Joseph Fargnoli
Overview
Explore the profile of Joseph Fargnoli including associated specialties, affiliations and a list of published articles.
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Articles
32
Citations
721
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0
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Recent Articles
1.
Cherney E, Zhang L, Nara S, Zhu X, Gullo-Brown J, Maley D, et al.
ACS Med Chem Lett
. 2021 Feb;
12(2):288-294.
PMID: 33603977
Indoleamine 2,3-dioxygenase 1 (IDO1) is a heme-containing dioxygenase enzyme implicated in cancer immune response. This account details the discovery of BMS-986242, a novel IDO1 inhibitor designed for the treatment of...
2.
Velaparthi U, Padmakar Darne C, Warrier J, Liu P, Rahaman H, Augustine-Rauch K, et al.
ACS Med Chem Lett
. 2020 Feb;
11(2):172-178.
PMID: 32071685
Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics. Herein, we report the discovery, optimization, and evaluation of a potent, selective, and orally...
3.
Zhang Y, Zhao Y, Tebben A, Sheriff S, Ruzanov M, Fereshteh M, et al.
ACS Med Chem Lett
. 2018 Nov;
9(11):1117-1122.
PMID: 30429955
The multifunctional cytokine TGFβ plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFβ signaling in concert with checkpoint blockade will provide improved and...
4.
Harikrishnan L, Warrier J, Tebben A, Tonukunuru G, Madduri S, Baligar V, et al.
Bioorg Med Chem
. 2018 Feb;
26(5):1026-1034.
PMID: 29422332
The TGFβ-TGFβR signaling pathway has been reported to play a protective role in the later stages of tumorigenesis via increasing immunosuppressive Treg cells and facilitating the epithelial to mesenchymal transition...
5.
Villaume M, Sella E, Saul G, Borzilleri R, Fargnoli J, Johnston K, et al.
ACS Cent Sci
. 2016 May;
2(1):27-31.
PMID: 27163023
The fungal-derived Taiwanese natural product antroquinonol A has attracted both academic and commercial interest due to its reported exciting biological properties. This reduced quinone is currently in phase II trials...
6.
Talbott R, Borzilleri R, Chaudhry C, Fargnoli J, Shen H, Fairchild C, et al.
Exp Cell Res
. 2015 Aug;
338(2):251-60.
PMID: 26302264
Cellular levels of inhibitor of apoptosis (IAP) proteins are elevated in multiple human cancers and their activities often play a part in promoting cancer cell survival by blocking apoptotic pathways,...
7.
Zhang Y, Seigal B, Terrett N, Talbott R, Fargnoli J, Naglich J, et al.
ACS Med Chem Lett
. 2015 Jul;
6(7):770-5.
PMID: 26191364
A series of dimeric macrocyclic compounds were prepared and evaluated as antagonists for inhibitor of apoptosis proteins. The most potent analogue 11, which binds to XIAP and c-IAP proteins with...
8.
Seigal B, Connors W, Fraley A, Borzilleri R, Carter P, Emanuel S, et al.
J Med Chem
. 2015 Feb;
58(6):2855-61.
PMID: 25695766
Affinity selection screening of macrocycle libraries derived from DNA-programmed chemistry identified XIAP BIR2 and BIR3 domain inhibitors that displace bound pro-apoptotic caspases. X-ray cocrystal structures of key compounds with XIAP...
9.
Perez H, Chaudhry C, Emanuel S, Fanslau C, Fargnoli J, Gan J, et al.
J Med Chem
. 2015 Jan;
58(3):1556-62.
PMID: 25584393
The prominent role of IAPs in controlling cell death and their overexpression in a variety of cancers has prompted the development of IAP antagonists as potential antitumor therapies. We describe...
10.
Roongta U, Pabalan J, Wang X, Ryseck R, Fargnoli J, Henley B, et al.
Mol Cancer Res
. 2011 Sep;
9(11):1551-61.
PMID: 21954435
Emerging literature suggests that metabolic pathways play an important role in the maintenance and progression of human cancers. In particular, recent studies have implicated lipid biosynthesis and desaturation as a...