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BET bromodomain inhibitors PFI-1 and JQ1 are identified in an epigenetic compound screen to enhance C9ORF72 gene expression and shown to ameliorate C9ORF72-associated pathological and behavioral abnormalities in a C9ALS/FTD model
(2021)
Abstract
Background
An intronic GGGGCC (G4C2) hexanucleotide repeat expansion (HRE) in the C9ORF72 gene is the most common cause of amyotrophic lateral sclerosis (ALS) and ...
Dietary compound resveratrol is a pan-BET bromodomain inhibitor
(2017-11-01)
The chemopreventive and anticancer effects of resveratrol (RSV) are widely reported in the literature. Specifically, mechanisms involving epigenetic regulation are promising targets to regulate tumor development. Bromodomains ...
Peptides based on CcdB protein as novel inhibitors of bacterial topoisomerases
(Pergamon-Elsevier B.V. Ltd, 2008-12-01)
The ccd toxin-antitoxin system of the F plasmid encodes CcdB, a protein that poisons the essential Escherichia coli DNA gyrase, unique type IIA topoisomerase able to introduce negative supercoils into DNA. Based on CcdB ...
Peptides based on CcdB protein as novel inhibitors of bacterial topoisomerases
(Pergamon-Elsevier B.V. Ltd, 2008-12-01)
The ccd toxin-antitoxin system of the F plasmid encodes CcdB, a protein that poisons the essential Escherichia coli DNA gyrase, unique type IIA topoisomerase able to introduce negative supercoils into DNA. Based on CcdB ...
Peptides based on CcdB protein as novel inhibitors of bacterial topoisomerases
(Pergamon-Elsevier B.V. Ltd, 2014)
ETP-46321, a dual p110?/? class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis
Class IA phosphoinositide 3-kinases (PI3Ks) are essential to function of normal and tumor cells, and to modulate immune responses. T lymphocytes express high levels of p110? and p110? class IA PI3K. Whereas the functioning ...
The characterisation of the protective film formed by benzotriazole on the 90/10 copper-nickel alloy surface in H2SO4 media
(Pergamon-Elsevier B.V. Ltd, 2008-03-01)
The nature of the protective film formed by benzotriazole (BTAH) on the surface of the 90/10 CuNi alloy in deaerated 0.5 mol L-1 H2SO4 solution containing Fe(III) ions as oxidant was investigated by weight-loss, calorimetric ...
The characterisation of the protective film formed by benzotriazole on the 90/10 copper-nickel alloy surface in H2SO4 media
(Pergamon-Elsevier B.V. Ltd, 2008-03-01)
The nature of the protective film formed by benzotriazole (BTAH) on the surface of the 90/10 CuNi alloy in deaerated 0.5 mol L-1 H2SO4 solution containing Fe(III) ions as oxidant was investigated by weight-loss, calorimetric ...
Síntese de derivados de chalconas e de 2-quinolinonas visando a busca por inibidores das enzimas cruzaína e da família BET bromodomain
(Universidade Federal de São CarlosBRUFSCarPrograma de Pós-Graduação em Química - PPGQ, 2014-09-12)
The first part of this work involved the synthesis of chalcone derivatives towards the development of inhibitors of the enzyme cruzain from Trypanosoma cruzi. Different green chemistry approaches were employed to functionalize ...
Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain
(American Chemical Society - ACSWashington, DC, 2013-12)
Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower ...