Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Anthony C. Varca"'
Autor:
Wai Cheung Chan, Xiaoxi Liu, Robert S. Magin, Nicholas M. Girardi, Scott B. Ficarro, Wanyi Hu, Maria I. Tarazona Guzman, Cara A. Starnbach, Alejandra Felix, Guillaume Adelmant, Anthony C. Varca, Bin Hu, Ariana S. Bratt, Ethan DaSilva, Nathan J. Schauer, Isabella Jaen Maisonet, Emma K. Dolen, Anthony X. Ayala, Jarrod A. Marto, Sara J. Buhrlage
Publikováno v:
Nature Communications, Vol 14, Iss 1, Pp 1-13 (2023)
Deubiquitinases (DUBs) are key signaling enzymes, many of which lack selective inhibitors. Chan et al. pair a DUB-focused covalent library to mass spectrometry activity-based protein profiling, leading to selective hits against 23 endogenous DUBs and
Externí odkaz:
https://doaj.org/article/d6b807ef0bbf47468c2c964d3363d37f
Publikováno v:
STAR Protocols, Vol 2, Iss 4, Pp 100896- (2021)
Summary: Identification of selective deubiquitinase (DUB) inhibitors is critical for probe development to further understand and explore DUB biological function. Here, we detail the optimization and deployment of an in vitro fluorogenic ubiquitin-rho
Externí odkaz:
https://doaj.org/article/a9c38f7b02f84904905e697a3e8f17d7
Autor:
Julien Olivet, Soon Gang Choi, Salvador Sierra, Tina M. O’Grady, Mario de la Fuente Revenga, Florent Laval, Vladimir V. Botchkarev, Christoph Gorgulla, Paul W. Coote, Jérémy Blavier, Ezekiel A. Geffken, Jimit Lakhani, Kijun Song, Zoe C. Yeoh, Bin Hu, Anthony C. Varca, Jonathan Bruyr, Samira Ibrahim, Tasneem Jivanjee, Joshua D. Bromley, Sarah K. Nyquist, Aaron Richardson, Hong Yue, Yang Wang, Natalia Calonghi, Alessandra Stefan, Kerstin Spirohn, Didier Vertommen, Maria F. Baietti, Irma Lemmens, Hyuk-Soo Seo, Mikhail G. Dozmorov, Luc Willems, Jan Tavernier, Kalyan Das, Eleonora Leucci, Alejandro Hochkoeppler, Zhen-Yu Jim Sun, Michael A. Calderwood, Tong Hao, Alex K. Shalek, David E. Hill, Andras Boeszoermenyi, Haribabu Arthanari, Sara J. Buhrlage, Sirano Dhe-Paganon, Javier González-Maeso, Franck Dequiedt, Jean-Claude Twizere, Marc Vidal
Enzymatic pockets such as those of histone deacetylases (HDACs) are among the most favored targets for drug development. However, enzymatic inhibitors often exhibit low selectivity and high toxicity due to targeting multiple enzyme paralogs, which ar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8635e9e2aa438eb8f00e273e12bf49c9
https://doi.org/10.1101/2022.12.07.519454
https://doi.org/10.1101/2022.12.07.519454
Publikováno v:
STAR Protocols, Vol 2, Iss 4, Pp 100896-(2021)
STAR Protocols
STAR Protocols
Summary Identification of selective deubiquitinase (DUB) inhibitors is critical for probe development to further understand and explore DUB biological function. Here, we detail the optimization and deployment of an in vitro fluorogenic ubiquitin-rhod
Autor:
Eric S. Fischer, Nathan J. Schauer, Wanyi Hu, Katherine A. Donovan, Xiaoxi Liu, Jonathan W. Bushman, Sara J. Buhrlage, Anthony C. Varca
Publikováno v:
Cell Chem Biol
Deubiquitinating enzymes (DUBs) catalyze the removal of ubiquitin, thereby reversing the activity of E3 ubiquitin ligases and are central to the control of protein abundance and function. Despite the growing interest in DUBs as therapeutic targets, c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84c5cdb4a2f877df106a83ea1f7518f4
https://europepmc.org/articles/PMC7855594/
https://europepmc.org/articles/PMC7855594/
Autor:
Douglas S. Auld, Robert S. Magin, Wai Cheung Chan, Xiaoxi Liu, Sara J. Buhrlage, Hyuk-Soo Seo, Bin Hu, Rebekka M. Roberts, Sirano Dhe-Paganon, Anthony C. Varca, He Zhu, Jarrod A. Marto, Dominick Casalena
Publikováno v:
Cell Chem Biol
Deubiquitinating enzymes (DUBs) are a class of isopeptidases that regulate ubiquitin dynamics through catalytic cleavage of ubiquitin from protein substrates and ubiquitin precursors. Despite growing interest in DUB biological function and potential
Autor:
Samuel Kitara, Angela Su, Giovanni Roti, Andrew L. Kung, Marta Sanchez-Martin, James E. Bradner, Anthony C. Varca, Jun Qi, Adolfo A. Ferrando, Kimberly Stegmaier, Lei Wu, Amy Saur Conway
Publikováno v:
The Journal of Experimental Medicine
NOTCH1 is an attractive cancer target, particularly in T cell acute lymphoblastic leukemia (T-ALL), with activating mutations in this gene identified in more than 50% of cases. In this study, Roti et al. describe the synthesis, characterization, and
Autor:
Michael Hadler, William B. Smith, Sirano Dhe-Paganon, Alexander J. Federation, Scott A. Armstrong, Lei Wu, Roodolph St. Pierre, Anthony C. Varca, Jason J. Marineau, Joanna S. Yi, Jun Qi, Emma J. Chory, James E. Bradner, Amanda Souza, Xiang Xu
Publikováno v:
ACS Chemical Biology
The DOT1L lysine methyltransferase has emerged as a validated therapeutic target in MLL-rearranged (MLLr) acute leukemias. Although S-adenosylmethionine competitive inhibitors have demonstrated pharmacological proof-of-principle in MLLr-leukemia, the
Autor:
Kimberly Stegmaier, Jun Qi, Samuel Kitara, Marta Sanchez-Martin, Anthony C. Varca, Adolfo A. Ferrando, James E. Bradner, Giovanni Roti, Andrew L. Kung
Publikováno v:
Blood. 128:889-889
Several studies strongly support the development of Notch1 inhibitors for targeted cancer therapy. This idea is most compelling for T cell acute lymphoblastic leukemia/lymphoma (T-ALL) where activating mutations of NOTCH1 are present in 55-60% of the
Autor:
Sirano Dhe-Paganon, Scott A. Armstrong, Joanna S. Yi, Jun Qi, Roodolph St. Pierre, Anthony C. Varca, Alexander J. Federation, James E. Bradner, Xiang Xu, Michael Hadler
Publikováno v:
Blood. 124:4811-4811
Cooperation between several epigenetic modulators defines MLL-rearranged leukemia as an epigenomic-driven cancer. Wild type MLL catalyzes trimethylation of lysine 4 on histone 3 from the methyl donor S-adenosylmethionine (SAM) at homeobox and other g