Results 21 to 30 of about 147,757 (263)

An Update on Development of Small-Molecule Plasmodial Kinase Inhibitors

Molecules, 2020
Malaria control relies heavily on the small number of existing antimalarial drugs. However, recurring antimalarial drug resistance necessitates the continual generation of new antimalarial drugs with novel modes of action.
Chantalle Moolman, Rencia van der Sluis, Richard M. Beteck, Lesetja J. Legoabe   +3 more
doaj   +1 more source

δ-Opioid Receptor as a Molecular Target for Increasing Cardiac Resistance to Reperfusion in Drug Development

Biomedicines, 2023
An analysis of published data and the results of our own studies reveal that the activation of a peripheral δ2-opioid receptor (δ2-OR) increases the cardiac tolerance to reperfusion.
Natalia V. Naryzhnaya, Alexander V. Mukhomedzyanov, Maria Sirotina, Leonid N. Maslov, Boris K. Kurbatov, Alexander S. Gorbunov, Mikhail Kilin, Artur Kan, Andrey V. Krylatov, Yuri K. Podoksenov, Sergey V. Logvinov   +10 more
doaj   +1 more source

Profiling Substrate Promiscuity of Wild-Type Sugar Kinases for Multi-fluorinated Monosaccharides [PDF]

, 2020
Fluorinated sugar-1-phosphates are of emerging importance as intermediates in the chemical and biocatalytic synthesis of modified oligosaccharides, as well as probes for chemical biology. Here we present a systematic study of the activity of a wide range
Parmeggiani F., Malassis J., Wendy, Offen, Peter, Both, Clement, Fontenelle, Jean-Baptiste, Vendeville, Charnock S. J., Sabine, Flitsch, Fontenelle C. Q., Vendeville J. -B., Bruno, Linclau, Offen W., Flitsch S. L., Alex, Heyam, Keenan T., Julien, Malassis, kun, huang, Carl, Young, Marchesi A., Davies G. J., Tessa, Keenan, Huang K., Heyam A., Both P., Fascione M. A., Gideon J., Davies, Martin, Fascione, Young C., Andrea, Marchesi, Simon J., Charnock, Fabio, Parmeggiani, Linclau B.   +31 more
core   +3 more sources

A Chemical Proteomics Approach to Discover Regulators of Innate Immune Signaling

Viruses, 2023
Innate immune pathways are tightly regulated to balance an appropriate response to infectious agents and tolerable levels of inflammation. Dysregulation of innate immune pathways can lead to severe autoinflammatory disorders or susceptibility to ...
Andrew P. Kurland, Boris Bonaventure, Jeffrey R. Johnson   +2 more
doaj   +1 more source

Machine learning identifies molecular regulators and therapeutics for targeting SARS‐CoV2‐induced cytokine release

Molecular Systems Biology, 2021
Although 15–20% of COVID‐19 patients experience hyper‐inflammation induced by massive cytokine production, cellular triggers of this process and strategies to target them remain poorly understood.
Marina Chan, Siddharth Vijay, John McNevin, M Juliana McElrath, Eric C Holland, Taranjit S Gujral   +5 more
doaj   +1 more source

Interactions of Equine Viruses with the Host Kinase Machinery and Implications for One Health and Human Disease

Viruses, 2023
Zoonotic pathogens that are vector-transmitted have and continue to contribute to several emerging infections globally. In recent years, spillover events of such zoonotic pathogens have increased in frequency as a result of direct contact with livestock,
Carol Anderson, Haseebullah Baha, Niloufar Boghdeh, Michael Barrera, Farhang Alem, Aarthi Narayanan   +5 more
doaj   +1 more source

MST kinases in innate immune signaling [PDF]

, 2017
The mammalian STE20-like (MST) protein kinases are composed of MST1, MST2, MST3, MST4 and YSK1. They play crucial roles in cell growth, migration, polarity and apoptosis. Dysfunction of these kinases often leads to diseases.
Zhaocai Zhou, Zhubing Shi
core   +1 more source

Kinases and Cancer [PDF]

Cancers, 2018
Protein kinases are a large family of enzymes catalyzing protein phosphorylation. The human genome contains 518 protein kinase genes, 478 of which belong to the classical protein kinase family and 40 are atypical protein kinases [...]
Jonas Cicenas, Egle Zalyte, Amos Bairoch, Pascale Gaudet   +3 more
openaire   +5 more sources

2-(3-Bromophenyl)-8-fluoroquinazoline-4-carboxylic Acid as a Novel and Selective Aurora A Kinase Inhibitory Lead with Apoptosis Properties: Design, Synthesis, In Vitro and In Silico Biological Evaluation

Life, 2022
New quinazoline derivatives were designed based on the structural modification of the reported inhibitors to enhance their selectivity toward Aurora A. The synthesized compounds were tested over Aurora A, and a cytotoxicity assay was performed over NCI ...
Mohamed H. Elsherbeny, Usama M. Ammar, Magda H. Abdellattif, Mohammed A. S. Abourehab, Ahmed Abdeen, Samah F. Ibrahim, Doaa Abdelrahaman, Wessam Mady, Eun Joo Roh, Ahmed Elkamhawy   +9 more
doaj   +1 more source

Disease-related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors

eLife, 2021
Class I Phosphoinositide 3-kinases (PI3Ks) are master regulators of cellular functions, with the class IB PI3K catalytic subunit (p110γ) playing key roles in immune signalling.
Manoj K Rathinaswamy, Zied Gaieb, Kaelin D Fleming, Chiara Borsari, Noah J Harris, Brandon E Moeller, Matthias P Wymann, Rommie E Amaro, John E Burke   +8 more
doaj   +1 more source