Rishi G Vaswani
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Explore the profile of Rishi G Vaswani including associated specialties, affiliations and a list of published articles.
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Articles
15
Citations
390
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Recent Articles
1.
Vaswani R, Huang D, Anthony N, Xu L, Centore R, Schiller S, et al.
J Med Chem
. 2025 Jan;
68(2):1772-1792.
PMID: 39801091
BRM (SMARCA2) and BRG1 (SMARCA4) are mutually exclusive ATPase subunits of the mSWI/SNF (BAF) chromatin remodeling complex. BAF is an attractive therapeutic target because of its role in transcription, and...
2.
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...
3.
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...
4.
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...
5.
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...
6.
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...
7.
Hewitt M, LeBlanc Y, Gehling V, Vaswani R, Cote A, Nasveschuk C, et al.
Bioorg Med Chem Lett
. 2015 Apr;
25(9):1842-8.
PMID: 25851940
In this report we detail the evolution of our previously reported thiophene isoxazole BET inhibitor chemotype exemplified by CPI-3 to a novel bromodomain selective chemotype (the methyl isoxazoleazepine chemotype) exemplified...
8.
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...
9.
Vaswani R, Albrecht B, Audia J, Cote A, Dakin L, Duplessis M, et al.
Org Lett
. 2014 Jul;
16(16):4114-7.
PMID: 25068576
A method for the synthesis of N-functionalized C2-/C3-substituted indoles via Pd-catalyzed C-N bond coupling of halo-aryl enamines is described. The general strategy utilizes a variety of amines and β-keto esters...
10.
Gehling V, Hewitt M, Vaswani R, LeBlanc Y, Cote A, Nasveschuk C, et al.
ACS Med Chem Lett
. 2014 Jun;
4(9):835-40.
PMID: 24900758
The identification of a novel series of small molecule BET inhibitors is described. Using crystallographic binding modes of an amino-isoxazole fragment and known BET inhibitors, a structure-based drug design effort...