Hydrogen Bonding (Base Pairing) in Antiviral Activity [PDF]
Viruses, 2023 Base pairing based on hydrogen bonding has, since its inception, been crucial in the antiviral activity of arabinosyladenine, 2′-deoxyuridines (i.e., IDU, TFT, BVDU), acyclic nucleoside analogues (i.e., acyclovir) and nucleoside reverse transcriptase ...
Erik De Clercq
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Development of fluorine-substituted NH2-biphenyl-diarylpyrimidines as highly potent non-nucleoside reverse transcriptase inhibitors: Boosting the safety and metabolic stability [PDF]
Acta Pharmaceutica Sinica B, 2023 Our recent studies for nonnucleoside reverse transcriptase inhibitors identified a highly potent compound JK-4b against WT HIV-1 (EC50 = 1.0 nmol/L), but the poor metabolic stability in human liver microsomes (t1/2 = 14.6 min) and insufficient ...
Xin Jin +9 more
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Picomolar inhibitor of reverse transcriptase featuring significantly improved metabolic stability [PDF]
Acta Pharmaceutica Sinica B, 2023 Considering the undesirable metabolic stability of our recently identified NNRTI 5 (t1/2 = 96 min) in human liver microsomes, we directed our efforts to improve its metabolic stability by introducing a new favorable hydroxymethyl side chain to the C-5 ...
Ya-Li Sang +4 more
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Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs [PDF]
Molecules, 2020 Scaffold hopping is a frequently-used strategy in the development of non-nucleoside reverse transcriptase inhibitors. Herein, CH(CN)-DAPYs were designed by hopping the cyano-methylene linker of our previous published CH(CN)-DABOs onto the etravirine (ETR)
Ting-Ting Li +4 more
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Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years [PDF]
Acta Pharmaceutica Sinica B, 2020 Human immunodeficiency virus (HIV) is the primary infectious agent of acquired immunodeficiency syndrome (AIDS), and non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the cornerstone of HIV treatment.
Chunlin Zhuang +3 more
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Identification of Novel Diarylpyrimidines as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors by Exploring the Primer Grip Region [PDF]
Pharmaceuticals, 2022 HIV-1 reverse transcriptase (RT) plays a crucial role in the viral replication cycle, and RT inhibitors can represent a promising pathway in treating AIDS.
Tao Zhang +8 more
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Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV [PDF]
Pharmaceuticals, 2020 In the treatment of acquired immune deficiency syndrome (AIDS), the diarylpyrimidine (DAPY) analogs etravirine (ETR) and rilpivirine (RPV) have been widely effective against human immunodeficiency virus (HIV) variants that are resistant to other non ...
Daniel M. Himmel, Eddy Arnold
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Labeling Nuclear DNA Using DAPI [PDF]
Cold Spring Harbor Protocols, 2011 INTRODUCTIONA number of fluorescent stains are available that label DNA and allow easy visualization of the nucleus in interphase cells and chromosomes in mitotic cells, including Hoechst, 4′,6-diamidino-2-phenylindole (DAPI), ethidium bromide, propidium iodide, and acridine orange.
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DAPI Fluorescence in Nuclei Isolated from Tumors [PDF]
Journal of Histochemistry & Cytochemistry, 2005 In DNA histograms of some human solid tumors stained with nuclear isolation medium-4,6-diamidino-2-phenylindole dihydrochloride (NIM-DAPI), the coefficient of variation (CV) of the G0/G1 peak was broad, and in nuclear volume vs DNA scattergrams, a prominent slope was seen.
Awtar, Krishan, Payal D, Dandekar
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Molecular Models of DAPI [PDF]
Journal of Chemical Education, 2007 This month’s Featured Molecule is DAPI (4',6-diamidino-2-phenylindole), a minor-groove binder to DNA.
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