Results 121 to 130 of about 19,917 (239)

Is Mycobacterial InhA a Suitable Target for Rational Drug Design?

open access: yesChemMedChem, Accepted Article.
InhA, an NAD‐dependent enoyl‐acyl carrier protein reductase, is involved in the biosynthesis of mycolic acids, specific lipids to mycobacteria. InhA is the target of isoniazid, a first‐line anti‐tuberculosis drug used since the 1950s. Isoniazid is a prodrug that needs to be activated by the catalase‐peroxidase KatG.
Julien Rizet   +7 more
wiley   +1 more source

Loss of SMARCB1 evokes targetable epigenetic vulnerabilities in epithelioid sarcoma

open access: yes
Cancer Communications, EarlyView.
Jia Xiang Jin   +12 more
wiley   +1 more source

Novel quinazolinones active against multidrug‐resistant Mycobacterium tuberculosis: synthesis, antimicrobial evaluation and in silico exploration of PonA1 as a potential target

open access: yesChemMedChem, Accepted Article.
Quinazolinone derivatives have emerged as promising scaffolds in antimicrobial drug discovery. This work focuses on the design, synthesis, and evaluation of novel quinazolinone‐based compounds and predicts their potential to interact with mycobacterial penicillin‐binding proteins (PBPs).
MAREK KERDA   +15 more
wiley   +1 more source

Multiple allostery in the regulation of PDGFR beta kinase activities

open access: yesActa Biochimica et Biophysica Sinica
Platelet-derived growth factor receptor beta (PDGFRβ), a type III receptor tyrosine kinase (RTK) with a featured kinase insert, regulates important cellular functions. Dysregulation of PDGFRβ is associated with cardiovascular and fibrosis diseases. Thus,
Zhang Yanfeng   +6 more
doaj   +1 more source

Allosteric transitions of phosphorylase a and the regulation of glycogen metabolism.

open access: hybrid, 1978
Neil B. Madsen   +2 more
openalex   +1 more source

A Phase 1 Randomized Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Escalating Oral Doses of Dordaviprone and the Effects of Food on the Bioavailability of Dordaviprone in Healthy Adult Subjects

open access: yesClinical Pharmacology in Drug Development, EarlyView.
Abstract Dordaviprone (ONC201) is a novel, small molecule imipridone with antitumor effects in glioma patients. This study evaluated the pharmacokinetics and safety of dordaviprone following single escalating doses (Part A), as a capsule content mixed with applesauce or Gatorade (sports drink) [Part B1]), and with or without food [Part B2].
Shamia L. Faison   +7 more
wiley   +1 more source

The RGG motif proteins: Interactions, functions, and regulations

open access: yesWIREs RNA, Volume 14, Issue 1, January/February 2023., 2023
RGG motif proteins play vital roles in the translation process from mRNA transport to translational regulation. Functions of RGG motif proteins depend on their ability to bind to RNAs and proteins, localize to various compartments of the cell and post‐translational modifications.
Mashiat N. Chowdhury, Hong Jin
wiley   +1 more source

Allosteric communication mediated by protein contact clusters: A dynamical model [PDF]

open access: yesarXiv
Allostery refers to the puzzling phenomenon of long-range communication between distant sites in proteins. Despite its importance in biomolecular regulation and signal transduction, the underlying dynamical process is not well understood. This study introduces a dynamical model of allosteric communication based on "contact clusters"-localized groups of
arxiv  

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