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
1.
Keller P, Adams E, Wu R, Cote A, Arora S, Cantone N, et al.
Cancer Res
. 2024 Jun;
84(15):2501-2517.
PMID: 38833522
Recurrent somatic mutations in the BRG1/BRM-associated factor (BAF) chromatin remodeling complex subunit ARID1A occur frequently in advanced urothelial, endometrial, and ovarian clear cell carcinomas, creating an alternative chromatin state that...
2.
Cantone N, Cummings R, Trojer P
Methods Mol Biol
. 2022 Jun;
2529:477-490.
PMID: 35733027
Potent and highly selective small-molecule inhibitors are needed to unravel the biological complexities of histone methyltransferases and to reveal their therapeutic potential. A prerequisite to developing these inhibitors is the...
3.
Stuckey J, Cantone N, Cote A, Arora S, Vivat V, Ramakrishnan A, et al.
J Biol Chem
. 2021 Feb;
296:100349.
PMID: 33524394
The histone methyltransferase EZH2 has been the target of numerous small-molecule inhibitor discovery efforts over the last 10+ years. Emerging clinical data have provided early evidence for single agent activity...
4.
Wilson J, Patel G, Patel C, Brucelle F, Huhn A, Gardberg A, et al.
ACS Med Chem Lett
. 2020 Jun;
11(6):1324-1329.
PMID: 32551019
The histone acetyltransferases, CREB binding protein (CBP) and EP300, are master transcriptional co-regulators that have been implicated in numerous diseases, such as cancer, inflammatory disorders, and neurodegeneration. A novel, highly...
5.
Gehling V, McGrath J, Duplessis M, Khanna A, Brucelle F, Vaswani R, et al.
ACS Med Chem Lett
. 2020 Jun;
11(6):1213-1220.
PMID: 32551003
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label...
6.
Khanna A, Cote A, Arora S, Moine L, Gehling V, Brenneman J, et al.
ACS Med Chem Lett
. 2020 Jun;
11(6):1205-1212.
PMID: 32551002
Histone methyltransferase EZH2, which is the catalytic subunit of the PRC2 complex, catalyzes the methylation of histone H3K27-a transcriptionally repressive post-translational modification (PTM). EZH2 is commonly mutated in hematologic malignancies...
7.
Crawford T, Audia J, Bellon S, Burdick D, Bommi-Reddy A, Cote A, et al.
ACS Med Chem Lett
. 2017 Jul;
8(7):737-741.
PMID: 28740608
The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of the bromodomain of...
8.
Vaswani R, Gehling V, Dakin L, Cook A, Nasveschuk C, Duplessis M, et al.
J Med Chem
. 2016 Oct;
59(21):9928-9941.
PMID: 27739677
Polycomb repressive complex 2 (PRC2) has been shown to play a major role in transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3. Dysregulation of...
9.
Labadie S, Dragovich P, Cummings R, Deshmukh G, Gustafson A, Han N, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(18):4492-4496.
PMID: 27499454
Features from a high throughput screening (HTS) hit and a previously reported scaffold were combined to generate 1,7-naphthyridones as novel KDM5 enzyme inhibitors with nanomolar potencies. These molecules exhibited high...
10.
Gehling V, Bellon S, Harmange J, LeBlanc Y, Poy F, Odate S, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(17):4350-4.
PMID: 27476424
This communication describes the identification and optimization of a series of pan-KDM5 inhibitors derived from compound 1, a hit initially identified against KDM4C. Compound 1 was optimized to afford compound...