Structure-activity relationships of HDAC8 inhibitors: Non-hydroxamates as anticancer agents
Pharmacological Research, 2018 Histone deacetylase inhibitors (HDACIs) have a paramount importance in the acetylation process of histone and non-histone proteins that are crucial players in the cellular epigenetic modifications. HDACIs exert effective antiproliferation through DNA repairing, cell cycle arrest, apoptosis induction and alteration of genetic expression. HDAC8 is one of
Sk. Abdul Amin +2 more
openaire +2 more sources
Acta Crystallographica Section E: Crystallographic Communications, 2016 The centrosymmetric binuclear complex, [Cu2(C2H2N2O4)(C10H8N2)2(C2H6OS)2](ClO4)2, contains two copper(II) ions, connected through an N-deprotonated oxalodihydroxamic acid dianion, two terminal 2,2′-bipyridine ligands, and two apically coordinating ...
Irina A. Odarich +3 more
doaj +1 more source
Microwave-assisted synthesis and antitumor evaluation of a new series of thiazolylcoumarin derivatives [PDF]
A new series of thiazolylcoumarin derivatives was synthesized. The designed strategy embraced a molecular hybridization approach which involves the combination of the thiazole and coumarin pharmacophores together. The new hybrid compounds were tested for
El-Bendary, Eman R. +4 more
core +1 more source
Regulation of Activity and Selectivity of Histone Deacetylases [PDF]
, 2021 Acetylation is an important post-translational modification (PTM). Lysine acetylation is a reversible PTM, where deacetylation is catalyzed by histone deacetylases (HDACs).
Diffley, Kelsey
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Current Status and Perspectives of Protease Inhibitors and Their Combination with Nanosized Drug Delivery Systems for Targeted Cancer Therapy [PDF]
, 2021 : In cancer treatments, many natural and synthetic products have been examined; among them, protease inhibitors are promising candidates for anti-cancer agents. Since dysregulated proteolytic activities can contribute to tumor development and metastasis,
Antoine, R +5 more
core +3 more sources
In Silico and Experimental ADAM17 Kinetic Modeling as Basis for Future Screening System for Modulators [PDF]
, 2022 Understanding the mechanisms of modulators’ action on enzymes is crucial for optimizing and designing pharmaceutical substances. The acute inflammatory response, in particular, is regu lated mainly by a disintegrin and metalloproteinase (ADAM) 17 ...
Bienstein, Marian +4 more
core +1 more source
Design, (radio)synthesis and applications of radiolabelled matrix metalloproteinase inhibitors for PET [PDF]
, 2015 Ontregeling van de activiteit van ‘matrix metalloproteinases’ (MMPs) en ‘a disintegrin and metalloproteinases’ (ADAMs) treedt op bij een groot aantal ziekten, waaronder ontstekingen en kanker.
Matusiak, Nathalie
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Angewandte Chemie International Edition, EarlyView.Synopsis. The [68Ga]GaIII‐TREN‐CAM radiochelate selectively accumulates in Gram‐negative sites of infection and noninvasively monitors treatment response a siderophore antibiotic. ABSTRACT Positron emission tomography (PET) is an emerging tool under clinical investigation for the detection of bacterial infections.
M. Andrey Joaqui‐Joaqui +6 more
wiley +1 more source
Effectiveness of the histone deacetylase inhibitor (S)-2 against LNCaP and PC3 human prostate cancer cells. [PDF]
PLoS ONE, 2013 Histone deacetylase inhibitors (HDACi) represent a promising class of epigenetic agents with anticancer properties. Here, we report that (S)-2, a novel hydroxamate-based HDACi, shown previously to be effective against acute myeloid leukemia cells, was ...
Anna Laurenzana +4 more
doaj +1 more source
Boron Neutron Capture Therapy at a Crossroads: Translational Gap and Emerging Delivery Agents
Chemistry – A European Journal, EarlyView.This review surveys recent advances in boron delivery agents for BNCT, emphasizing the shift from classical small molecules to multifunctional nanocarriers and theranostic systems. By integrating targeting, imaging, and therapy, next‐generation boron compounds aim to bridge the gap between (bio)chemical innovation and clinical translation.
Christoph Selg, Evamarie Hey‐Hawkins
wiley +1 more source