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Effects of Moloney Leukemia Virus 10 Protein on Hepatitis B Virus Infection and Viral Replication.

Puray-Chavez MN, Farghali MH, Yapo V, Huber AD, Liu D, Ndongwe TP, Casey MC, Laughlin TG, Hannink M, Tedbury PR, Sarafianos SG.

Viruses. 2019 Jul 17;11(7). pii: E651. doi: 10.3390/v11070651.


Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase.

Singh K, Sarafianos SG, Sönnerborg A.

Pharmaceuticals (Basel). 2019 Apr 20;12(2). pii: E62. doi: 10.3390/ph12020062. Review.


Novel Intersubunit Interaction Critical for HIV-1 Core Assembly Defines a Potentially Targetable Inhibitor Binding Pocket.

Craveur P, Gres AT, Kirby KA, Liu D, Hammond JA, Deng Y, Forli S, Goodsell DS, Williamson JR, Sarafianos SG, Olson AJ.

MBio. 2019 Mar 12;10(2). pii: e02858-18. doi: 10.1128/mBio.02858-18.


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.


CMCdG, a Novel Nucleoside Analog with Favorable Safety Features, Exerts Potent Activity against Wild-Type and Entecavir-Resistant Hepatitis B Virus.

Higashi-Kuwata N, Hayashi S, Das D, Kohgo S, Murakami S, Hattori SI, Imoto S, Venzon DJ, Singh K, Sarafianos SG, Tanaka Y, Mitsuya H.

Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02143-18. doi: 10.1128/AAC.02143-18. Print 2019 Apr.


5-Aminothiophene-2,4-dicarboxamide analogues as hepatitis B virus capsid assembly effectors.

Tang J, Huber AD, Pineda DL, Boschert KN, Wolf JJ, Kankanala J, Xie J, Sarafianos SG, Wang Z.

Eur J Med Chem. 2019 Feb 15;164:179-192. doi: 10.1016/j.ejmech.2018.12.047. Epub 2018 Dec 21.


Novel Hepatitis B Virus Capsid-Targeting Antiviral That Aggregates Core Particles and Inhibits Nuclear Entry of Viral Cores.

Huber AD, Pineda DL, Liu D, Boschert KN, Gres AT, Wolf JJ, Coonrod EM, Tang J, Laughlin TG, Yang Q, Puray-Chavez MN, Ji J, Singh K, Kirby KA, Wang Z, Sarafianos SG.

ACS Infect Dis. 2019 May 10;5(5):750-758. doi: 10.1021/acsinfecdis.8b00235. Epub 2019 Jan 14.


Strain-specific effect on biphasic DNA binding by HIV-1 integrase.

Hill KJ, Rogers LC, Njenda DT, Burke DH, Sarafianos SG, Sönnerborg A, Neogi U, Singh K.

AIDS. 2019 Mar 1;33(3):588-592. doi: 10.1097/QAD.0000000000002078.


Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2.

Wu X, Xu G, Li X, Xu W, Li Q, Liu W, Kirby KA, Loh ML, Li J, Sarafianos SG, Qu CK.

J Med Chem. 2019 Feb 14;62(3):1125-1137. doi: 10.1021/acs.jmedchem.8b00513. Epub 2018 Dec 5.


Identification of a Structural Element in HIV-1 Gag Required for Virus Particle Assembly and Maturation.

Novikova M, Adams LJ, Fontana J, Gres AT, Balasubramaniam M, Winkler DC, Kudchodkar SB, Soheilian F, Sarafianos SG, Steven AC, Freed EO.

MBio. 2018 Oct 16;9(5). pii: e01567-18. doi: 10.1128/mBio.01567-18.


Visualization of HIV-1 RNA Transcription from Integrated HIV-1 DNA in Reactivated Latently Infected Cells.

Ukah OB, Puray-Chavez M, Tedbury PR, Herschhorn A, Sodroski JG, Sarafianos SG.

Viruses. 2018 Sep 30;10(10). pii: E534. doi: 10.3390/v10100534.


The High Genetic Barrier of EFdA/MK-8591 Stems from Strong Interactions with the Active Site of Drug-Resistant HIV-1 Reverse Transcriptase.

Takamatsu Y, Das D, Kohgo S, Hayashi H, Delino NS, Sarafianos SG, Mitsuya H, Maeda K.

Cell Chem Biol. 2018 Oct 18;25(10):1268-1278.e3. doi: 10.1016/j.chembiol.2018.07.014. Epub 2018 Aug 30.


Capsid-CPSF6 Interaction Licenses Nuclear HIV-1 Trafficking to Sites of Viral DNA Integration.

Achuthan V, Perreira JM, Sowd GA, Puray-Chavez M, McDougall WM, Paulucci-Holthauzen A, Wu X, Fadel HJ, Poeschla EM, Multani AS, Hughes SH, Sarafianos SG, Brass AL, Engelman AN.

Cell Host Microbe. 2018 Sep 12;24(3):392-404.e8. doi: 10.1016/j.chom.2018.08.002. Epub 2018 Aug 30.


Structural Implications of Genotypic Variations in HIV-1 Integrase From Diverse Subtypes.

Rogers L, Obasa AE, Jacobs GB, Sarafianos SG, Sönnerborg A, Neogi U, Singh K.

Front Microbiol. 2018 Aug 2;9:1754. doi: 10.3389/fmicb.2018.01754. eCollection 2018.


Contribution of a Multifunctional Polymerase Region of Foot-and-Mouth Disease Virus to Lethal Mutagenesis.

de la Higuera I, Ferrer-Orta C, Moreno E, de Ávila AI, Soria ME, Singh K, Caridi F, Sobrino F, Sarafianos SG, Perales C, Verdaguer N, Domingo E.

J Virol. 2018 Sep 26;92(20). pii: e01119-18. doi: 10.1128/JVI.01119-18. Print 2018 Oct 15.


Antiretroviral potency of 4'-ethnyl-2'-fluoro-2'-deoxyadenosine, tenofovir alafenamide and second-generation NNRTIs across diverse HIV-1 subtypes.

Njenda DT, Aralaguppe SG, Singh K, Rao R, Sönnerborg A, Sarafianos SG, Neogi U.

J Antimicrob Chemother. 2018 Oct 1;73(10):2721-2728. doi: 10.1093/jac/dky256.


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.


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.


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.


4'-Ethynyl-2-fluoro-2'-deoxyadenosine, MK-8591: a novel HIV-1 reverse transcriptase translocation inhibitor.

Markowitz M, Sarafianos SG.

Curr Opin HIV AIDS. 2018 Jul;13(4):294-299. doi: 10.1097/COH.0000000000000467. Review.


The Heteroaryldihydropyrimidine Bay 38-7690 Induces Hepatitis B Virus Core Protein Aggregates Associated with Promyelocytic Leukemia Nuclear Bodies in Infected Cells.

Huber AD, Wolf JJ, Liu D, Gres AT, Tang J, Boschert KN, Puray-Chavez MN, Pineda DL, Laughlin TG, Coonrod EM, Yang Q, Ji J, Kirby KA, Wang Z, Sarafianos SG.

mSphere. 2018 Apr 18;3(2). pii: e00131-18. doi: 10.1128/mSphereDirect.00131-18. Print 2018 Apr 25.


Ex-vivo antiretroviral potency of newer integrase strand transfer inhibitors cabotegravir and bictegravir in HIV type 1 non-B subtypes.

Neogi U, Singh K, Aralaguppe SG, Rogers LC, Njenda DT, Sarafianos SG, Hejdeman B, Sönnerborg A.

AIDS. 2018 Feb 20;32(4):469-476. doi: 10.1097/QAD.0000000000001726.


Multiplex single-cell visualization of nucleic acids and protein during HIV infection.

Puray-Chavez M, Tedbury PR, Huber AD, Ukah OB, Yapo V, Liu D, Ji J, Wolf JJ, Engelman AN, Sarafianos SG.

Nat Commun. 2017 Dec 1;8(1):1882. doi: 10.1038/s41467-017-01693-z.


Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H.

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

Eur J Med Chem. 2017 Dec 1;141:149-161. doi: 10.1016/j.ejmech.2017.09.054. Epub 2017 Sep 28.


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.


Impact of HIV-1 Integrase L74F and V75I Mutations in a Clinical Isolate on Resistance to Second-Generation Integrase Strand Transfer Inhibitors.

Hachiya A, Kirby KA, Ido Y, Shigemi U, Matsuda M, Okazaki R, Imamura J, Sarafianos SG, Yokomaku Y, Iwatani Y.

Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00315-17. doi: 10.1128/AAC.00315-17. Print 2017 Aug.


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.


Molecular and Functional Bases of Selection against a Mutation Bias in an RNA Virus.

de la Higuera I, Ferrer-Orta C, de Ávila AI, Perales C, Sierra M, Singh K, Sarafianos SG, Dehouck Y, Bastolla U, Verdaguer N, Domingo E.

Genome Biol Evol. 2017 May 1;9(5):1212-1228. doi: 10.1093/gbe/evx075.


Exposing HIV's weaknesses.

Tedbury PR, Sarafianos SG.

J Biol Chem. 2017 Apr 7;292(14):6027-6028. doi: 10.1074/jbc.H117.777714. Epub 2017 Apr 7. Review.


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.


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.


Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity.

Kimani SG, Kumar S, Bansal N, Singh K, Kholodovych V, Comollo T, Peng Y, Kotenko SV, Sarafianos SG, Bertino JR, Welsh WJ, Birge RB.

Sci Rep. 2017 Mar 8;7:43908. doi: 10.1038/srep43908.


6-Cyclohexylmethyl-3-hydroxypyrimidine-2,4-dione as an inhibitor scaffold of HIV reverase transcriptase: Impacts of the 3-OH on inhibiting RNase H and polymerase.

Tang J, Kirby KA, Huber AD, Casey MC, Ji J, Wilson DJ, Sarafianos SG, Wang Z.

Eur J Med Chem. 2017 Mar 10;128:168-179. doi: 10.1016/j.ejmech.2017.01.041. Epub 2017 Jan 30.


Increased replication capacity following evolution of PYxE insertion in Gag-p6 is associated with enhanced virulence in HIV-1 subtype C from East Africa.

Aralaguppe SG, Winner D, Singh K, Sarafianos SG, Quiñones-Mateu ME, Sönnerborg A, Neogi U.

J Med Virol. 2017 Jan;89(1):106-111. doi: 10.1002/jmv.24610. Epub 2016 Jul 6.


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.


3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.

Wu B, Tang J, Wilson DJ, Huber AD, Casey MC, Ji J, Kankanala J, Xie J, Sarafianos SG, Wang Z.

J Med Chem. 2016 Jul 14;59(13):6136-48. doi: 10.1021/acs.jmedchem.6b00040. Epub 2016 Jun 17.


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.


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.


Factors influencing the efficacy of rilpivirine in HIV-1 subtype C in low- and middle-income countries.

Neogi U, Häggblom A, Singh K, Rogers LC, Rao SD, Amogne W, Schülter E, Zazzi M, Arnold E, Sarafianos SG, Sönnerborg A.

J Antimicrob Chemother. 2016 Feb;71(2):367-71. doi: 10.1093/jac/dkv359. Epub 2015 Oct 30.


4'-modified nucleoside analogs: potent inhibitors active against entecavir-resistant hepatitis B virus.

Takamatsu Y, Tanaka Y, Kohgo S, Murakami S, Singh K, Das D, Venzon DJ, Amano M, Higashi-Kuwata N, Aoki M, Delino NS, Hayashi S, Takahashi S, Sukenaga Y, Haraguchi K, Sarafianos SG, Maeda K, Mitsuya H.

Hepatology. 2015 Oct;62(4):1024-36. doi: 10.1002/hep.27962. Epub 2015 Aug 25.


STRUCTURAL VIROLOGY. X-ray crystal structures of native HIV-1 capsid protein reveal conformational variability.

Gres AT, Kirby KA, KewalRamani VN, Tanner JJ, Pornillos O, Sarafianos SG.

Science. 2015 Jul 3;349(6243):99-103. doi: 10.1126/science.aaa5936. Epub 2015 Jun 4.


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.


Multifunctionality of a picornavirus polymerase domain: nuclear localization signal and nucleotide recognition.

Ferrer-Orta C, de la Higuera I, Caridi F, Sánchez-Aparicio MT, Moreno E, Perales C, Singh K, Sarafianos SG, Sobrino F, Domingo E, Verdaguer N.

J Virol. 2015 Jul;89(13):6848-59. doi: 10.1128/JVI.03283-14. Epub 2015 Apr 22.


Fast hepatitis C virus RNA elimination and NS5A redistribution by NS5A inhibitors studied by a multiplex assay approach.

Liu D, Ji J, Ndongwe TP, Michailidis E, Rice CM, Ralston R, Sarafianos SG.

Antimicrob Agents Chemother. 2015;59(6):3482-92. doi: 10.1128/AAC.00223-15. Epub 2015 Apr 6.


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.


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.


Structural basis of clade-specific HIV-1 neutralization by humanized anti-V3 monoclonal antibody KD-247.

Kirby KA, Ong YT, Hachiya A, Laughlin TG, Chiang LA, Pan Y, Moran JL, Marchand B, Singh K, Gallazzi F, Quinn TP, Yoshimura K, Murakami T, Matsushita S, Sarafianos SG.

FASEB J. 2015 Jan;29(1):70-80. doi: 10.1096/fj.14-252262. Epub 2014 Oct 28.


Remembering Professor Walter A. Scott.

Sarafianos SG.

Viruses. 2014 Oct 20;6(10):3873-4. doi: 10.3390/v6103873.


Drug resistance in non-B subtype HIV-1: impact of HIV-1 reverse transcriptase inhibitors.

Singh K, Flores JA, Kirby KA, Neogi U, Sonnerborg A, Hachiya A, Das K, Arnold E, McArthur C, Parniak M, Sarafianos SG.

Viruses. 2014 Sep 24;6(9):3535-62. doi: 10.3390/v6093535. Review.


Antiviral drugs specific for coronaviruses in preclinical development.

Adedeji AO, Sarafianos SG.

Curr Opin Virol. 2014 Oct;8:45-53. doi: 10.1016/j.coviro.2014.06.002. Epub 2014 Jul 2. Review.

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