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Drug Evaluations

Dolutegravir: an exciting new kid on the block

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Jose Luis Blanco, Gary Whitlock, Ana Milinkovic & Graeme Moyle. (2015) HIV integrase inhibitors: a new era in the treatment of HIV. Expert Opinion on Pharmacotherapy 16:9, pages 1313-1324.
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Manoj Patel, Christopher Cianci, Christopher W. Allard, Dawn D. Parker, Jean Simmermacher, Susan Jenkins, Brian Mcauliffe, Beatrice Minassian, Linda Discotto, Mark Krystal, Nicholas A. Meanwell & B. Narasimhulu Naidu. (2020) Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors. Bioorganic & Medicinal Chemistry Letters 30:21, pages 127516.
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Manoj Patel, B. Narasimhulu Naidu, Ira Dicker, Helen Higley, Zeyu Lin, Brian Terry, Tricia Protack, Mark Krystal, Susan Jenkins, Dawn Parker, Chiradeep Panja, Richard Rampulla, Arvind Mathur, Nicholas A. Meanwell & Michael A. Walker. (2020) Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors. Bioorganic & Medicinal Chemistry 28:13, pages 115541.
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José L. Blanco, Anne-Geneviéve Marcelin, Christine Katlama & Esteban Martinez. (2018) Dolutegravir resistance mutations. Current Opinion in Infectious Diseases 31:3, pages 237-245.
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Kaitlin Anstett, Bluma Brenner, Thibault Mesplede & Mark A. Wainberg. (2017) HIV drug resistance against strand transfer integrase inhibitors. Retrovirology 14:1.
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Sergio R. Ribone & Mario A. Quevedo. (2017) Structural basis for the potent inhibition of the HIV integrase-LEDGF/p75 protein–protein interaction. Journal of Molecular Graphics and Modelling 75, pages 189-198.
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Erica Lazarus, Simone Nicol, Lisa Frigati, Martina Penazzato, Mark F. Cotton, Elizabeth Centeno-Tablante, Avy Violari & Liesl Nicol. (2017) Second- and Third-line Antiretroviral Therapy for Children and Adolescents. Pediatric Infectious Disease Journal 36:5, pages 492-499.
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Pamela Tau & Stefano Rusconi. (2016) Integrase inhibitors against HIV: efficacy and resistance. Future Virology 11:2, pages 109-112.
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Jannik Fonager, Jonas T. Larsson, Christian Hussing, Frederik Neess Engsig, Claus Nielsen & Thea Kølsen Fischer. (2015) Identification of minority resistance mutations in the HIV-1 integrase coding region using next generation sequencing. Journal of Clinical Virology 73, pages 95-100.
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Mario A. Quevedo, Sergio R. Ribone, Margarita C. Briñón & Wim Dehaen. (2014) Development of a receptor model for efficient in silico screening of HIV-1 integrase inhibitors. Journal of Molecular Graphics and Modelling 52, pages 82-90.
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