Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Daniel P, Uccello"'
Autor:
James Schiemer, Andrew Maxwell, Reto Horst, Shenping Liu, Daniel P. Uccello, Kris Borzilleri, Nisha Rajamohan, Matthew F. Brown, Matthew F. Calabrese
Publikováno v:
Nature Communications, Vol 14, Iss 1, Pp 1-12 (2023)
Bridging covalent ligand discovery with chimeric degrader design has emerged as a mechanism to target proteins that lack enzymatic activity or are intractable. Here, the authors use biochemical and cellular tools to deconvolute the role of covalent m
Externí odkaz:
https://doaj.org/article/8332ec11fd3e488aa9daf64205146e29
Autor:
Xidong Feng, Ye Che, Adam M. Gilbert, Reto Horst, Kris A. Borzilleri, Matthew Merrill Hayward, Carolyn A. Leverett, James Schiemer, Yilin Meng, Justin I. Montgomery, Matthew F. Calabrese, Mark C. Noe, Daniel P. Uccello, Stephen P. Brown, Matthew Frank Brown, Yingrong Xu
Publikováno v:
Nature Chemical Biology. 17:152-160
Heterobifunctional chimeric degraders are a class of ligands that recruit target proteins to E3 ubiquitin ligases to drive compound-dependent protein degradation. Advancing from initial chemical tools, protein degraders represent a mechanism of growi
Autor:
Laura A. McAllister, Michael Aaron Brodney, Jane M. Withka, Jiangli Yan, Thomas N. O'Connell, Laurence Philippe, Kevin Ogilvie, Lara C. Czabaniuk, Matthew Frank Brown, Guoyun Bai, Adam M. Gilbert, Daniel P. Uccello, Erik Alphie Lachapelle, Chao Li, Michael J. Shapiro, Christopher Ryan Butler, Romelia Salomon-Ferrer, Jeremy T. Starr
Publikováno v:
ACS Med Chem Lett
[Image: see text] The ring strain present in azetidines can lead to undesired stability issues. Herein, we described a series of N-substituted azetidines which undergo an acid-mediated intramolecular ring-opening decomposition via nucleophilic attack
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61495fbd8a53cc5202ef7fb9ae427eaa
https://europepmc.org/articles/PMC8521649/
https://europepmc.org/articles/PMC8521649/
Publikováno v:
Organic letters. 22(15)
The polyethylene glycol (PEG) moiety has become increasingly important in medicinal chemistry. Herein, we describe the PEG functionalization of amines via hydrogen borrowing reductive amination. This was accomplished using the [Ru(
Autor:
James, Schiemer, Reto, Horst, Yilin, Meng, Justin I, Montgomery, Yingrong, Xu, Xidong, Feng, Kris, Borzilleri, Daniel P, Uccello, Carolyn, Leverett, Stephen, Brown, Ye, Che, Matthew F, Brown, Matthew M, Hayward, Adam M, Gilbert, Mark C, Noe, Matthew F, Calabrese
Publikováno v:
Nature chemical biology. 17(2)
Heterobifunctional chimeric degraders are a class of ligands that recruit target proteins to E3 ubiquitin ligases to drive compound-dependent protein degradation. Advancing from initial chemical tools, protein degraders represent a mechanism of growi
Autor:
Michael Herr, Daniel P. Canterbury, Derek M. Erion, Janice A. Brown, Mark Niosi, Bhagyashree Khunte, Matthew Gorgoglione, Jaclyn Siderewicz, Jana Polivkova, Carmen N. Garcia-Irizarry, Nathan E. Genung, Adam M. Gilbert, Justin I. Montgomery, Daniel P. Uccello, Timothy P. Rolph, Adhiraj Lanba, Qifang Li, Nicholas B. Vera, Kentaro Futatsugi, Gary Erik Aspnes, Zhenhong Li, James R. Gosset, Kim Huard, Matthew Merrill Hayward, Shawn Cabral, Magee Thomas Victor, Julie Purkal, Kevin B. Bahnck
Publikováno v:
Journal of Medicinal Chemistry. 59:1165-1175
Inhibition of the sodium-coupled citrate transporter (NaCT or SLC13A5) has been proposed as a new therapeutic approach for prevention and treatment of metabolic diseases. In a previous report, we discovered dicarboxylate 1a (PF-06649298) which inhibi
Autor:
Jennifer A. Young, Mark Edward Flanagan, Jinshan M. Chen, Carmen N. Garcia-Irizarry, R. Scott Obach, Brandon P. Schuff, Jeremy T. Starr, Upendra P. Dahal, Daniel P. Uccello, Adam M. Gilbert
Publikováno v:
MedChemComm. 7:864-872
Covalent drugs contain a reactive electrophilic moiety or covalent reactive group (CRG), which forms an irreversible bond between the drug and a biological target. Consequently, the intrinsic reactivity of the CRG is an important consideration in the
Autor:
Suman Luthra, Graham M. West, Jeremy T. Starr, Matthew Frank Brown, Matthew F. Calabrese, Jinshan Chen, Hongyao Zhu, Xiayang Qiu, Daniel P. Uccello, Matthew Merrill Hayward, Jeanne S. Chang, Jotham Wadsworth Coe, Kathleen A. Farley, Kris A. Borzilleri, Mark C. Noe, Justin I. Montgomery, Adam M. Gilbert, Veerabahu Shanmugasundaram, Lara C. Czabaniuk, Robert M. Oliver, Carmen N. Garcia-Irrizary, Brandon P. Schuff, Chuong Nguyen, Yingrong Xu, James Schiemer, Jaymin C. Shah, Xidong Feng, Mark Niosi, Jennifer A. Young, WeiDong Ding, Ayman El-Kattan, Adelajda Zorba, James F. Smith
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that simultaneously bind to a target protein and an E3 ligase, thereby leading to ubiquitination and subsequent degradation of the target. They present an exciting opport
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf434de63be490efb6416cf59a222839
https://europepmc.org/articles/PMC6077745/
https://europepmc.org/articles/PMC6077745/
Autor:
Timothy L. Foley, Justin I. Montgomery, Daniel P. Uccello, Anthony R. Harris, Steven Victor O'neil, Bruce N. Rogers, Douglas S. Johnson, Justin R. Piro, Tarek A. Samad, Christopher Ryan Butler, Stephen Noell, Rafael G. Silva, Deane M. Nason, Christopher John Helal, Adam M. Gilbert, Julie Cianfrogna, Laura A. McAllister, Scot Richard Mente, Christopher L. Shaffer, Kari R. Fonseca, Damien Webb, Jayvardhan Pandit, Michael Aaron Brodney
Publikováno v:
Journal of medicinal chemistry. 61(7)
Monoacylglycerol lipase (MAGL) inhibition provides a potential treatment approach to neuroinflammation through modulation of both the endocannabinoid pathway and arachidonoyl signaling in the central nervous system (CNS). Herein we report the discove
Autor:
Daniel P. Uccello, Jeremy T. Starr, Matthew Merrill Hayward, R. Scott Obach, Mark C. Noe, Adam M. Gilbert, Justin I. Montgomery, Mark Edward Flanagan, Veerabahu Shanmugasundaram, Dennis P. Anderson, Ann Aulabaugh, Ye Che, Matthew Frank Brown, Michael J. Shapiro, Chao Li, Tim F. Ryder, Stacey R. Oppenheimer, Laurence Philippe, Gregory S. Walker, Yan Wu, Brandon P. Schuff, Joseph A. Abramite, Jinshan M. Chen, Justin G. Stroh, Upendra P. Dahal
Publikováno v:
Journal of Medicinal Chemistry. 57:10072-10079
Interest in drugs that covalently modify their target is driven by the desire for enhanced efficacy that can result from the silencing of enzymatic activity until protein resynthesis can occur, along with the potential for increased selectivity by ta