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Items: 1 to 50 of 165

1.

Conformational Changes in HIV-1 Reverse Transcriptase that Facilitate Its Maturation.

Slack RL, Ilina TV, Xi Z, Giacobbi NS, Kawai G, Parniak MA, Sarafianos SG, Sluis Cremer N, Ishima R.

Structure. 2019 Oct 1;27(10):1581-1593.e3. doi: 10.1016/j.str.2019.08.004. Epub 2019 Aug 27.

PMID:
31471129
2.

Nanocrystal Formulation Improves Vaginal Delivery of CSIC for HIV Prevention.

Gong T, Patel SK, Parniak MA, Ballou B, Rohan LC.

AAPS PharmSciTech. 2019 Aug 13;20(7):286. doi: 10.1208/s12249-019-1503-z.

PMID:
31410664
3.

Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.

Tang J, Do HT, Huber AD, Casey MC, Kirby KA, Wilson DJ, Kankanala J, Parniak MA, Sarafianos SG, Wang Z.

Eur J Med Chem. 2019 Mar 15;166:390-399. doi: 10.1016/j.ejmech.2019.01.081. Epub 2019 Feb 2.

PMID:
30739822
4.

6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H.

Wang L, Tang J, Huber AD, Casey MC, Kirby KA, Wilson DJ, Kankanala J, Parniak MA, Sarafianos SG, Wang Z.

Eur J Med Chem. 2018 Aug 5;156:680-691. doi: 10.1016/j.ejmech.2018.07.035. Epub 2018 Jul 17.

5.

6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.

Wang L, Tang J, Huber AD, Casey MC, Kirby KA, Wilson DJ, Kankanala J, Xie J, Parniak MA, Sarafianos SG, Wang Z.

Eur J Med Chem. 2018 Aug 5;156:652-665. doi: 10.1016/j.ejmech.2018.07.039. Epub 2018 Jul 17.

6.

Effect of tRNA on the Maturation of HIV-1 Reverse Transcriptase.

Ilina TV, Slack RL, Elder JH, Sarafianos SG, Parniak MA, Ishima R.

J Mol Biol. 2018 Jun 22;430(13):1891-1900. doi: 10.1016/j.jmb.2018.02.027. Epub 2018 May 8.

7.

Preformulation and Vaginal Film Formulation Development of Microbicide Drug Candidate CSIC for HIV prevention.

Gong T, Zhang W, Parniak MA, Graebing PW, Moncla B, Gupta P, Empey KM, Rohan LC.

J Pharm Innov. 2017 Jun;12(2):142-154. doi: 10.1007/s12247-017-9274-0. Epub 2017 Mar 3.

8.

A 2-Hydroxyisoquinoline-1,3-Dione Active-Site RNase H Inhibitor Binds in Multiple Modes to HIV-1 Reverse Transcriptase.

Kirby KA, Myshakina NA, Christen MT, Chen YL, Schmidt HA, Huber AD, Xi Z, Kim S, Rao RK, Kramer ST, Yang Q, Singh K, Parniak MA, Wang Z, Ishima R, Sarafianos SG.

Antimicrob Agents Chemother. 2017 Sep 22;61(10). pii: e01351-17. doi: 10.1128/AAC.01351-17. Print 2017 Oct.

9.

Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity.

Vernekar SKV, Tang J, Wu B, Huber AD, Casey MC, Myshakina N, Wilson DJ, Kankanala J, Kirby KA, Parniak MA, Sarafianos SG, Wang Z.

J Med Chem. 2017 Jun 22;60(12):5045-5056. doi: 10.1021/acs.jmedchem.7b00440. Epub 2017 May 31.

10.

Synthesis, biological evaluation and molecular modeling of 2-Hydroxyisoquinoline-1,3-dione analogues as inhibitors of HIV reverse transcriptase associated ribonuclease H and polymerase.

Tang J, Vernekar SKV, Chen YL, Miller L, Huber AD, Myshakina N, Sarafianos SG, Parniak MA, Wang Z.

Eur J Med Chem. 2017 Jun 16;133:85-96. doi: 10.1016/j.ejmech.2017.03.059. Epub 2017 Mar 29.

11.

3-Hydroxypyrimidine-2,4-Diones as Novel Hepatitis B Virus Antivirals Targeting the Viral Ribonuclease H.

Huber AD, Michailidis E, Tang J, Puray-Chavez MN, Boftsi M, Wolf JJ, Boschert KN, Sheridan MA, Leslie MD, Kirby KA, Singh K, Mitsuya H, Parniak MA, Wang Z, Sarafianos SG.

Antimicrob Agents Chemother. 2017 May 24;61(6). pii: e00245-17. doi: 10.1128/AAC.00245-17. Print 2017 Jun.

12.

Structural basis of HIV inhibition by translocation-defective RT inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA).

Salie ZL, Kirby KA, Michailidis E, Marchand B, Singh K, Rohan LC, Kodama EN, Mitsuya H, Parniak MA, Sarafianos SG.

Proc Natl Acad Sci U S A. 2016 Aug 16;113(33):9274-9. doi: 10.1073/pnas.1605223113. Epub 2016 Aug 3.

13.

Efficient Inhibition of HIV Replication in the Gastrointestinal and Female Reproductive Tracts of Humanized BLT Mice by EFdA.

Shanmugasundaram U, Kovarova M, Ho PT, Schramm N, Wahl A, Parniak MA, Garcia JV.

PLoS One. 2016 Jul 20;11(7):e0159517. doi: 10.1371/journal.pone.0159517. eCollection 2016.

14.

Design, Synthesis, and Biological Evaluations of Hydroxypyridonecarboxylic Acids as Inhibitors of HIV Reverse Transcriptase Associated RNase H.

Kankanala J, Kirby KA, Liu F, Miller L, Nagy E, Wilson DJ, Parniak MA, Sarafianos SG, Wang Z.

J Med Chem. 2016 May 26;59(10):5051-62. doi: 10.1021/acs.jmedchem.6b00465. Epub 2016 Apr 29.

15.

3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations.

Tang J, Liu F, Nagy E, Miller L, Kirby KA, Wilson DJ, Wu B, Sarafianos SG, Parniak MA, Wang Z.

J Med Chem. 2016 Mar 24;59(6):2648-59. doi: 10.1021/acs.jmedchem.5b01879. Epub 2016 Mar 8.

16.

Nucleotide Sugar Pucker Preference Mitigates Excision by HIV-1 RT.

Yamada K, Wahba AS, Bernatchez JA, Ilina T, Martínez-Montero S, Habibian M, Deleavey GF, Götte M, Parniak MA, Damha MJ.

ACS Chem Biol. 2015 Sep 18;10(9):2024-33. doi: 10.1021/acschembio.5b00263. Epub 2015 Jul 22.

17.

Structural integrity of the ribonuclease H domain in HIV-1 reverse transcriptase.

Slack RL, Spiriti J, Ahn J, Parniak MA, Zuckerman DM, Ishima R.

Proteins. 2015 Aug;83(8):1526-38. doi: 10.1002/prot.24843. Epub 2015 Jul 1.

18.

Oral administration of the nucleoside EFdA (4'-ethynyl-2-fluoro-2'-deoxyadenosine) provides rapid suppression of HIV viremia in humanized mice and favorable pharmacokinetic properties in mice and the rhesus macaque.

Stoddart CA, Galkina SA, Joshi P, Kosikova G, Moreno ME, Rivera JM, Sloan B, Reeve AB, Sarafianos SG, Murphey-Corb M, Parniak MA.

Antimicrob Agents Chemother. 2015 Jul;59(7):4190-8. doi: 10.1128/AAC.05036-14. Epub 2015 May 4.

19.

Vaginal Microbicide Film Combinations of Two Reverse Transcriptase Inhibitors, EFdA and CSIC, for the Prevention of HIV-1 Sexual Transmission.

Zhang W, Hu M, Shi Y, Gong T, Dezzutti CS, Moncla B, Sarafianos SG, Parniak MA, Rohan LC.

Pharm Res. 2015 Sep;32(9):2960-72. doi: 10.1007/s11095-015-1678-2. Epub 2015 Mar 21.

20.

Synthesis and properties of 2'-deoxy-2',4'-difluoroarabinose-modified nucleic acids.

Martínez-Montero S, Deleavey GF, Dierker-Viik A, Lindovska P, Ilina T, Portella G, Orozco M, Parniak MA, González C, Damha MJ.

J Org Chem. 2015 Mar 20;80(6):3083-91. doi: 10.1021/jo502948t. Epub 2015 Mar 5.

21.

Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1,3-diones: dual inhibition against HIV reverse transcriptase-associated RNase H and polymerase with antiviral activities.

Vernekar SK, Liu Z, Nagy E, Miller L, Kirby KA, Wilson DJ, Kankanala J, Sarafianos SG, Parniak MA, Wang Z.

J Med Chem. 2015 Jan 22;58(2):651-64. doi: 10.1021/jm501132s. Epub 2014 Dec 30.

22.

4'-Ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) inhibits HIV-1 reverse transcriptase with multiple mechanisms.

Michailidis E, Huber AD, Ryan EM, Ong YT, Leslie MD, Matzek KB, Singh K, Marchand B, Hagedorn AN, Kirby KA, Rohan LC, Kodama EN, Mitsuya H, Parniak MA, Sarafianos SG.

J Biol Chem. 2014 Aug 29;289(35):24533-48. doi: 10.1074/jbc.M114.562694. Epub 2014 Jun 26.

23.

Structure of a dihydroxycoumarin active-site inhibitor in complex with the RNase H domain of HIV-1 reverse transcriptase and structure-activity analysis of inhibitor analogs.

Himmel DM, Myshakina NS, Ilina T, Van Ry A, Ho WC, Parniak MA, Arnold E.

J Mol Biol. 2014 Jul 15;426(14):2617-31. doi: 10.1016/j.jmb.2014.05.006. Epub 2014 May 17.

24.

The p66 immature precursor of HIV-1 reverse transcriptase.

Sharaf NG, Poliner E, Slack RL, Christen MT, Byeon IJ, Parniak MA, Gronenborn AM, Ishima R.

Proteins. 2014 Oct;82(10):2343-52. doi: 10.1002/prot.24594. Epub 2014 May 12.

25.

In vitro transport characteristics of EFdA, a novel nucleoside reverse transcriptase inhibitor using Caco-2 and MDCKII cell monolayers.

Zhang W, Parniak MA, Sarafianos SG, Empey PE, Rohan LC.

Eur J Pharmacol. 2014 Jun 5;732:86-95. doi: 10.1016/j.ejphar.2014.03.022. Epub 2014 Mar 29.

26.

Development of a vaginal delivery film containing EFdA, a novel anti-HIV nucleoside reverse transcriptase inhibitor.

Zhang W, Parniak MA, Sarafianos SG, Cost MR, Rohan LC.

Int J Pharm. 2014 Jan 30;461(1-2):203-13. doi: 10.1016/j.ijpharm.2013.11.056. Epub 2013 Dec 9.

27.

Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus.

Sirivolu VR, Vernekar SK, Ilina T, Myshakina NS, Parniak MA, Wang Z.

J Med Chem. 2013 Nov 14;56(21):8765-80. doi: 10.1021/jm401232v. Epub 2013 Oct 28.

28.

Effects of substitutions at the 4' and 2 positions on the bioactivity of 4'-ethynyl-2-fluoro-2'-deoxyadenosine.

Kirby KA, Michailidis E, Fetterly TL, Steinbach MA, Singh K, Marchand B, Leslie MD, Hagedorn AN, Kodama EN, Marquez VE, Hughes SH, Mitsuya H, Parniak MA, Sarafianos SG.

Antimicrob Agents Chemother. 2013 Dec;57(12):6254-64. doi: 10.1128/AAC.01703-13. Epub 2013 Oct 7.

29.

Preformulation studies of EFdA, a novel nucleoside reverse transcriptase inhibitor for HIV prevention.

Zhang W, Parniak MA, Mitsuya H, Sarafianos SG, Graebing PW, Rohan LC.

Drug Dev Ind Pharm. 2014 Aug;40(8):1101-11. doi: 10.3109/03639045.2013.809535. Epub 2013 Jul 10.

30.

Hypersusceptibility mechanism of Tenofovir-resistant HIV to EFdA.

Michailidis E, Ryan EM, Hachiya A, Kirby KA, Marchand B, Leslie MD, Huber AD, Ong YT, Jackson JC, Singh K, Kodama EN, Mitsuya H, Parniak MA, Sarafianos SG.

Retrovirology. 2013 Jun 24;10:65. doi: 10.1186/1742-4690-10-65.

31.

Evaluation of Combinations of 4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine with Clinically Used Antiretroviral Drugs.

Hachiya A, Reeve AB, Marchand B, Michailidis E, Ong YT, Kirby KA, Leslie MD, Oka S, Kodama EN, Rohan LC, Mitsuya H, Parniak MA, Sarafianos SG.

Antimicrob Agents Chemother. 2013 Sep;57(9):4554-4558. doi: 10.1128/AAC.00283-13. Epub 2013 Jun 24.

32.

The utility of self-emulsifying oil formulation to improve the poor solubility of the anti HIV drug CSIC.

Obitte NC, Rohan LC, Adeyeye CM, Parniak MA, Esimone CO.

AIDS Res Ther. 2013 May 31;10(1):14. doi: 10.1186/1742-6405-10-14.

33.

Inhibitors of HIV-1 Reverse Transcriptase-Associated Ribonuclease H Activity.

Ilina T, Labarge K, Sarafianos SG, Ishima R, Parniak MA.

Biology (Basel). 2012 Oct 19;1(3):521-41. doi: 10.3390/biology1030521.

34.

The hepatitis B virus ribonuclease H is sensitive to inhibitors of the human immunodeficiency virus ribonuclease H and integrase enzymes.

Tavis JE, Cheng X, Hu Y, Totten M, Cao F, Michailidis E, Aurora R, Meyers MJ, Jacobsen EJ, Parniak MA, Sarafianos SG.

PLoS Pathog. 2013 Jan;9(1):e1003125. doi: 10.1371/journal.ppat.1003125. Epub 2013 Jan 22.

35.

Effect of translocation defective reverse transcriptase inhibitors on the activity of N348I, a connection subdomain drug resistant HIV-1 reverse transcriptase mutant.

Michailidis E, Singh K, Ryan EM, Hachiya A, Ong YT, Kirby KA, Marchand B, Kodama EN, Mitsuya H, Parniak MA, Sarafianos SG.

Cell Mol Biol (Noisy-le-grand). 2012 Dec 22;58(1):187-95.

36.

The anti-HIV microbicide candidate RC-101 inhibits pathogenic vaginal bacteria without harming endogenous flora or mucosa.

Eade CR, Cole AL, Diaz C, Rohan LC, Parniak MA, Marx P, Tarwater PM, Gupta P, Cole AM.

Am J Reprod Immunol. 2013 Feb;69(2):150-8. doi: 10.1111/aji.12036. Epub 2012 Nov 20.

37.

Biochemical mechanism of HIV-1 resistance to rilpivirine.

Singh K, Marchand B, Rai DK, Sharma B, Michailidis E, Ryan EM, Matzek KB, Leslie MD, Hagedorn AN, Li Z, Norden PR, Hachiya A, Parniak MA, Xu HT, Wainberg MA, Sarafianos SG.

J Biol Chem. 2012 Nov 2;287(45):38110-23. doi: 10.1074/jbc.M112.398180. Epub 2012 Sep 6.

38.

Structural basis of the allosteric inhibitor interaction on the HIV-1 reverse transcriptase RNase H domain.

Christen MT, Menon L, Myshakina NS, Ahn J, Parniak MA, Ishima R.

Chem Biol Drug Des. 2012 Nov;80(5):706-16. doi: 10.1111/cbdd.12010. Epub 2012 Aug 31.

39.

Response of simian immunodeficiency virus to the novel nucleoside reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine in vitro and in vivo.

Murphey-Corb M, Rajakumar P, Michael H, Nyaundi J, Didier PJ, Reeve AB, Mitsuya H, Sarafianos SG, Parniak MA.

Antimicrob Agents Chemother. 2012 Sep;56(9):4707-12. doi: 10.1128/AAC.00723-12. Epub 2012 Jun 19.

40.
41.

The safety, persistence, and acceptability of an antiretroviral microbicide candidate UC781.

Bunge K, Macio I, Meyn L, Noguchi L, Parniak MA, Schwartz JL, Moncla B, Hillier S.

J Acquir Immune Defic Syndr. 2012 Aug 1;60(4):337-43. doi: 10.1097/QAI.0b013e3182575914.

PMID:
22495787
42.

A thermodynamic study of the cyclodextrin-UC781 inclusion complex using a HPLC method.

Yang H, Parniak MA, Hillier SL, Rohan LC.

J Incl Phenom Macrocycl Chem. 2012 Apr;72(3-4):459-465.

43.

Structural and inhibition studies of the RNase H function of xenotropic murine leukemia virus-related virus reverse transcriptase.

Kirby KA, Marchand B, Ong YT, Ndongwe TP, Hachiya A, Michailidis E, Leslie MD, Sietsema DV, Fetterly TL, Dorst CA, Singh K, Wang Z, Parniak MA, Sarafianos SG.

Antimicrob Agents Chemother. 2012 Apr;56(4):2048-61. doi: 10.1128/AAC.06000-11. Epub 2012 Jan 17.

44.

First-in-class small molecule inhibitors of the single-strand DNA cytosine deaminase APOBEC3G.

Li M, Shandilya SM, Carpenter MA, Rathore A, Brown WL, Perkins AL, Harki DA, Solberg J, Hook DJ, Pandey KK, Parniak MA, Johnson JR, Krogan NJ, Somasundaran M, Ali A, Schiffer CA, Harris RS.

ACS Chem Biol. 2012 Mar 16;7(3):506-17. doi: 10.1021/cb200440y. Epub 2012 Jan 17.

45.

Biochemical, inhibition and inhibitor resistance studies of xenotropic murine leukemia virus-related virus reverse transcriptase.

Ndongwe TP, Adedeji AO, Michailidis E, Ong YT, Hachiya A, Marchand B, Ryan EM, Rai DK, Kirby KA, Whatley AS, Burke DH, Johnson M, Ding S, Zheng YM, Liu SL, Kodama E, Delviks-Frankenberry KA, Pathak VK, Mitsuya H, Parniak MA, Singh K, Sarafianos SG.

Nucleic Acids Res. 2012 Jan;40(1):345-59. doi: 10.1093/nar/gkr694. Epub 2011 Sep 8.

46.

The effects of RNase H inhibitors and nevirapine on the susceptibility of HIV-1 to AZT and 3TC.

Davis CA, Parniak MA, Hughes SH.

Virology. 2011 Oct 25;419(2):64-71. doi: 10.1016/j.virol.2011.08.010. Epub 2011 Sep 9.

47.

Identification of alternative binding sites for inhibitors of HIV-1 ribonuclease H through comparative analysis of virtual enrichment studies.

Felts AK, Labarge K, Bauman JD, Patel DV, Himmel DM, Arnold E, Parniak MA, Levy RM.

J Chem Inf Model. 2011 Aug 22;51(8):1986-98. doi: 10.1021/ci200194w. Epub 2011 Jul 26.

48.

The sugar ring conformation of 4'-ethynyl-2-fluoro-2'-deoxyadenosine and its recognition by the polymerase active site of HIV reverse transcriptase.

Kirby KA, Singh K, Michailidis E, Marchand B, Kodama EN, Ashida N, Mitsuya H, Parniak MA, Sarafianos SG.

Cell Mol Biol (Noisy-le-grand). 2011 Feb 12;57(1):40-6.

49.

Interaction of HIV-1 reverse transcriptase ribonuclease H with an acylhydrazone inhibitor.

Gong Q, Menon L, Ilina T, Miller LG, Ahn J, Parniak MA, Ishima R.

Chem Biol Drug Des. 2011 Jan;77(1):39-47. doi: 10.1111/j.1747-0285.2010.01052.x. Epub 2010 Nov 29.

50.

Synthesis of Boranoate, Selenoate, and Thioate Analogs of AZTp(4)A and Ap(4)A.

Han Q, Sarafianos SG, Arnold E, Parniak MA, Gaffney BL, Jones RA.

Tetrahedron. 2009 Sep 19;65(38):7915-7920.

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