Inhibitor of histone acetyltransferases. Medical search. Frequent questions

In the beginning, CPTH2 selectively inhibits the acetylation of histone H3 by recombinant human Gcn5 in a substrate-competitive manner. (cancer-research-network.com)
In vivo, it decreased acetylation of bulk histone H3 at the specific H3-AcK14 site. (cancer-research-network.com)
In general, histone acetylation increases gene expression. (wikipedia.org)
In general, histone acetylation is linked to transcriptional activation and associated with euchromatin. (wikipedia.org)
When it was first discovered, it was thought that acetylation of lysine neutralizes the positive charge normally present, thus reducing affinity between histone and (negatively charged) DNA, which renders DNA more accessible to transcription factors. (wikipedia.org)
Research has emerged, since, to show that lysine acetylation and other posttranslational modifications of histones generate binding sites for specific protein-protein interaction domains, such as the acetyllysine-binding bromodomain[citation needed]. (wikipedia.org)
Type A HATs are located in the nucleus and are involved in the regulation of gene expression through acetylation of nucleosomal histones in the context of chromatin. (wikipedia.org)
shRNA knockdown of p300/CBP led to increased Histac FRET, thus suggesting a role for p300/CBP in the acetylation of the histone H4 tail. (nih.gov)
Inhibits histone acetylation in vivo . (abcam.com)
The structure of the epigenome consists of covalent modifications of chromatin components, including acetylation by histone acetyltransferases (HATs) and deacetylation by histone deacetylases (HDACs). (iu.edu)
Additionally, CREBBP has histone acetylation activity, transferring an acetyl group to histones which impact gene expression. (fredhutch.org)
CREBPP deletion, truncating and missense mutations frequently occur in the histone acetyltransferase (HAT) domains to abrogate CREBBP-mediated histone acetylation. (fredhutch.org)
To dissect the molecular underpinnings of the relationship between CREBBP and CDH1, the authors showed that histone acetylation may be the method by which CREBBP is regulating the expression of CDH1 and other cellular adhesion genes. (fredhutch.org)
Acetylation of histone H4 by p300 was more sensitive to inhibition by garcinol compared with that of H3. (enzolifesciences.com)
Histone H4 acetylation was completely inhibited at 1 µM while acetylation of H3 was not abolished at 20 µM. (enzolifesciences.com)
and they are associated with altered histone acetylation and transcription factor (nerve growth factor-induced clone A [NGFIA]) binding to the glucocorticoid receptor promoter. (deepdyve.com)
The importance of acetylation has recently been elevated by the utilization of histone deacetylase (HDAC) inhibitors in pre-clinical research and the treatment of hypertrophic heart disease 6,7 , as well as the discovery of several critical acetylated forms of myosin amino acids that need to be modified in order for the sarcomere to function correctly 8,9 . (cytoskeleton.com)
While studying HDAC inhibitors in cardiac function, Dr. Mahesh Gupta's laboratory showed that acetylation is important for sarcomere function. (cytoskeleton.com)
Histone acetylation is required in many cellular processes including transcription, DNA repair, and chromatin assembly. (embl.de)
Loss of KAT11 results in the loss of H3K56 acetylation, both on bulk histone and on chromatin (PMID:17046836). (embl.de)
Acetylation of histone H3 lysine 56 (H3-K56) occurs in S phase, and cells lackingH3-K56 acetylation are sensitive to DNA-damaging agents. (embl.de)
GM-CSF expression and release in AM is controlled by NF-kappaB activation, and this is modulated by phosphorylation of MKK-1 and p38 MAP kinase acting on histone acetylation. (nih.gov)
In vertebrates as well as in Drosophila an increase in histone H4 acetylation precedes the H-P switch, while the switch is accompanied by introduction of DNA breaks. (uni-marburg.de)
In the mammalian model systems the H4 acetylation is proposed as the start-signal for the H-P switch and the DNA breaks may be related to the activity of topoisomerases involved in the relaxation of histone deprived DNA. (uni-marburg.de)
Histone acetylation Histone acetylation turned out to be essential to the correct development of postmeiotic cysts. (uni-marburg.de)
However, HDAC-inhibitor induced, premature histone acetylation did not lead to premature signs of the H-P switch. (uni-marburg.de)
Thus, histone H4 acetylation alone is not sufficient to be the start-signal of the H-P switch in Drosophila. (uni-marburg.de)
The HAT responsible for histone H4 acetylation in the H-P switch of Drosophila is not known so far. (uni-marburg.de)
Cell viability/proliferation assays, cell cycle analysis by flow cytometry, immunodetection of specific histone and p53 acetylation marks, western blotting, siRNA and RT-qPCR. (biomedcentral.com)
In addition to its effects on histone modifications, garcinol was found to block CBP/p300-mediated acetylation of the C-terminal activation domain of p53, but resulted in enhanced acetylation of p53K120, and accumulation of p53 in the cytoplasmic compartment. (biomedcentral.com)
In contrast, acetylation of histones H3 and H4 increased. (biomedcentral.com)
HDAC inhibitors increase the acetylation of lysine residues on histone proteins, thereby changing the gene expression pattern for important genes involved in cell cycle, maturation, and cell death. (aml-hub.com)
A clinically significant mechanism of tuberculosis resistance to the aminoglycoside kanamycin (KAN) is its acetylation catalyzed by upregulated Mycobacterium tuberculosis (Mtb) acetyltransferase Eis. (cdc.gov)

Histone deacetylase and acetyltransferase inhibitors decrease organic dust-mediated activation of proinflammatory gene expression. (cdc.gov)
RESULTS: We report here the surprising observation that treatment of a human bronchial epithelial cell line, BEAS-2B cells, with the inhibitor histone deacetylase, trichostatin A, or the histone acetyltransferase inhibitor, anacardic acid, strongly inhibited induction of both IL-6 and IL-8 protein upon stimulation with organic dust. (cdc.gov)
The application, filed in April 2016, is focused on using histone deacetylase (HDAC) inhibitors and/or histone acetyltransferases (HAT) activators to treat heart failure in humans. (unc.edu)
TSA (10 ng/ml), an inhibitor of histone deacetylase (HDAC), reversed the inhibitory effect of PD 098059, SB 203580, SN 50 and AS602868 on GM-CSF release. (nih.gov)
Histone acetyltransferase (HAT) and histone deacetylase (HDAC) activity was manipulated via inhibitor treatment of cultured pupal testes and isolated cysts. (uni-marburg.de)
Histone Deacetylase 4& 6 as prognostic markers and therapeutic targets in Triple negative breast cancer. (sharjah.ac.ae)
A number of natural and synthetic molecules that inhibit histone acetyltransferase (HAT) or histone deacetylase (HDAC) activities have been described. (biomedcentral.com)
We show that NST-1 is an H4-specific histone deacetylase. (biomedcentral.com)
The authors investigate an interaction between two pathways: enhancer of zeste homolog 2 (EZH2) and histone deacetylase (HDAC). (chicagobiomedicalconsortium.org)

Activation of histone acetyltransferase (HAT) or inhibition of histone deacetylases (HDAC) is generally believed to allow chromatin to assume a more open state, permitting transcriptional activity. (cdc.gov)
the authors employed a HDAC inhibitor, Pracinostat on SCLC cell lines and mouse models and found that loss of CREBBP increased therapeutic responses. (fredhutch.org)
Specifically, the invention relates to the method of increasing expression of Brg1, Brm, Cx40, Cx43, and or Scn5a mRNA and/or protein, or decreasing expression of c-Myc mRNA or protein using HDAC inhibitors and/or HAT activators. (unc.edu)
p300/CBP-associated factor [PCAF]) and a HDAC (HDAC4) are localized to the sarcomere matrix and that a HDAC inhibitor increases force generation in treated myofilaments 8 . (cytoskeleton.com)
HDAC inhibitors have shown promise in clinical trials as anticancer therapies, especially when used in combination with other chemotherapies. (biomedcentral.com)
Congratulations to Neil Kelleher, NU, for contributing to a recent publication in Clinical Cancer Research , "Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas. (chicagobiomedicalconsortium.org)
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas. (chicagobiomedicalconsortium.org)
Lymphoma cell lines (n=21) were exposed to GSK126, an EZH2 inhibitor, and romidepsin, a pan-HDAC inhibitor. (chicagobiomedicalconsortium.org)

We are particularly interested in the function of the MYST family of histone acetyltransferases in stem cell populations. (edu.au)
Thus, we are particularly interested in the function of chromatin modifiers, including the MYST family of histone acetyltransferases. (edu.au)
A family of histone acetyltransferases that is structurally-related to CREB-BINDING PROTEIN and to E1A-ASSOCIATED P300 PROTEIN. (bvsalud.org)

Histone acetyltransferases (HATs) are enzymes that acetylate conserved lysine amino acids on histone proteins by transferring an acetyl group from acetyl-CoA to form ε-N-acetyllysine. (wikipedia.org)
Histone acetyltransferases can also acetylate non-histone proteins, such as nuclear receptors and other transcription factors to facilitate gene expression. (wikipedia.org)
Adding chemical groups to the DNA backbone and modifying histone proteins impart distinct characteristics on chromatin architecture. (frontiersin.org)
RATIONALE: Post-translational modification of histone proteins are major mechanisms that modify chromatin structure and regulate gene expression in eukaryotes. (cdc.gov)
With ~1750 lysine-acetylated proteins in the human proteome, Reaction Biology's histone acetyltransferase assays provide an important advantage in terms of assay flexibility as well as gold standard quality. (reactionbiology.com)
Histone acetyltransferases acetylate lysines on histones and other proteins using tritium-labeled acetyl-Coenzyme A as the acetyl donor. (reactionbiology.com)
Post-translational modifications (PTMs) of histones and other proteins are perturbed in tumours. (biomedcentral.com)
Histone modifications act as signals that are 'read' by sensory proteins containing bromodomains, PHD fingers and other domains, many of which function as coregulators of DNA-binding transcription factors [ 4 ]. (biomedcentral.com)
Bromodomains are proteins that contain modules of ~110 amino acids that recognize and bind acetylated lysine residues in histones and other proteins. (frontiersin.org)
Additionally, BRDs contain several catalytic domains that enable them to act as methyltransferases, ATP-dependent re-modellers or histone acetyltransferases and helicases ( 8 ) Bromodomain and extra-terminal domain (BET) proteins are a family of transcriptional mediators that regulate gene expression ( 8 , 9 ). (frontiersin.org)

Here, we summarize the different types of epigenetic enzymes which target corresponding protein domains, emphasize DNA methylation , histone modifications, and microRNA-mediated cooperation with epigenetic modification, and highlight recent achievements in developing targets for epigenetic inhibitor therapy. (frontiersin.org)
This article reviews current anticancer small-molecule inhibitors targeting epigenetic modified enzymes and displays their performances in different stages of clinical trials. (frontiersin.org)
Histone acetyltransferase enzymes (HATs) are important therapeutic targets, but there are few cell-based assays available for evaluating the pharmacodynamics of HAT inhibitors. (nih.gov)
Therefore, identifying key chromatin regulatory factors such as histone modifying enzymes and chromatin remodeling complexes, understanding their activity, specificity and functional roles, and inventing potent and selective drug compounds embody demanding needs in today's biology and pharmaceutical research. (uga.edu)
Targeting these enzymes with inhibitors to restore epigenetic homeostasis has been explored for many cancers. (iu.edu)
Garcinol treatment alters expression of chromatin modifying enzymes in MCF7 cells, resulting in reprogramming of key histone and p53 PTMs and growth arrest, underscoring its potential as a cancer chemopreventive agent. (biomedcentral.com)
Thus, drug-like molecules that target chromatin modifying enzymes to reprogram selected histone PTMs in tumour cells may have potential as cancer chemopreventive agents. (biomedcentral.com)

Potent histone acetyltransferase p300 and PCAF inhibitor (IC 50 values are 7 and 5 μM for p300 and PCAF respectively). (abcam.com)
iP300w is a potent p300/CBP inhibitor. (tocris.com)
It is a potent inhibitor of histone acetyltransferases (HATs) p300 (IC 50 =7µM) and PCAF (IC 50 =5µM) both in vitro and in vivo . (enzolifesciences.com)
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC 50 of 9 μM. (medchemexpress.com)
Galanthamine is a potent acetylcholinesterase ( AChE ) inhibitor with an IC 50 of 500 nM. (medchemexpress.com)
Donepezil is a specific and potent AChE inhibitor. (medchemexpress.com)
Amprenavir is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV. (absource.de)
A structure-activity relationship study of 38 compounds in this structural family yielded highly potent (IC(50) 1M) Eis inhibitors, which did not inhibit other acetyltransferases. (cdc.gov)
We discovered that an antipsychotic drug, haloperidol (HPD, 1), was a potent Eis inhibitor with IC(50) = 0.39 0.08 M. We determined the crystal structure of the Eis-haloperidol (1) complex, which guided synthesis of 34 analogues. (cdc.gov)

We demonstrate the presence of telomeric silencing in Neurospora and show a dependence on histone deacetylases and methylation of histone H3 lysine 9. (biomedcentral.com)
Histone acetyltransferases and histone deacetylases (HDACs) have opposite functions, but both are involved in regulating a variety of oncogenic processes. (aml-hub.com)

TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. (medchemexpress.com)
Garcinol also inhibits histone acetyltransferases ( HATs , IC 50 = 7 μM) and p300/CPB-associated factor ( PCAF , IC 50 = 5 μM). (medchemexpress.com)

The acetyl groups added by type B HATs to the histones are removed by HDACs once they enter the nucleus and are incorporated into chromatin. (wikipedia.org)

Histone acetyltransferase (HATS) is an enzyme that acetylates the conserved lysine amino acids in histones by transferring acetyl from acetyl coenzyme A toε-N-acetyllysine. (cancer-research-network.com)
Specifically, HATS add lysine at the N-terminal of acetyl histones H3 and H4 to specific groups. (cancer-research-network.com)
Type B HATs are located in the cytoplasm and are responsible for acetylating newly synthesized histones prior to their assembly into nucleosomes. (wikipedia.org)
These HATs are generally characterized by the presence of a bromodomain, and they are found to acetylate lysine residues on histones H2B, H3, and H4. (wikipedia.org)
Histone acetyltransferases (HATs) of the MYST family are associated with a variety of human cancers. (biomedcentral.com)
The Histone acetyltransferases (HATs) of the MYST family are highly conserved from yeast to humans and function exclusively in multisubunit protein complexes [ 6 ]. (biomedcentral.com)

In this review, we summarize the basic principles manipulating the abovementioned epigenetic pathways and highlight the evidence of the promising clinical and preclinical results using small-molecule inhibitors against chromatin regulators for cancer treatment. (frontiersin.org)
This effect is accompanied by epigenetic changes involving histone post-translational modifications at the mineralocorticoid receptor (MR) gene and decreased MR expression in the hippocampus. (nature.com)
Epigenetic information can be transmitted by several different molecular mechanisms, which include but are not limited to DNA methylation and histone post-translational modifications (PTMs). (plos.org)
The Thomas lab has a long-term interest in understanding the epigenetic regulation of embryonic development and in particular has characterised the function of histone acetyltransferases. (edu.au)
Histone modification is an epigenetic process involved in the regulation of gene expression. (aml-hub.com)
Among the epigenetic mechanisms, histone modification has received widespread attention and has been researched in depth. (psych.ac.cn)

DNA is wrapped around histones, and, by transferring an acetyl group to the histones, genes can be turned on and off. (wikipedia.org)

In addition, CPTH2 decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B). (cancer-research-network.com)
20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100 µM inhibitor). (sigmaaldrich.com)
Combination of romidepsin with other EZH2 inhibitors also demonstrated synergy suggesting a class effect of EZH2 inhibition with romidepsin. (chicagobiomedicalconsortium.org)
Crystal structures of Eis in complexes with three of the inhibitors showed that the inhibitors were bound in the aminoglycoside binding site of Eis, consistent with the competitive mode of inhibition, as established by kinetics measurements. (cdc.gov)
When tested in Mtb cultures, two inhibitors (47 and 55) completely abolished resistance to KAN of the highly KAN-resistant strain Mtb mc(2) 6230 K204, likely due to Eis inhibition as a major mechanism. (cdc.gov)

The tritium-acetyl group is transferred onto the histone substrate that is measured directly to reflect the enzyme activity. (reactionbiology.com)
Modification of histones by adding one or more chemical groups (such as acetyl group, methyl group, etc.) can lead to changes in chromatin structure and gene transcriptional activity, consequently regulating the level of gene expression. (psych.ac.cn)

In this study we assessed the effects of the phytocompounds garcinol and curcumin on histone and p53 modification in cancer cells, focussing on the breast tumour cell line MCF7. (biomedcentral.com)
Although treatment with curcumin, garcinol or the garcinol derivative LTK-14 hampered MCF7 cell proliferation, differential effects of these compounds on histone modifications were observed. (biomedcentral.com)
In summary, although garcinol and curcumin can both inhibit histone acetyltransferase activities, our results show that these compounds have differential effects on cancer cells in culture. (biomedcentral.com)

A cell-permeable ( bis -benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC 50 = 7.1 µM with PABP1 as substrate). (sigmaaldrich.com)
Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC 50 of 6.7 nM for AChE activity. (medchemexpress.com)
Ketorolac (Ketorolac tromethamine) is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. (absource.de)
Thus, isoform-specific and mutant selective inhibitors have been of significant interest. (bvsalud.org)

dim-5 , which encodes a histone H3 K9 methyltransferase and hpo , which encodes heterochromatin protein-1. (biomedcentral.com)

Chromatin immunoprecipitation assay was performed to evaluate the histone modification of gene loci that are regulated by lunasin and cytokine. (weeksmd.com)
By combining ChIP with quantitative PCR (qPCR) technology, DNA microarray (also known as gene chip) technology or deep sequencing (Seq) technology, researchers can study the relationship between various types of histone modification and gene expression. (psych.ac.cn)

Rtt109, also known as KAT11, is a recently characterized fungal-specific histone acetyltransferase (HAT) that modifies histone H3 lysine 56 (H3K56) to promotegenome stability. (embl.de)

This gold standard approach can be used regardless of whether the substrate is a peptide, histone, nucleosome, or non-histone protein. (reactionbiology.com)
New inhibitors of protein tyrosine phosphatase (SHP2) as potential anti-cancer compounds. (sharjah.ac.ae)
Overexpression of the enhanced intracellular survival (Eis) protein by Mtb confers resistance to the second-line antibiotic kanamycin (KAN). Eis is an acetyltransferase that acetylates KAN, inactivating its antimicrobial function. (cdc.gov)
The enhanced intracellular survival (Eis) protein of Mycobacterium tuberculosis (Mtb) is a versatile acetyltransferase that multiacetylates aminoglycoside antibiotics abolishing their binding to the bacterial ribosome. (cdc.gov)

Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6 µM inhibitor). (sigmaaldrich.com)
These and other PTMs generate a combinatorial histone code that demarcates chromatin regions for transcription activation or repression [ 2 ]. (biomedcentral.com)

PD 098059, but not SB 203580, inhibited LPS-induced histone acetyltransferase (HAT) activity, indicating chromatin modification. (nih.gov)
In recent years, histone modification has been implicated as an essential part in the pathogenesis of PTSD for the following reason: the development of PTSD is usually related to the maladaptation of fear memory induced by traumatic events, and histone modification plays an important role in the consolidation and extinction of fear memory correspondingly. (psych.ac.cn)
At present, techniques commonly used for the measurement of histone modification are Western Blotting and chromatin immunoprecipitation (ChIP), both based on the antibody technology. (psych.ac.cn)
What's more, animal models are the main methods to explore the association between histone modification and PTSD, using electric shocks (e.g., inescapable foot shock, tail shock, and tone shock), social stress (e.g., predator exposure), and single prolonged stress (SPS) to simulate symptoms of PTSD in the laboratory. (psych.ac.cn)
We systematically searched and screened the literatures of histone modification in PTSD through PubMed ( http://www.ncbi.nlm.nih.gov/pubmed/ ), PsychINFO ( http://psycnet.apa.org/ ), and PsychArticles ( http://psycnet.apa.org/ ), with finally 16 literatures selected for detailed integration and discussion. (psych.ac.cn)

Rtt109 acetylates histone H3 lysine 56 and functions in DNA replication. (embl.de)

Small molecules, including pan-PI3K and dual PI3K/mTOR inhibitors, have shown moderate success clinically, due to broad on-target/off-tissue effects. (bvsalud.org)

Recent achievements highlight the accelerated development of epigenetics, such as the definition of a human DNA methylome at single-nucleotide resolution, the various discoveries of histone variants and modifications, the study of the CpG island in the genome, and the progress of genome-wide nucleosome positioning maps ( Baldi, 2019 ). (frontiersin.org)
A closely related debate around chromatin modifications is about causality: several histone PTMs correlate with specific transcriptional states, but in many cases they are not responsible for a transcriptional outcome but rather are a consequence of it [7] . (plos.org)
Characterization of histone modifications at subtelomeric regions revealed H3 trimethyl-K9, H3 trimethyl-K27, and H4 trimethyl-K20 enrichment. (biomedcentral.com)

The fission yeast S. pombe lacks Sir3p and Sir4p but employs methylation of histone H3 lysine 9 (K9) plus a Sir2p homologue (Sir2) for silencing [ 15 ]. (biomedcentral.com)

They contain a bromodomain, which helps them recognize and bind to acetylated lysine residues on histone substrates. (wikipedia.org)
This is supported by pharmacological targeting where the first-generation pan-BET bromodomain inhibitor JQ1(+) displays anti-inflammatory effects and inhibit tumor cell eradication, while the novel bivalent BET bromodomain inhibitor AZD5153, which shows differential activity towards BET family members, does not. (frontiersin.org)

Both gain-of-function EZH2 mutations and inactivating histone acetyltransferases mutations, such as CREBBP and EP300, have been implicated in the pathogenesis of germinal center (GC) derived lymphomas. (chicagobiomedicalconsortium.org)

It is responsible for most of the cytoplasmic HAT activity in yeast, and it binds strongly to histone H4 by virtue of its association with an additional subunit, Hat2. (wikipedia.org)
CARM1 Inhibitor The CARM1 Inhibitor controls the biological activity of CARM1. (sigmaaldrich.com)
Histone acetyltransferase assays performed at Reaction Biology are radiometric activity assays using tritiated acetyl-Coenzyme A as a cofactor. (reactionbiology.com)
Rtt109 does not show sequence conservation with other knownHATs and depends on association with either of two histone chaperones, Asf1 orVps75, for HAT activity. (embl.de)

Implications forunderstanding histone substrate and chaperone binding by Rtt109 are discussed. (embl.de)

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. (rndsystems.com)
Drug-like molecules that can reprogram selected histone PTMs in tumour cells are therefore of interest as potential cancer chemopreventive agents. (biomedcentral.com)

Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. (absource.de)

Several voices have questioned this use of the word epigenetics, because many histone PTMs do not carry heritable information [1] - [8] . (plos.org)

Histone PTMs are also critical for other genomic functions, such as DNA replication and induction of repair mechanisms at sites of DNA damage [ 3 ]. (biomedcentral.com)

During spermatogenesis of many species the histone-based chromatin structure of the paternal genome becomes disassembled. (uni-marburg.de)

This family also incorporates the p300/CBP histone acetyltransferase domain which has different catalytic properties and cofactor regulation to KAT11 (PMID:18568037). (embl.de)

Targeting Tyrosyl-DNA phosphodiesterase 1 enzyme with natural products as a potential method for improving efficacy of topoisomerase I inhibitors in cancer therapy. (sharjah.ac.ae)
Allopurinol is a purine analog inhibitor of the enzyme xanthine oxidase, used to treat gout or kidney stones, and to decrease levels of uric acid. (absource.de)
We obtained 12 crystal structures of enzyme-inhibitor complexes, which guided our rational structure-based design of 72 thieno[2,3-d]pyrimidine analogues divided into three families. (cdc.gov)

Ketoprofen is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. (absource.de)
Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. (absource.de)

Fungal Rtt109 histone acetyltransferase is an unexpected structural homolog ofmetazoan p300/CBP. (embl.de)

Additionally, we describe a new p300/CBP HAT inhibitor, C107, and show that it can also increase cellular Histac FRET. (nih.gov)
Investigating the role of the histone acetyltransferase CBP in orchestrating cellular response to genotoxic stress involved in breast tumorigenesis and response to chemotherapy. (sharjah.ac.ae)

Anatomy7

Organisms1

Chemicals and Drugs50

Analytical, Diagnostic and Therapeutic Techniques and Equipment8

Phenomena and Processes30

Information Science3

Acetylation33

Deacetylase9

HDAC8

Family of histone acetyltransferases3

Proteins10

Enzymes7

Potent9

Deacetylases2

Inhibits2

HDACs1

HATS6

Epigenetic6

Transferring an acetyl group1

Inhibition5

Acetyl group2

Garcinol3

Selective4

Methyltransferase1

Gene2

Specific histone1

Protein4

Transcription2

Modification5

Acetylates1

MTOR1

Modifications3

Methylation1

Bromodomain2

CREBBP1

Activity4

Substrate1

Tumour2

Competitive inhibitor1

Epigenetics1

PTMs1

Chromatin structure1

Regulation1

Enzyme3

Anti-inflammatory2

Homolog1

Cellular2