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Anti-infectives Clinical progress of HIV-1 integrase inhibitors

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Pages 213-225 | Published online: 08 Jun 2008

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Sangeetha Balasubramanian, Muthukumaran Rajagopalan, Ravi Shankar Bojja, Anna Marie Skalka, Mark D. Andrake & Amutha Ramaswamy. (2017) The conformational feasibility for the formation of reaching dimer in ASV and HIV integrase: a molecular dynamics study. Journal of Biomolecular Structure and Dynamics 35:16, pages 3469-3485.
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Janice Soo Fern Lee, Alexandra Calmy, Isabelle Andrieux-Meyer & Nathan Ford. (2012) Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings. HIV/AIDS - Research and Palliative Care 4, pages 5-15.
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Philippe Cotelle. (2011) 3-Hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones as new HIV-1 integrase inhibitors WO2011046873 A1. Expert Opinion on Therapeutic Patents 21:11, pages 1799-1804.
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Articles from other publishers (42)

Urvashi, J. B. Senthil Kumar, Parthasarathi Das & Vibha Tandon. (2022) Development of Azaindole-Based Frameworks as Potential Antiviral Agents and Their Future Perspectives. Journal of Medicinal Chemistry 65:9, pages 6454-6495.
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Jay Trivedi, Dinesh Mahajan, Russell J. Jaffe, Arpan Acharya, Debashis Mitra & Siddappa N. Byrareddy. (2020) Recent Advances in the Development of Integrase Inhibitors for HIV Treatment. Current HIV/AIDS Reports 17:1, pages 63-75.
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Mark Andrew Phillips, Marisa A. Stewart, Darby L. Woodling & Zhong-Ru Xie. 2018. Molecular Docking. Molecular Docking.
Cosme Sandoval, Ngiap-Kie Lim & Haiming Zhang. (2018) Two-Step Synthesis of 3,4-Dihydropyrrolopyrazinones from Ketones and Piperazin-2-ones. Organic Letters 20:4, pages 1252-1255.
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Hong-Min Wu, Kuo Zhou, Tao Wu & Yin-Guang Cao. (2016) Synthesis of Pyrazine-1,3-thiazine Hybrid Analogues as Antiviral Agent Against HIV-1, Influenza A (H1N1), Enterovirus 71 (EV71), and Coxsackievirus B3 (CVB3). Chemical Biology & Drug Design 88:3, pages 411-421.
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Vibha Tandon, Urvashi, Pooja Yadav, Souvik Sur, Sheenu Abbat, Vinod Tiwari, Raymond Hewer, Maria A. Papathanasopoulos, Rameez Raja, Akhil C. Banerjea, Akhilesh K. Verma, Shrikant Kukreti & Prasad V. Bharatam. (2015) Design, Synthesis, and Biological Evaluation of 1,2-Dihydroisoquinolines as HIV-1 Integrase Inhibitors. ACS Medicinal Chemistry Letters 6:10, pages 1065-1070.
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Francesca Esposito & Enzo Tramontano. (2014) Past and Future. Current Drugs Targeting HIV-1 Integrase and Reverse Transcriptase-Associated Ribonuclease H Activity: Single and Dual Active Site Inhibitors. Antiviral Chemistry and Chemotherapy 23:4, pages 129-144.
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Roberto Di Santo. (2013) Inhibiting the HIV Integration Process: Past, Present, and the Future. Journal of Medicinal Chemistry 57:3, pages 539-566.
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Peter K. Quashie, Thibault Mesplède & Mark A. Wainberg. (2012) HIV Drug Resistance and the Advent of Integrase Inhibitors. Current Infectious Disease Reports 15:1, pages 85-100.
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Mauro Carcelli, Alessia Bacchi, Paolo Pelagatti, Gabriele Rispoli, Dominga Rogolino, Tino W. Sanchez, Mario Sechi & Nouri Neamati. (2013) Ruthenium arene complexes as HIV-1 integrase strand transfer inhibitors. Journal of Inorganic Biochemistry 118, pages 74-82.
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Peter K Quashie, Richard D Sloan & Mark A Wainberg. (2012) Novel therapeutic strategies targeting HIV integrase. BMC Medicine 10:1.
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Dominga Rogolino, Mauro Carcelli, Mario Sechi & Nouri Neamati. (2012) Viral enzymes containing magnesium: Metal binding as a successful strategy in drug design. Coordination Chemistry Reviews 256:23-24, pages 3063-3086.
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Isabelle Malet, Vincent Calvez & Anne-Geneviève Marcelin. (2012) The future of integrase inhibitors of HIV-1. Current Opinion in Virology 2:5, pages 580-587.
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Vo Cam Quy, Sergio Pantano, Giulia Rossetti, Mauro Giacca & Paolo Carloni. (2012) HIV-1 Tat Binding to PCAF Bromodomain: Structural Determinants from Computational Methods. Biology 1:2, pages 277-296.
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Manuel Tsiang, Gregg S. Jones, Anita Niedziela-Majka, Elaine Kan, Eric B. Lansdon, Wayne Huang, Magdeleine Hung, Dharmaraj Samuel, Nikolai Novikov, Yili Xu, Michael Mitchell, Hongyan Guo, Kerim Babaoglu, Xiaohong Liu, Romas Geleziunas & Roman Sakowicz. (2012) New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action. Journal of Biological Chemistry 287:25, pages 21189-21203.
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Mark A. Wainberg. (2012) The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance. Scientifica 2012, pages 1-28.
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Alessia Bacchi, Mauro Carcelli, Carlotta Compari, Emilia Fisicaro, Nicolino Pala, Gabriele Rispoli, Dominga Rogolino, Tino W. Sanchez, Mario Sechi, Valentina Sinisi & Nouri Neamati. (2011) Investigating the Role of Metal Chelation in HIV-1 Integrase Strand Transfer Inhibitors. Journal of Medicinal Chemistry 54:24, pages 8407-8420.
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Sheo B. Singh. 2011. HIV‐1 Integrase. HIV‐1 Integrase 309 323 .
Nouri Neamati. 2011. HIV‐1 Integrase. HIV‐1 Integrase 165 196 .
Kevin D. Mohammed, Michael B. Topper & Mark A. Muesing. (2011) Sequential Deletion of the Integrase (Gag-Pol) Carboxyl Terminus Reveals Distinct Phenotypic Classes of Defective HIV-1. Journal of Virology 85:10, pages 4654-4666.
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Ted W. Johnson, Steven P. Tanis, Scott L. Butler, Deepak Dalvie, Dorothy M. DeLisle, Klaus R. Dress, Erik J. Flahive, Qiyue Hu, Jon E. Kuehler, Atsuo Kuki, Wen Liu, Guy A. McClellan, Qinghai Peng, Michael B. Plewe, Paul F. Richardson, Graham L. Smith, Jim Solowiej, Khanh T. Tran, Hai Wang, Xiaoming Yu, Junhu Zhang & Huichun Zhu. (2011) Design and Synthesis of Novel N -Hydroxy-Dihydronaphthyridinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors . Journal of Medicinal Chemistry 54:9, pages 3393-3417.
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Arnout R. D. Voet, Marc De Maeyer, Frauke Christ & Zeger Debyser. 2011. Antiviral Drug Strategies. Antiviral Drug Strategies 51 71 .
Alessia Bacchi, Mauro Carcelli, Carlotta Compari, Emilia Fisicaro, Nicolino Pala, Gabriele Rispoli, Dominga Rogolino, Tino W. Sanchez, Mario Sechi & Nouri Neamati. (2011) HIV-1 IN Strand Transfer Chelating Inhibitors: A Focus on Metal Binding. Molecular Pharmaceutics 8:2, pages 507-519.
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Horrick Sharma, Shivaputra Patil, Tino W. Sanchez, Nouri Neamati, Raymond F. Schinazi & John K. Buolamwini. (2011) Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors. Bioorganic & Medicinal Chemistry 19:6, pages 2030-2045.
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Laith Q. Al‐Mawsawi & Nouri Neamati. (2011) Allosteric Inhibitor Development Targeting HIV‐1 Integrase. ChemMedChem 6:2, pages 228-241.
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Muriel Billamboz, Fabrice Bailly, Cédric Lion, Christina Calmels, Marie-Line Andréola, Myriam Witvrouw, Frauke Christ, Zeger Debyser, Laura De Luca, Alba Chimirri & Philippe Cotelle. (2011) 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: Influence of the alkylation of position 4. European Journal of Medicinal Chemistry 46:2, pages 535-546.
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L. Van Wesenbeeck, E. Rondelez, M. Feyaerts, A. Verheyen, K. Van der Borght, V. Smits, C. Cleybergh, H. De Wolf, K. Van Baelen & L. J. Stuyver. (2011) Cross-Resistance Profile Determination of Two Second-Generation HIV-1 Integrase Inhibitors Using a Panel of Recombinant Viruses Derived from Raltegravir-Treated Clinical Isolates. Antimicrobial Agents and Chemotherapy 55:1, pages 321-325.
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Steven P. Tanis, Michael B. Plewe, Ted W. Johnson, Scott L. Butler, Deepak Dalvie, Dorothy DeLisle, Klaus R. Dress, Qiyue Hu, Buwen Huang, Jon E. Kuehler, Atsuo Kuki, Wen Liu, Qinghai Peng, Graham L. Smith, Jim Solowiej, Khanh T. Tran, Hai Wang, Anle Yang, Chunfeng Yin, Xiaoming Yu, Junhu Zhang & Huichun Zhu. (2010) Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK. Bioorganic & Medicinal Chemistry Letters 20:24, pages 7429-7434.
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Kavya Ramkumar, Erik Serrao, Srinivas Odde & Nouri Neamati. (2010) HIV-1 integrase inhibitors: 2007-2008 update. Medicinal Research Reviews 30:6, pages 890-954.
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Stefania Ferro, Laura De Luca, Maria Letizia Barreca, Sara De Grazia, Frauke Christ, Zeger Debyser & Alba Chimirri. (2010) New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action. Bioorganic & Medicinal Chemistry 18:15, pages 5510-5518.
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Chenzhong Liao & Marc C. Nicklaus. (2010) Tautomerism and Magnesium Chelation of HIV-1 Integrase Inhibitors: A Theoretical Study. ChemMedChem 5:7, pages 1053-1066.
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Chenzhong Liao, Christophe Marchand, Terrence R Burke Jr, Yves Pommier & Marc C Nicklaus. (2010) Authentic HIV-1 integrase inhibitors. Future Medicinal Chemistry 2:7, pages 1107-1122.
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Chenzhong Liao & Marc C Nicklaus. (2010) Computer tools in the discovery of HIV-1 integrase inhibitors. Future Medicinal Chemistry 2:7, pages 1123-1140.
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Qi Yin, DaoMing Zhuang, YaQin Jiang, ChuanKe Zhao, Xin Zeng & ShiYou Li. (2010) Establishment of a high-throughput screening system for universal anti-HIV targets. Chinese Science Bulletin 55:10, pages 937-942.
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Erik Serrao, Srinivas Odde, Kavya Ramkumar & Nouri Neamati. (2009) Raltegravir, elvitegravir, and metoogravir: the birth of "me-too" HIV-1 integrase inhibitors. Retrovirology 6:1.
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Michael B. Plewe, Scott L. ButlerKlaus R. Dress, Qiyue Hu, Ted W. Johnson, Jon E. Kuehler, Atsuo Kuki, Hieu Lam, Wen Liu, Dawn Nowlin, Qinghai Peng, Sadayappan V. Rahavendran, Steven P. Tanis, Khanh T. Tran, Hai Wang, Anle Yang & Junhu Zhang. (2009) Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors. Journal of Medicinal Chemistry 52:22, pages 7211-7219.
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Arnout RD Voet, Marc De Maeyer, Zeger DebyserFrauke Christ. (2009) In search of second-generation HIV integrase inhibitors: targeting integration beyond strand transfer. Future Medicinal Chemistry 1:7, pages 1259-1274.
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Mario Sechi, Mauro Carcelli, Dominga Rogolino & Nouri Neamati. 2009. Drug Design of Zinc‐Enzyme Inhibitors. Drug Design of Zinc‐Enzyme Inhibitors 911 936 .
Mariusz Jaskolski, Jerry N. Alexandratos, Grzegorz Bujacz & Alexander Wlodawer. (2009) Piecing together the structure of retroviral integrase, an important target in AIDS therapy. FEBS Journal 276:11, pages 2926-2946.
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Ahmad R Sedaghat, Robert F Siliciano & Claus O Wilke. (2009) Constraints on the dominant mechanism for HIV viral dynamics in patients on raltegravir. Antiviral Therapy 14:2, pages 263-271.
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John M Murray. (2009) HIV Dynamics and Integrase Inhibitors. Antiviral Chemistry and Chemotherapy 19:4, pages 157-164.
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Li-Fan Zeng, Xiao-Hua Jiang, Tino Sanchez, Hu-Shan Zhang, Raveendra Dayam, Nouri Neamati & Ya-Qiu Long. (2008) Novel dimeric aryldiketo containing inhibitors of HIV-1 integrase: Effects of the phenyl substituent and the linker orientation. Bioorganic & Medicinal Chemistry 16:16, pages 7777-7787.
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