Richard T Cummings
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Explore the profile of Richard T Cummings including associated specialties, affiliations and a list of published articles.
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31
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1057
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Recent Articles
11.
Vinogradova M, Gehling V, Gustafson A, Arora S, Tindell C, Wilson C, et al.
Nat Chem Biol
. 2016 May;
12(7):531-8.
PMID: 27214401
The KDM5 family of histone demethylases catalyzes the demethylation of histone H3 on lysine 4 (H3K4) and is required for the survival of drug-tolerant persister cancer cells (DTPs). Here we...
12.
Taylor A, Cote A, Hewitt M, Pastor R, LeBlanc Y, Nasveschuk C, et al.
ACS Med Chem Lett
. 2016 May;
7(5):531-6.
PMID: 27190605
CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology. As part of our effort to explore the potential therapeutic implications of selectively...
13.
Ghosh S, Taylor A, Chin M, Huang H, Conery A, Mertz J, et al.
J Biol Chem
. 2016 Apr;
291(25):13014-27.
PMID: 27056325
Covalent modification of histones is a fundamental mechanism of regulated gene expression in eukaryotes, and interpretation of histone modifications is an essential feature of epigenetic control. Bromodomains are specialized binding...
14.
Taylor A, Vaswani R, Gehling V, Hewitt M, LeBlanc Y, Audia J, et al.
ACS Med Chem Lett
. 2016 Mar;
7(2):145-50.
PMID: 26985289
Inhibition of the bromodomains of the BET family, of which BRD4 is a member, has been shown to decrease myc and interleukin (IL) 6 in vivo, markers that are of...
15.
Albrecht B, Gehling V, Hewitt M, Vaswani R, Cote A, LeBlanc Y, et al.
J Med Chem
. 2016 Jan;
59(4):1330-9.
PMID: 26815195
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising approach to...
16.
Gehling V, Vaswani R, Nasveschuk C, Duplessis M, Iyer P, Balasubramanian S, et al.
Bioorg Med Chem Lett
. 2015 Jul;
25(17):3644-9.
PMID: 26189078
The discovery and optimization of a series of small molecule EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit (2), a series of indole-based EZH2 inhibitors were identified. Biochemical potency...
17.
Bradley W, Arora S, Busby J, Balasubramanian S, Gehling V, Nasveschuk C, et al.
Chem Biol
. 2014 Dec;
21(11):1463-75.
PMID: 25457180
The histone lysine methyltransferase (MT) Enhancer of Zeste Homolog 2 (EZH2) is considered an oncogenic driver in a subset of germinal center B-cell-like diffuse large B cell lymphoma (GCB-DLBCL) and...
18.
Cummings R, Maegley K, Hill W, Sims R, Mohin S
Assay Drug Dev Technol
. 2014 Aug;
12(8):452-6.
PMID: 25127183
No abstract available.
19.
Ni Y, Di Marco S, Condra J, Peterson L, Wang W, Wang F, et al.
J Lipid Res
. 2010 Oct;
52(1):78-86.
PMID: 20959675
Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) regulates LDL cholesterol levels by inhibiting LDL receptor (LDLr)-mediated cellular LDL uptake. We have identified a fragment antigen-binding (Fab) 1D05 which binds PCSK9 with...
20.
Ni Y, Condra J, Orsatti L, Shen X, Di Marco S, Pandit S, et al.
J Biol Chem
. 2010 Feb;
285(17):12882-91.
PMID: 20172854
PCSK9 binds to the low density lipoprotein receptor (LDLR) and leads to LDLR degradation and inhibition of plasma LDL cholesterol clearance. Consequently, the role of PCSK9 in modulating circulating LDL...