Results 1 to 10 of about 125 (122)

Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs [PDF]

open access: goldMolecules, 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
doaj   +2 more sources

Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs

open access: greenJournal of Medicinal Chemistry, 2021
A series of novel heteroaromatic-difluoro-biphenyl-diarylpyrimidines were designed as non-nucleoside anti-HIV inhibitors targeting reverse transcriptase by a fragment-based replacement strategy with the purpose of improving the druggability. Hopping five- or six-membered heterocycle groups on the biphenyl moiety as bioisosterism for intrinsically ...
Li Ding   +4 more
openalex   +4 more sources

Hydrogen Bonding (Base Pairing) in Antiviral Activity

open access: yesViruses, 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
doaj   +1 more source

Identification of Novel Diarylpyrimidines as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors by Exploring the Primer Grip Region

open access: yesPharmaceuticals, 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
doaj   +1 more source

Distributed Optimal Secondary Frequency Control in Power Networks with Delay Independent Stability [PDF]

open access: yesIEEE Transactions on Automatic Control,2023, 2022
Distributed secondary frequency control for power systems, is a problem that has been extensively studied in the literature, and one of its key features is that an additional communication network is required to achieve optimal power allocation.
arxiv   +1 more source

Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV

open access: yesPharmaceuticals, 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
doaj   +1 more source

Cell segmentation of in situ transcriptomics data using signed graph partitioning [PDF]

open access: yesGbRPR 2023. Lecture Notes in Computer Science, vol 14121. Springer, Cham, 2023
The locations of different mRNA molecules can be revealed by multiplexed in situ RNA detection. By assigning detected mRNA molecules to individual cells, it is possible to identify many different cell types in parallel. This in turn enables investigation of the spatial cellular architecture in tissue, which is crucial for furthering our understanding ...
arxiv   +1 more source

Molecular Models of DAPI [PDF]

open access: yesJournal of Chemical Education, 2007
This month’s Featured Molecule is DAPI (4',6-diamidino-2-phenylindole), a minor-groove binder to DNA.
openaire   +1 more source

Shared lateral control with on-line adaptation of the automation degree for driver steering assist system: A weighting design approach [PDF]

open access: yes2015 54th IEEE Conference on Decision and Control (CDC), Dec 2015, Osaka, France. pp.857-862, 2020
This paper addresses the shared lateral control for both lane-keeping and obstacle avoidance tasks of a driver steering assist system (DSAS). In this work, we propose a novel approach to deal with the interactions between the human (driver) and the machine (DSAS) by introducing into the vehicle system a fictive nonlinear term representing the driver ...
arxiv   +1 more source

Labeling Nuclear DNA Using DAPI [PDF]

open access: yesCold 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.
openaire   +2 more sources

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