H, KATSUURA K, TAKAYAMA H, SHIRAKAWA S, YAMAGUCHI K, SATAI S-I, IJICHI K, FUJIWARA M, KONNOK, YOKOTA T, SHIGETA S, BABA M: Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. J. Med. Chem. (1995) 38:2038–2040.
   PubMed Web of Science ®Google Scholar
• ANTONUCCI T, WARMUS JS, HODGES JC, NICKELL DG: Characterization of the antiviral activity of highly sub-stituted pyrroles: a novel class of non-nucleoside HIV-1 reverse transcriptase inhibitor. Antiviral Chem. Chemother. (1995) 6:98–108.
   Google Scholar
• ZHANG H, VRANG L, BACKBRO K, LIND P, SAHLBERG C, LTNGE T, OBERG B: Inhibition of human immunodefi-cienty virus type 1 wild-type and mutant reverse tran-scriptases by the phenyl ethyl thiazolyl thiourea derivatives trovirdine and MSC-127. Antiviral Res. (1995) 28:331–342.
   PubMedGoogle Scholar
• BELL FW, CANTRELL AS, HOGBERG M, JASKUNAS SR, JOHANSSON NG, JORDAN CL, KINNICK MD, LIND P, MORN JR. JM, NOREEN R, OBERG B, PALKOWITZ JA, PARRISH CA, PRANC P, SAHLBERG C, TERNANSKY R, VASILEFF RT, VRANG L, WEST SJ, ZHANG H, ZHOU X-X: Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors 1. Syn-thesis and bask structure-activity relationship studies of PETE analogs. J. Med. Chem. (1995) 38:4929–4936.
   Google Scholar
• CHENG C-W, UN M-T, LEE S-S, CHEN-LIU KCS, HSU F-L, UN J-Y: Differential inhibition of reverse transcriptase and cellular DNA polymerase activities by lignans iso-lated from chinese herbs, Pbyllantbus nsyrtifolius moon and tanning from lonicera japonica thunb and castanopsis hystrix. Antiviral Res. (1995) 27:367–374.
   PubMedGoogle Scholar
• X1E L, XIE J-X, KASHIWADA Y, COSENTINO LM, LIU S-H, PAI RB, CHENG Y-C, LEE K-H: Anti-AIDS (acquired immu-nodeficiency syndrome) agents 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents. J. Med. Chem. (1995) 38:3003–3008.
   Google Scholar
• PROUDFOOT JR, PATEL UR, KAPADIA SR, HARGRAVE KD: Novel non-nucleoside inhibitors of H1V-1 reverse tran-scriptase 3. Dipyrido [2,3-b: 2',3'-e]diazepinones. J. Med. Chem. (1995) 38:1406–1410.
   Google Scholar
• BOYODE BP, SINET M, FARESE A, FORESTIER-ROUX MA, CONDOM R, AYI IA, KIRN A, MOOG C, GUEDJ R: Synthesis and antiviral evaluation of fluorinated dipyridodiazepi-nones and dipyridodiazepines (nevirapine deriva-tives). Antiviral Chem. Chemotber. (1995) 6:162–168.
   Google Scholar
• PROUDFOOT JR, HARGRAVE KD, KAPADIA SR, PATEL UR, GROZINGER KG, MCNEIL DW, CULLEN E, CARDOZO M, TONG L, KELLY TA, ROSE J, DAVID E, MAULDIN SC, FUCHS VU, VITONS J, HOERMANN M, KLUNDER JM, RAGHAVAN P, SICILES JW, MUI P, RICHMAN DD, SULLIVAN JL, SHIH C-K, GROB PM, ADAMS J: Novel non-nucleoside inhibi-tors of human immunodeficiency virus type 1 (11W-1) reverse transcriptase 4. 2-substituted dipyridodiazapi-nones as potent inhibitors of both wild-type and cys-tein-181 HIV-1 reverse transcriptase enzymes. J. Med. Chem. (1995) 38:4830–4838.
   Google Scholar
• KELLY TA, PROUDFOOT JR, MCNEIL DW, PATEL UR, DAVID E, HARGRAVE KD, GROB PM, CARDOZO M, AGAR-WAR A, ADAMS J: Novel non-nucleoside inhibitors of human Immunodeficiency virus type 1 reverse tran-scriptase 5.4-Substituted and 2,4-disubstituted analogs of nevirapine. J. Med. Chem. (1995) 38:4839–4847.
   Google Scholar
• MARUENDA H, JOHNSON F: Design and synthesis of novel inhibitors of HIV-1 reverse transcriptase. J. Med. Chem. (1995) 38:2145–2151.
   PubMed Web of Science ®Google Scholar
• TANAKA H, TAKASHIMA H, UBASAWA M, SEKIYA K, INONYE N, BABA M, SHIGETA S, WALKER RT, DECLERCQ E, MIYASAKA T: Synthesis and antiviral activity of 6-ben-zyl analogs of 1-[(2-hydroxyethoxy)methy1]-6-(phettylthio)thymine HEFT as potent and selective anti-HIV-1 agents. J. Med. Chem. (1995) 38:2860–2865.
   PubMed Web of Science ®Google Scholar
• BRENNAN TM, TAYLOR DL, BRIDGES CG, LEYDA JP, TYMS AS: The inhibition of human immunodeficiency virus type 1 in vitro by anon-nucleoside reverse transcriptase inhlibitor MKC-442 alone and in combination with other anti-HIV compounds. Antiviral Res. (1995) 26:173–187.
   PubMedGoogle Scholar
• SEKI M, SADAKATA Y, YIJASA 5, BABA M: Isolation andcharacterization of human immunodeficiency virus type-1 mutants resistant to the non-nuc.leoside reverse transcriptase inhibitor MKC-442. Antiviral Chem. Chemotber. (1995) 6:73–79.
   Google Scholar
• MASSA S, MAT A, ARTICO M, SHARDELLA G, TRAMONTANOE, LOI AG, SCANO P, LACOLLA P: Synthesis and antiviral activity of new 2,4-dihydro-2-alkoxy-6-benzy1-4-oxopyrimidines (DABOs), specific inhibitors of human immunodeficiency virus type 1. Antiviral Chem. Chemother. (1995) 6:1–8.
   Google Scholar
• MAT A, ARTICO M, SBARDELLA G, MASSA 5, LOI AG, TRAMONTANO E, SCANO P, LACOLLA P: Synthesis and anti-HIV-1 activity of analogues of dihydroalkoxyben-zyloxopyrimidines. J. Med. Chem. (1995) 38:3258–3263.
   PubMed Web of Science ®Google Scholar
• INGATE S, PÉREZ-PÉREZ M-J, DECLERCQ E, BALZARINI J,CAMARASA M-J: Synthesis and anti-H1V-1 activity of novel 1SAO-T derivatives modified at the 2'-and 5'-po-sitions of the sugar moiety. Antiviral Res. (1995) 27:281–299.
   PubMedGoogle Scholar
• BALZARINI J, JONCKHEERE H, HARRISON WA, DA0 DC, ANNE J, DECLERCQ E, }CARLSSON A: Oxathiin carbox-anilkle derivatives: a class of non-nucleoside IIIV-1 specific reverse transcriptase inhibitors (NWT's) that are active against mutant HIV-1 strains resistant to other NNKTIs. Antiviral Chem. Chemother. (1995) 6:169–178.
   Web of Science ®Google Scholar
• VELAZQUEZ S, ALVAREZ R, SAN-FELIX A, JIMENO ML, DECLERCQ E, BALZARINI J, CAMARASA MJ: Synthesis and anti-HIV activity of [AZTHISAO-TI and [AZIRIBIPTI dimers as potential multifunctional inhibitors of 111V-1 reverse transcriptase. J. Med. Chem. (1995) 38:1641–1649.
   PubMed Web of Science ®Google Scholar
• ECICER DJ, WYATT JR, VICKERS T, BUCKHEIT R, ROBER-SON J, IMBACH J-L: Novel guanosine quartet structure binds to the HIV envelope and inhibits envelope medi-ated cell fusion. Nucleosides Nucleotides (1995) 14:1117–1127.
   Google Scholar
• BROOM AD, AGRAWAL VK, TUTONDA MG, FAIN HD, BUCKHEIT JR. RW: Unusual single-stranded polyribonu-cleotides as potent anti-HIV agents. J. Med. Chem. (1995) 38:3253–3257.
   Google Scholar
• WEI X, GHOSH SK, TAYLOR ME, JOHNSON VA, EMINI EA, DEUTSCH P, LIFSON JD, BONHOEFFER S, NOWAK MA, HAHN BH, SAAG MS, SHAW GM: Viral dynamics in human immunodeficiency virus type 1 infection. Nature (1995) 373:117–122.
   PubMed Web of Science ®Google Scholar
• HO DD, NEUMANN AU, PERELSON AS, CHEN W, LEONARD JM, MARKOWITZ M: Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection. Nature (1995) 373:123–126.
   PubMed Web of Science ®Google Scholar
• BILLICH A, SCHOLZ D, CHARPIOT B, GSTACH H, LEHR P, PEICHL P, ROSENWIRTH B: Potent and orally bioavail-able HIV-1 proteinase inhibitors containing the 2-ami-nobenzylstatine moiety. Antiviral Chem. Chemother. (1995) 6:327–336.
   Google Scholar
• HOLLOWAY, MK, WAI JM, HALGREN TA, FITZGERALD PMD, VACCA JP, DORSEY BD, LEVIN RB, THOMPSON WJ, CHEN LJ, DESOLMS SJ, GAFFIN N, GHOSH AK, GIULIANI EA, GRAHAM SL, GUARE JP, HLTNGATE RW, LYLE TA, SANDERS WM, TUCKER TJ, WIGGINS M, W1SCOUTN CM, WOLTERSDORF OW, YOUNG SD, DARKE PL, ZUGAY JA: A pylori prediction of activity for WV-1 protease inhibi-tors employing energy minimization in the active site Med. Chem. (1995) 38:305–317.
   Google Scholar
• VAZQUES, ML, BRYANT ML, CLARE M, DECRESCENZO GA, DOHERTY EM, FRESKOS JN, GETMAN DP, HOUSEMAN KA, JULIEN JA, KOCAN GP, MUELLER RA, SHLEH H-S, STALL-INGS WC, STEGEMAN RA, TALLEY JJ: Inhibitors of HIV-1 protease cont2ining the novel and potent (R)-(Hy-drox-yethybsulfonamide isostere. J. Med. Chem. (1995) 38:581–584.
   PubMedGoogle Scholar
• VARA PRASAD JVN, PARA KS, TUMMINO PJ, FERGUSON D, MCQUADE TJ, LUNNEY EA, RAPUNDALO ST, BATLEY BL, HINGORANI G, DOMAGALA JM, GRACHECK SJ, BHAT TN, LIU B, BALDWIN ET, ERIC1CSON JW, SAWYER TK: Nonpep-tidk potent HIV-1 protease inhibitors: (4-hydroxy-6-pheny1-2-oxo-2H-pyran-3-yOthiomethanes that span subsites in a unique mode of active site binding. J Med. Chem. (1995) 38:898–905.
   PubMedGoogle Scholar
• THAISRIVONGS S, WATENPAUGH ICD, HOWE WJ, TOMICH PK, DOLAK LA, CHONG K-T, TOMICH C-SC, TOMASSELLI AG, TURNER SR, STROHBACK JW, MULICHAK AM, JANAICI-RAMAN MN, MOON JB, LYNN JC, HORNG M-M, HINSHAW RR, CURRY KA, ROTHROCK DJ: Structure-based design of novel HIV protease inhibitors: carboxamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as po-tent nonpeptidic inhibitors./ Med. Chem. (1995) 38: 3624–3637.
   PubMed Web of Science ®Google Scholar
• ROJMINES KR, WATERNPAUGH KD, TOMICH PK, HOWEWJ, MORRIS JK, LOVASZ ICD, MULICHAK AM, FINZEL BC, LYNN JC, HORN M-M, SCHWENDE FJ, RUWART MJ, ZIPP GL, CHONG K-T, DOLAK LA, TOTH LN, HOWARD GM, RUSH BD, WILKINSON ICE, POSSERT PL, DALGA RJ, HIN-SHAW RR: Use of medium-sized cycloallcyl rings to enhance secondary binding: discovery of a new class of human inimunodefickncy virus (HIV) protease in-hibitors. J. Med. Chem. (1995) 38:1884–1891.
   PubMedGoogle Scholar
• VAILLANCOURT M, SAUVE G, COHEN E: Antiviral prop-erties of simple difunctionalized enols targeted to the HIV-1 protease. Antiviral Res. (1995) 27:205–218.
   PubMedGoogle Scholar
• FRITZ CC, ZAPP ML, GREEN MR: A human nucleoporin like protein that specifically interacts with HIV Rev. Nature (1995) 376:530–533.
   PubMed Web of Science ®Google Scholar
• FISHER U, HUBER J, BOELENS WC, MATTAJ IW, LUHR-MANN R: The HIV-1 Rev activation domain is a nuclear export signal that accesses an export pathway used by specific cellular RNAs. Cell (1995) 82:475–483.
   PubMedGoogle Scholar
• BOGERD HP, FRIDELL RA, MADORE S, CULLEN BR: Iden-tification of a novel cellular co-factor for the Rev/Rex class of retroviral regulatory proteins. Cell(1995) 82:485–494.
   PubMed Web of Science ®Google Scholar
• LUND OS, NIELSEN JO, HANSEN J-ES: Inhibition of HIV-1in vitro by C-5 propyne phosphorothioate antisense to Rev. Antiviral Res. (1995) 28:81–91.
   PubMedGoogle Scholar
• CHANG LJ, ZHANG C: Infection and replication of Tat-human immunodeficiency viruses: genetic analyses of LTR and Tat mutations in primary and long-term hu-man lymphoid cells. Virology (1995) 211:157–169.
   PubMedGoogle Scholar
• WESTERNDORP MO, FRANK R, OCHSENBAUER C, STRICKER K, DHEIN J, WALCZAK H, DEBATIN KM, KRAM-MER PH: SensibRization of T-cells to CD95-mediated apoptosis byTat and gp120. Nature (1995) 375:497–500.
   PubMedGoogle Scholar
• VELLUTINI C, HORSHOWSKI N, PHILIPPON V, GAM-BARELLI D, NAVE KA, FILIPPI P: Development of lym-phoid hyperplasia in transgenic mice expressing the HIV tat gene. AIDS Res. Hum. Retroviruses (1995) 11:21–29.
   PubMed Web of Science ®Google Scholar
• ALBINI A, BARILLARI G, BENELLI R, GALLS RC, ENSOLI B: Angiogenic properties of human immunodeficiency virus type 1 Tat protein. Proc. Natl. Acad. Sd USA (1995) 92:4838–4842.
   PubMed Web of Science ®Google Scholar
• MAGNUSON DS, KNUDSEN BE, GEIGER JD, BROWNSTONE RM, NATH A: Human immunodeficiency virus type 1 Tat activates non N-methyl-D-aspartate excitatory amino acid receptors and causes neurotoxkity. Ann. Neurol. (1995) 37:373–380.
   PubMed Web of Science ®Google Scholar
• WESTENDORP MO, SHATROV VA, SCHULZE-OSTHOFF K, FRANK R, KRAFT M, LOS M, KRAMMER PH, DORGE W, LEHMANN V: HIV-1 Tat potentiates TNF-induced NF-Kappa B activation and cytotoxicity by altering the cellular redox state. EMBO. J. (1959) 14:546–554.
   Google Scholar
• TAYLOR JP, POMERANTZ RJ, OAKES JW, KHALIKI K, AMINI S: A CNS-enriched factor that binds to NF-Kappa B and Is required for interaction with HIV-1 Tat. Oncogene (1995) 10:395–400.
   PubMedGoogle Scholar
• LAPIDOT A, BEN-ASHER E, EISENSThIN M: Tetrahydro- pyrimidine derivatives inhibit binding of a Tat-like arginine-containing peptide to HIV TAR RNA in vitro. FEI3S. Lett. (1995) 367:33–38.
   Google Scholar
• CAPELLI LA, HSU MC: The human Immunodeficiency virus type 1 Tat antagonist Ro 5-3335 predominantly Inhibits transcription initiation from the viral pro-moter. J. Virology (1995) 69:2640–2643.
   PubMedGoogle Scholar
• LUZNIK L, KRAUS G, GUATELLI J, RICHMAN D, WONG STAAL F: Tat independent replication of human immu-nodeficiency viruses. J. Clin. Invest. (1995) 95:328–332.
   PubMedGoogle Scholar
• MICHNE WE, SHROEDER JD, BAILEY TR, NEUMANN HC, COOKED, YOUND DC, HUGHES JV, KINGSLEY SD, RYAN KA, PUTZ HS, SHAW LJ, DUTHO F: Keto/enol epoxy steroids as HIV-1 Tat inhibitors: structure-activity rela-tionships and pharmacophore localization. J. Med. Chem. (1995) 38:3197–3206.
   PubMedGoogle Scholar
• WILD C, GREENWELL T, SHUGARS D, RINSKY-CLARICE L, MATTHEWS T: The inhibitory activity of an HIV type 1peptide correlates with its ability to interact with a leucine zipper structure. AIDS Res. Hum. Retroviruses (1995) 11:323–325.
   PubMed Web of Science ®Google Scholar
• YAHI N, FANTINI J, BAGHDIGUIAN S, MABROUK K, TAMALET C, ROCHAT H, VANRIETSCHOTEN J, SABATTER JM: SPC3, a synthetic peptide derived from the V3 domain of human immunodefidency virus type 1 (HIV-1) gp120, inhibits HIV-1 entry into CD4* and CD4- cells by two distinct mechanisms. Proc. Natl. Acad. Sci. USA (1995) 92:4867–4871.
   PubMedGoogle Scholar
• BRIDGER GJ, SKERLJ RT, 'THORNTON D, PADMANABHANS, MARTELLUCCI SA, HENSON GW, ABRAMS MJ, YAMAMOTO N, DEVREESE K, PAUWELS R, DECLERCQ E: Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocy-des that inhibit HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker. J. Med. Chem. (1995) 38:366–378.
   Google Scholar
• JOAO HC, DEVREESE K, PAUWELS R, DECLERCQ E, HEN▪SON GW, BRIDGER GJ: Quantitative structural activity relationship study of bis-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors. J. Med. Chem. (1995) 38:3865–3873.
   Google Scholar
• INOUYE Y, KANAMORI T, SUGIYAMA M, YOSHIDA T, KOIKE T, SHIONOYA M, ENOMOTO K, SUEHIRO K, KIMURA E: Dimeric macrocyclic polyamines with po-tent inhibitory activity against human irnmu.nodefi-ciency virus. Antiviral Chem. Chemother. (1995) 6:337–344.
   Web of Science ®Google Scholar
• ANSARI-LARI MA, DONEHOWER LA, GIBBS RA: Analysis of human immunodeficiency virus type 1 integrase mutants. Virology(1995) 211:332–335.
   PubMedGoogle Scholar
• EIJKELENBOOM APAM, LUTZKE RAP, BOELENS R, PLASTERK RHA, KAPTEIN R, HARD K: The DNA-binding do-main of HIV-1 integrase has an SH3-like fold. Nature Struct. Biol. (1995) 2:807–810.
   PubMedGoogle Scholar
• LODI PJ, ERNST JA, KUSZEWSKI J, HICKMAN AB, ENGELMAN A, CRAIGIE R, CLORE GM, GRONENBORN AM: Solu-tion structure of the DNA binding domain of 111V-1 integrase. Biochemistry (1995) 34:9826–9833.
   PubMed Web of Science ®Google Scholar
• RANDO RF, OJWANG J, ELBAGGARI A, REYES GR, TINDER R, MCGRATH MS, HOGAN ME: Suppression of humanimmunodeficiency virus type 1 activity in vitro by oligonucleotides which form intramolecular tetrads. j. Biol. Chem. (1995) 270:1754–1760.
   PubMed Web of Science ®Google Scholar
• LAFEMINA EL, GRAHAM PL, LEGROW K, HASTINGS JC,WOLFE A, YOUNG SD, EMINI EA, HAZUDA DJ: Inhibition of human immunodeficiency virus integrase by bis-catechols. Antimicrob. Agents Chemother. (1995) 39:320–324.
   PubMed Web of Science ®Google Scholar
• BURKE JR. TR, FESEN MR, MAZUMDER A, WANG J, CAROTHERS AM, GRUNBERGER D, DRISCOLL J, KOHN K, POMMIER Y: Hydroxylated aromatic inhibitors of 111V-1 integrase. J. Med. Chem. (1995) 38:4171–4178.
   PubMedGoogle Scholar
• CUSHMAN M, GOLEBIEWSKI WM, POMMIER Y, MAZUM-DER A, REYMEN D, DECLERCQ E, GRAHAM L, RICE WG: Cosalane analogues with enhanced potencies as inhibitors of 111V-1 protease and integrase. J. Med. Chem. (1995) 38:443–452.
   PubMedGoogle Scholar
• RAGHA VAN K, BOULAMWIMI JK, FESEN MR, POMMIER Y, KOWN KW, WEINSTEIN JN: Three-dimensional quantita-tive structure-activity relationship (QSAR) of HIV late-vase inhibitors: a comparative molecular field analysis (CoMFA) study. J. Med. Chem. (1995) 38:890–897.
   PubMedGoogle Scholar
• RICE WG, SUPKO JG, MALSPEIS L, BUCKHEIT JR. RW, CLANTO D, BU M, GRAHAM L, SCHAEFFER CA, TURPIN JA,DOMAGALA J, GOGLIOTTI R, BADER JP, HALLIDAY SM, COREN L, SOWDER II RC, ARTHUR LO, HENDERSON LE: Inhibitors of HIV nuckocapsid protein zinc fingers as candidates for the treatment of AIDS. Science (1995) 270:1194–1197.
   PubMed Web of Science ®Google Scholar
• FRIDELL RA, HARDING LS, BOGERD HP, CULLEN BR: Identification of a novel human zinc finger protein that specifically interacts with the activation domain of leutiviral Tat proteins. Virology (1995) 209:347–357 .
   PubMedGoogle Scholar
• OTSLTKA M, FUJITA M, TSUTOMU A, SHUNSUKE I, SUGIURA Y, YAMAMOTO T, NOVE J-I: Novel zinc chelators with dual activity in the inhibition of B site-binding proteinsand NF-KB. J. Med. Chem. (1995) 38:3264–3270.
   PubMedGoogle Scholar
• BILLICH A, HAMMERSCHMID F, PEICHL P, WENGER R, ZENKE G, QUESNIAUX V, ROSENWIRTH B: Mode of actionof SDZ NIM 811, a non-immunosuppressive cyckmporin A analog with activity against human immunodefi-ciency virus (HIV) type 1: interference with 111V pro-tein-cyclophilin A interactions. J. Virol. (1995) 69:2451–2461.
   PubMedGoogle Scholar
• STEINKASSERRER A, HARRISON R, BILLICH A, HAMMERSCHMID F, WERNER G, WOLFF B, PEICHL P, PALFI G, SCHNITZEL W, MLYNAR E, ROSENWIRTH B: Mode of action of SDZ NIM 811, a non-imuunosuppressive cy-closporin A analog with activity against human immu-nodeficiency virus type 1 (HIV): interference with early and late events in HIV-1 replication. J. Virol. (1995) 69:814–824.
   PubMedGoogle Scholar
• LEUNG DW, PETERSON PK, WEEKS R, GEKKER G, CHAOCC, KAPLAN AM, BALANTAC N, TOMPIUNS C, UNDERINER CF, BURSTEN S: CT-2576, an inhibitor of phospholipid sign. ling, suppresses constitutive and induced expres-sion of human immunodeficiency virus. Proc. Natl. Acad. Sci. USA (1995) 92:4813–4817.
   PubMedGoogle Scholar
• LEVY DN, REFAELY Y, WEINER DB: Fxtracelhdar Vprprotein increases cellular permissiveness to human immunodeficiency virus replication and reactivates vi-rus from latency. J Virol. (1995) 69:1243–1252.
   PubMed Web of Science ®Google Scholar
• MACRAEDIE IG, CASTELLI LA, HEWISH DR, KIRICPATRICK A, WARD AC, AZAD AA: A domain of human immunode-ficiency virus type 1 Vpr containing repeated H(S/F)RIG amino add motifs causes cell growth arrest and struc-tural defects. Proc. Natl. Acad. Sci. USA(1995) 92:2770–2774.
   PubMedGoogle Scholar
• WV X, LIU H, XINO H, KIM J, SESHAIAH P, NATSOULIS G, BOEICE JD, HAHN BH, KAPPES JC: Targeting foreign proteins to human immunodeficiency virus particles via fusion with Vpr and Vpx. j Vim!. (1995) 69:3889–339877????
   Google Scholar
• CHOWERS MY, PANDORI MN, SPINA CA, RICHMAN DD, GUATELLI JC: The growth advantage conferred by HIV-1 Nef is determined at the level of viral DNA formation and is independent of CD4 down regulation. Virology (1995) 212:451–457.
   PubMed Web of Science ®Google Scholar
• MJI I FR MD, WARMERDAM MT, PAGE KA, FEINBERG MB, GREENE WC: Expression of the human imnmunodefi-ciency virus type 1 (HIV-1) nef gene during HIV-1 production increases progency particle infectivity in-dependently of gp160 or viral entry. J. Virol. (1995) 69:579–584.
   PubMedGoogle Scholar
• BANDRES JC, SHAW AS, RATNER L: HIV-1 Nef proteindown regulation of CD4 surface expression: relevance of lck binding domain of CD4. Virology (1995) 207:338–341.
   PubMedGoogle Scholar
• SALGHETTI S, MARIAN' R, SHOWRONSKI J: Human immu-nodeficiency virus type 1 Nef and p561c1c protein-tyro-sine kinase interact with a common element in CD4 cytoplasmic tail. Proc. Natl. Acad. &I. USA (1995) 92:349–353.
   PubMedGoogle Scholar
• SCHWARTZ 0, DAUTRY-VARSAT A, GOUD B, MARECHAL V, SUBTIL A, HEARD JM, DANOS 0: Human immunode-ficiency virus type 1 Nef induces accumulation of CD4 In early endosomer. J. Virol. (1995) 69:528–533.
   PubMedGoogle Scholar
• GREENWAY A, AZAD A, MCPHEE D: Human Immunode-▪ficiency virus type 1 Nef protein inhibits activation pathways in peripheral blood mononuclear cells and T-cell lines. J. Virol. (1995) 69:1842–1850.
   PubMedGoogle Scholar
• DEACON NJ, TSYKIN A, SOLOMON A, SMITH K, LUNDOORD-MENTING M, HOOKER DJ, MCPHEE DA, GREEN-WAY AL, ELLETT A, CHATFIELD C, LAWSON VA, CROWE S, MAERZ A, SONZA S, LEARMONT J, SULLIVAN JS, CUN-NINHGAM A, DWYER D, DAWTON D, HILLS J: Genomic structures of an attenuated quasi species of HIV-1 from a blood transfusion donor and recipients. Science (1995) 270:988–991.
   PubMed Web of Science ®Google Scholar
• LISZIEWICZ J, SUN D, LISZIEWICZ A, GALLO RC: Antitatgene therapy: a candidate for late-stage AIDS patients. Gene. Ther. (1995) 2:218–222.
   PubMed Web of Science ®Google Scholar
• CARUSO M, SALOMON B. ZHANG S, BRISSON E, CLAVEL F, LOWY I, KLATZMANN D: Expression of a Tat-indudble herpes simplex virus-thymidine kinase gene protects acyclovir-treated CD4 cells fromspread by con-ditional suicide and inhibition of reverse transcription. Virology (1995) 206:495–503.
   PubMedGoogle Scholar
• CHOKEKEJCHAI S, SHIRASAKA T, WEINSTEIN JN, MITSUYA H: In vitro anti-HIV-1 activity of HIV protease inhibitor KNI-272 in resting and activated cells: implication for its combined use with AZT or &II. Antiviral Res. (1995) 28:25–38.
   PubMedGoogle Scholar
• COMPAGNIE DE DEVELOPPEMENT AGUETANT, W09517899 (1995).
   Google Scholar
• MERCK & CO., INC., W09510281 (1995).
   Google Scholar
• BIOCHEM. PHARMA., INC., W09529176 (1995).
   Google Scholar
• EMORY UNIVERSITY, W09515333 (1995).
   Google Scholar
• SANKYO ECK, JP7118289-A (1995).
   Google Scholar
• GERON CORP., et al., W09513383 (1995).
   Google Scholar
• DUPONT MERCK PHARM. CO., US5430155 (1995).
   Google Scholar
• ABBOTT LABS., U55455351 (1995).
   Google Scholar
• MERCK & CO., INC., W0956688 (1995).
   Google Scholar
• ABBOTT LABS., W09520384 (1995).
   Google Scholar
• MERCK & CO., GB2287938-A (1995).
   Google Scholar
• AGOURON PHARM., INC., W09509843 (1995).
   Google Scholar
• VERTEX PHARM., INC., W09524385 (1995).
   Google Scholar
• PARKE DAVIS & CO., W09514012 (1995).
   Google Scholar
• PARKE DAVIS & CO., W09514011 (1995).
   Google Scholar
• PARKE DAVIS & CO., W09514013 (1995).
   Google Scholar
• MERRELL DOW PHARM., INC., W09521186 (1995).
   Google Scholar
• ELI LILLY & CO., W09520965 (1995).
   Google Scholar
• ELI LILLY & CO., W09520962 (1995).
   Google Scholar
• ELI LILLY & CO., W09521164 (1995).
   Google Scholar
• UNIVERSITY OF CALIFORNIA, W09509856 (1995).
   Google Scholar
• MERCIAN ICK, JP7145161-A (1995).
   Google Scholar
• BIOMOLECULAR RES. INST. LTD. W09526361 (1995).
   Google Scholar
• LYNX THERAPEUTICS, INC., W09501456 (1995).
   Google Scholar
• RIBOZYME PHARMACEUTICALS, INC., W09504818 (1995).
   Google Scholar
• MACFARLANE BURNET CENTRE FOR MEDICAL RESEARCH, W09521912 (1995).
   Google Scholar
• cynx CORP., W09510265 (1995).
   Google Scholar