HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors.

Koneru PC, Francis AC, Deng N, Rebensburg SV, Hoyte AC, Lindenberger J, Adu-Ampratwum D, Larue RC, Wempe MF, Engelman AN, Lyumkis D, Fuchs JR, Levy RM, Melikyan GB, Kvaratskhelia M. HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors. Elife 2019 May 23;8. pii: e46344. doi: 10.7554/eLife.46344. PubMed PMID: 31120420; PubMed Central PMCID: PMC6581505.

Dominant negative MA-CA fusion protein is incorporated into HIV-1 cores and inhibits nuclear entry of viral preintegration complexes.

Anderson-Daniels J, Singh PK, Sowd GA, Li W, Engelman AN, Aiken C. Dominant negative MA-CA fusion protein is incorporated into HIV-1 cores and inhibits nuclear entry of viral preintegration complexes. J Virol 2019 Oct 15;93(21). pii: e01118-19. doi: 10.1128/JVI.01118-19. Print 2019 Nov 1. Epub 2019 Aug 14. PubMed PMID: 31413124; PubMed Central PMCID: _.

Disrupting MLV integrase:BET protein interaction biases integration into quiescent chromatin and delays but does not eliminate tumor activation in a MYC/Runx2 mouse model.

Loyola L, Achuthan V, Gilroy K, Borland G, Kilbey A, Mackay N, Bell M, Hay J, Aiyer S, Fingerman D, Villanueva RA, Cameron E, Kozak CA, Engelman AN, Neil J, Roth MJ. Disrupting MLV integrase:BET protein interaction biases integration into quiescent chromatin and delays but does not eliminate tumor activation in a MYC/Runx2 mouse model. PLoS Pathog 2019 Dec 9;15(12):e1008154. doi: 10.1371/journal.ppat.1008154. eCollection 2019 Dec. PubMed PMID: 31815961. PubMed Central PMCID: 6974304.

Differential role for phosphorylation in alternative polyadenylation function versus nuclear import of SR-like protein CPSF6.

Jang S, Cook NJ, Pye VE, Bedwell GJ, Dudek AM, Singh PK, Cherepanov P, Engelman AN. Differential role for phosphorylation in alternative polyadenylation function versus nuclear import of SR-like protein CPSF6. Nucleic Acids Res 2019 May 21;47(9):4663-4683. doi: 10.1093/nar/gkz206. Epub 2019 Mar 27. PubMed PMID: 30916345; PubMed Central PMCID: PMC6511849.

A HTRF based competitive binding assay for screening specific inhibitors of HIV-1 capsid assembly targeting the C-terminal domain of capsid.

Zhang DW, Luo RH, Xu L, Yang L-M, Xu X-S, Bedwell GJ, Engelman AN, Zheng Y-T, Chang S. A HTRF based competitive binding assay for screening specific inhibitors of HIV-1 capsid assembly targeting the C-terminal domain of capsid. Antiviral Res 2019 Sep;169:104544. doi: 10.1016/j.antiviral.2019.104544. Epub 2019 Jun 27. PubMed PMID: 31254557.

Cellular and molecular mechanisms of HIV-1 integration targeting.

Engelman AN, Singh PK. Cellular and molecular mechanisms of HIV-1 integration targeting. Cell Mol Life Sci 2018 July;75(14):2491-507. doi: 10.1007/s00018-018-2772-5. Epub 2018 Feb 7. PubMed PMID: 29417178; PubMed Central PMCID: PMC6004233.

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. Capsid-CPSF6 interaction licenses nuclear HIV-1 trafficking to sites of viral DNA integration. Cell Host Microbe 2018 Sep 12;24(3):392-404.e8. doi: 10.1016/j.chom.2018.08.002. Epub 2018 Aug 30. PubMed PMID: 30173955; PubMed Central PMCID: PMC6368089.

LEDGF/p75 is dispensable for hematopoiesis but essential for MLL-rearranged leukemogenesis.

El Ashkar S, Schwaller J, Pieters T, Goossens S, Demeulemeester J, Christ F, Van Belle S, Juege S, Boeckx N, Engelman A, Debyser Z, De Rijck J. LEDGF/p75 is dispensable for hematopoiesis but essential for MLL-rearranged leukemogenesis. Blood 2018 Jan 4;131(1):95-107. doi: 10.1182/blood-2017-05-786962. Epub 2017 Oct 30. PubMed PMID: 29084744; PubMed Central PMCID: PMC5755044.

Resistance to pyridine-based inhibitor KF116 reveals an unexpected role of integrase in HIV-1 Gag-Pol proteolytic processing.

Hoyte AC, Jamin AV, Koneru PC, Kobe MJ, Larue RC, Fuchs JR, Engelman AN, Kvaratskhelia M. Resistance to pyridine-based inhibitor KF116 reveals an unexpected role of integrase in HIV-1 Gag-Pol proteolytic processing. J Biol Chem 2017 Dec 1;292(48):19814-25. doi:10.1074/jbc.M117.816645. Epub 2017 Sep 28. PubMed PMID: 28972144; PubMed Central PMCID: PMC5712621.

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. Multiplex single-cell visualization of nucleic acids and protein during HIV infection. Nat Commun 2017 Dec 1;8(1):1882. doi: 10.1038/s41467-017-01693-z. PubMed PMID: 29192235; PubMed Central PMCID: PMC5709414.