Lead identification and optimization of novel collagenase inhibitors; pharmacophore and structure based studies [PDF]
In this study, chemical feature based pharmacophore models of MMP-1, MMP-8 and MMP-13 inhibitors have been developed with the aid of HypoGen module within Catalyst program package. In MMP-1 and MMP-13, all the compounds in the training set mapped HBA and
Jagarlapudi, Sarma ARP +4 more
core +2 more sources
Simple inhibitors of histone deacetylase activity that combine features of short-chain fatty acid and hydroxamic acid inhibitors [PDF]
, 2008 Butyric acid and trichostatin A (TSA) are anti-cancer compounds that cause the upregulation of genes involved in differentiation and cell cycle regulation by inhibiting histone deacetylase (HDAC) activity.
Abuaita, Basel +10 more
core +1 more source
Validation of a method for the determination of Aderamastat (FP-025) in K 2EDTA human plasma by LC-MS/MS [PDF]
Aderamastat (FP-025) is a small molecule, selective matrix metalloproteinase (MMP)-12 inhibitor, under development for respiratory conditions which may include chronic inflammatory airway diseases and pulmonary fibrosis.
Abd-Elaziz, Khalid S +9 more
core +1 more source
Iraqi Journal of Pharmaceutical SciencesHistone deacetylases (HDACs) are a class of proteins that responsible of the hydrolysis of N-acetyl lysine residues in histones as well as non-histone protein substrates. This phenomenon may provide an explanation for the involvement of these enzymes in
Rusul Mohammed Hasan Ali +1 more
doaj +1 more source
TP0586532, a non-hydroxamate LpxC inhibitor, reduces LPS release and IL-6 production both in vitro and in vivo. [PDF]
J Antibiot (Tokyo), 2022 Fujita K +4 more
europepmc +1 more source
Overview of MMP Biology and Gene Associations in Human Diseases [PDF]
, 2017 Interactions of cell with the extracellular matrix (ECM) are crucial for normal development and functioning of the human organism. By regulating ECM integrity and composition matrix metalloproteinases (MMPs) play the main role in ECM molecules signaling ...
Djuric, Tamara, Zivkovic, Maja
core +1 more source
Probing the Determinants of the Molecular Recognition in Metal-Dependent Deacetylase. [PDF]
, 2014 Metal-dependent deacetylases catalyze a variety of essential reactions in nature However,most metallohydrolases can be activated by a number of divalent metal ions, such as Zn(II) or Fe(II).
Kim, Byung Chul
core
Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase [PDF]
, 2017 We herein disclose a series of compounds with potent inhibitory activities towards histone deacetylases (HDAC) and cyclooxygenases (COX). These compounds potently inhibited the growth of cancer cell lines consistent with their anti-COX and anti-HDAC ...
Fathi, Shaghayegh +9 more
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Activity of 2-Aryl-2-(3-indolyl)acetohydroxamates Against Drug-Resistant Cancer Cells [PDF]
, 2017 Many types of tumor, including glioma, melanoma, non-small cell lung, esophageal, head and neck cancer, among others, are intrinsically resistant to apoptosis induction and poorly responsive to current therapies with proapoptotic agents.
Aksenov, Alexander V. +20 more
core +2 more sources
The Class I Histone Deacetylase Inhibitor as a Potent Therapeutic Target for Treating Glioblastoma and Mocetinostat as a Novel Inhibitor in the Induction Death of Cancer Cells [PDF]
Epigenetic abnormality is one of the hallmarks of glioblastoma cancer cells. Histone deacetylase (HDAC) modification has a crucial role in epigenetic abnormality, which results in the initiation and progression of glioblastoma cancer cells. The selective
Hameed Khathayer, Firas
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