The N137 and P140 amino acids in the p51 and the P95 amino acid in the p66 subunit of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase are instrumental to maintain catalytic activity and to design new classes of anti-HIV-1 drugs

FEBS Letters

Volumn 579, Issue 11, 2005, Pages 2294-2300

  Auwerx, Joeri ^a   Van Nieuwenhove, Joke ^a   Rodríguez Barrios, Fátima ^b   De Castro, Sonia ^c   Velázquez, Sonsoles ^c   Ceccherini Silberstein, Francesca ^d   De Clercq, Erik ^a   Camarasa, María José ^c   Perno, Carlo Federico ^d   Gago, Federico ^b   Balzarini, Jan ^a  

^a REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

^b UNIVERSITY OF ALCALÁ   (Spain)

^c INSTITUTO DE QUÍMICA MÉDICA   (Spain)

^d UNIVERSITY OF ROME TOR VERGATA   (Italy)

Author keywords

Anti HIV 1 drugs; HIV 1; p51; p66

Indexed keywords

2 ETHYL 7 FLUORO 1,2,3,4 TETRAHYDRO 3 OXO 1 QUINOXALINECARBOXYLIC ACID ISOPROPYL ESTER; 2',3' DIDEHYDRO 2',3' DIDEOXYTHYMIDINE 5' TRIPHOSPHATE; 2',3' DIDEOXYGUANOSINE TRIPHOSPHATE; ALANINE; AMINO ACID; ASPARTIC ACID; CALANOLIDE A; DELAVIRDINE; EFAVIRENZ; FOSCARNET; GLUTAMIC ACID; GLUTAMINE; HISTIDINE; LYSINE; MUTANT PROTEIN; N [4 CHLORO 3 (3 METHYL 2 BUTENYLOXY)PHENYL] 2 METHYL 3 FURANCARBOTHIOAMIDE; NEVIRAPINE; NUCLEOSIDE; PROTEIN SUBUNIT; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR; SERINE; THREONINE; THYMIDINE DERIVATIVE; TYROSINE; UNCLASSIFIED DRUG; UREA; [2',5' BIS O (TERT BUTYLDIMETHYLSILYL) BETA DEXTRO RIBOFURANOSYL] 3' SPIRO 5'' (4'' AMINO 1'',2'' OXATHIOLE 2'',2'' DIOXIDE);

AMINO ACID SUBSTITUTION; ARTICLE; BETA CHAIN; CATALYSIS; CONTROLLED STUDY; DENATURATION; DIMERIZATION; DRUG DESIGN; ENZYME ACTIVITY; GENE MUTATION; HUMAN IMMUNODEFICIENCY VIRUS 1; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN FUNCTION; PROTEIN INTERACTION; PROTEIN STABILITY; SENSITIVITY ANALYSIS; STATISTICAL SIGNIFICANCE;

EID: 20244372866     PISSN: 00145793     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.febslet.2005.02.077     Document Type: Article

References (27)

1. E. De Clercq Antiviral drugs in current clinical use J. Clin. Virol. 30 2004 115 133
2. E. De Clercq Reverse transcriptase inhibitors as anti-HIV drugs R.E. Unger J. Kreuter H. Rübsamen-Waigmann Antivirals Against AIDS 2000 Marcel Dekker NY 107 150
3. J. Balzarini Current status of the non-nucleoside reverse transcriptase inhibitors of human immunodeficiency virus type 1 Curr. Top. Med. Chem. 4 2004 921 944
4. J. Balzarini Suppression of resistance to drugs targeted to human immunodeficiency virus reverse transcriptase by combination therapy Biochem. Pharmacol. 58 1999 1 27
5. H. Pelemans, R. Esnouf, E. De Clercq, and J. Balzarini Mutational analysis of trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors Mol. Pharmacol. 57 2000 954 960
6. H. Pelemans, R.M. Esnouf, H. Jonckheere, E. De Clercq, and J. Balzarini Mutational analysis of Tyr-318 within the non-nucleoside reverse transcriptase inhibitor binding pocket of human immunodeficiency virus type I reverse transcriptase J. Biol. Chem. 273 1998 34234 34239
7. G. Tachedjian, H.E. Aronson, M. de los Santos, J. Seehra, J.M. McCoy, and S.P. Goff Role of residues in the tryptophan repeat motif for HIV-1 reverse transcriptase dimerization J. Mol. Biol. 326 2003 381 396
8. T. Restle, B. Muller, and R.S. Goody RNase H activity of HIV reverse transcriptases is confined exclusively to the dimeric forms FEBS Lett. 300 1992 97 100
9. T. Restle, B. Muller, and R.S. Goody Dimerization of human immunodeficiency virus type 1 reverse transcriptase. A target for chemotherapeutic intervention J. Biol. Chem. 265 1990 8986 8988
10. P.K. Pandey, N. Kaushik, T.T. Talele, P.N. Yadav, and V.N. Pandey The beta7-beta8 loop of the p51 subunit in the heterodimeric (p66/p51) human immunodeficiency virus type 1 reverse transcriptase is essential for the catalytic function of the p66 subunit Biochemistry 40 2001 9505 9512
11. P.K. Pandey, N. Kaushik, K. Singh, B. Sharma, A.K. Upadhyay, S. Kumar, D. Harris, and V.N. Pandey Insertion of a small peptide of six amino acids into the beta7-beta8 loop of the p51 subunit of HIV-1 reverse transcriptase perturbs the heterodimer and affects its activities BMC Biochem. 3 2002 18
12. L. Menéndez-Arias, A. Abraha, M.E. Quiñones-Mateu, A. Mas, M.J. Camarasa, and E.J. Arts Functional characterization of chimeric reverse transcriptases with polypeptide subunits of highly divergent HIV-1 group M and O strains J. Biol. Chem. 276 2001 27470 27479
13. M.J. Pérez-Pérez, A. San-Félix, J. Balzarini, E. De Clercq, and M.J. Camarasa TSAO analogues. Stereospecific synthesis and anti-HIV-1 activity of 1-[2′,5′-bis-O-(tert-butyldimethylsilyl)- beta-D-ribofuranosyl]-3′-spiro-5″-(4″-amino-1″, 2″-oxathiole 2″,2″-dioxide) pyrimidine and pyrimidine-modified nucleosides J. Med. Chem. 35 1992 2988 2995
14. R.T. D'Aquila, and W.C. Summers HIV-1 reverse transcriptase/ribonuclease H: high level expression in Escherichia coli from a plasmid constructed using the polymerase chain reaction J. Acquir. Immune Defic. Syndr. 2 1989 579 587
15. H. Jonckheere, K. De Vreese, Z. Debyser, J. Vandekerckhove, J. Balzarini, J. Desmyter, E. De Clercq, and J. Anné A two plasmid co-expression system in Escherichia coli for the production of virion-like reverse transcriptase of the human immunodeficiency virus type 1 J. Virol. Methods 61 1996 113 125
16. J. Auwerx, R. Esnouf, E. De Clercq, and J. Balzarini Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors Mol. Pharmacol. 65 2004 244 251
17. H. Huang, R. Chopra, G.L. Verdine, and S.C. Harrison Structure of a covalently trapped catalytic complex of HIV-1 reverse transcriptase: implications for drug resistance Science 282 1998 1669 1675
18. F. Rodríguez-Barrios, C. Pérez, E. Lobatón, S. Velázquez, C. Chamorro, A. San-Félix, M.J. Pérez- Pérez, M.J. Camarasa, H. Pelemans, J. Balzarini, and F. Gago Identification of a putative binding site for [2′,5′-bis-O-(tert- butyldimethylsilyl)-beta-d-ribofuranosyl]-3′-spiro-5″-(4″- amino-1″,2″-oxathiole-2″,2″-dioxide)thymine (TSAO) derivatives at the p51-p55 interface of HIV-1 reverse transcriptase J. Med. Chem. 44 2001 1853 1865
19. G. Tachedjian, M. Orlova, S.G. Sarafianos, E. Arnold, and S. Goff Nonnucleoside reverse transcriptase inhibitors are chemical enhancers of dimerization of the HIV type 1 reverse transcriptase Proc. Natl. Acad. Sci. USA 98 2001 7188 7193
20. N. Sluis-Cremer, and G. Tachedjian Modulation of the oligomeric structures of HIV-1 retroviral enzymes by synthetic peptides and small molecules Eur. J. Biochem. 269 2002 5103 5111
21. G. Tachedjian, and S.P. Goff The effect of NNRTIs on HIV reverse transcriptase dimerization Curr. Opin. Invest. Drugs 4 2003 966 973
22. D. Harris, R. Lee, H.S. Misra, P.K. Pandey, and V.N. Pandey The p51 subunit of human immunodeficiency virus type 1 reverse transcriptase is essential in loading the p66 subunit on the template primer Biochemistry 37 1998 5903 5908
23. N. Sluis-Cremer, G.I. Dmitrienko, J. Balzarini, M.J. Camarasa, and M.A. Parniak Human immunodeficiency virus type 1 reverse transcriptase dimer destabilization by 1-[spiro[4″-amino-2″,2″-dioxo-1″, 2″-oxathiole-5″,3′-[2′,5′-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]]]-3-ethylthy mine Biochemistry 39 2000 1427 1433
24. N. Sluis-Cremer, D. Arion, and M.A. Parniak Destabilization of the HIV-1 reverse transcriptase dimer upon interaction with N-acyl hydrazone inhibitors Mol. Pharmacol. 62 2002 398 405
25. M.J. Currens, J.M. Mariner, J.B. McMahon, M.R. Boyd, N. Shulman, and M. Winters Kinetic analysis of inhibition of human immunodeficiency virus type-1 reverse transcriptase by calanolide A J. Pharmacol. Exp. Ther. 279 1996 652 661
26. J. Balzarini, H. Pelemans, R. Esnouf, and E. De Clercq A novel mutation (F227L) arises in the reverse transcriptase of human immunodeficiency virus type 1 on dose-escalating treatment of HIV type 1-infected cell cultures with the nonnucleoside reverse transcriptase inhibitor thiocarboxanilide UC-781 AIDS Res. Hum. Retroviruses 14 1998 255 260
27. J. Ren, C.E. Nichols, P.P. Chamberlain, K.L. Weaver, S.A. Short, and D.K. Stammers Crystal structures of HIV-1 reverse transcriptases mutated at codons 100, 106 and 108 and mechanisms of resistance to non-nucleoside inhibitors J. Mol. Biol. 336 2004 569 578