Robert M Borzilleri
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Explore the profile of Robert M Borzilleri including associated specialties, affiliations and a list of published articles.
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32
Citations
1029
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Recent Articles
1.
Qiao J, Williams D, Gill P, Li L, Norris D, Tokarski J, et al.
J Med Chem
. 2024 Oct;
67(21):19736-19754.
PMID: 39437163
We describe the design, synthesis, and structure-activity relationship (SAR) of heterobifunctional RET ligand-directed degraders (LDDs) derived from three different second-generation RET inhibitors. These LDDs are composed of a target binding...
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.
Donnell A, Zhang Y, Stang E, Wei D, Tebben A, Perez H, et al.
Bioorg Med Chem Lett
. 2017 Nov;
27(23):5267-5271.
PMID: 29102228
Macrocyclic pyrrolobenzodiazepine dimers were designed and evaluated for use as antibody-drug conjugate payloads. Initial structure-activity exploration established that macrocyclization could increase the potency of PBD dimers compared with non-macrocyclic analogs....
6.
McCarver S, Qiao J, Carpenter J, Borzilleri R, Poss M, Eastgate M, et al.
Angew Chem Int Ed Engl
. 2016 Nov;
56(3):728-732.
PMID: 27860140
A method for the decarboxylative macrocyclization of peptides bearing N-terminal Michael acceptors has been developed. This synthetic method enables the efficient synthesis of cyclic peptides containing γ-amino acids and is...
7.
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...
8.
Discenza L, Cornelius G, Gan J, Szapiel N, Talbott R, Chaudhry C, et al.
Bioanalysis
. 2016 Jan;
8(4):265-74.
PMID: 26807991
Background: A target protein-based affinity extraction LC-MS/MS method was developed to enable plasma level determination following ultralow dosing (0.1-3 µg/kg) of an inhibitor of apoptosis proteins molecule. Methodology & results:...
9.
Chaudhry C, Davis J, Zhang Y, Posy S, Lei M, Shen H, et al.
Anal Biochem
. 2016 Jan;
497:8-17.
PMID: 26743718
XIAP (X-chromosome-linked inhibitor of apoptosis protein) is a central apoptosis regulator that blocks cell death by inhibiting caspase-3, caspase-7, and caspase-9 via binding interactions with the XIAP BIR2 and BIR3...
10.
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,...