Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Fiona Pachl"'
Autor:
Jonathan D. Taylor, Nathalie Barrett, Sergio Martinez Cuesta, Katelyn Cassidy, Fiona Pachl, James Dodgson, Radhika Patel, Tuula M. Eriksson, Aidan Riley, Matthew Burrell, Christin Bauer, D. Gareth Rees, Raffaello Cimbro, Andrew X. Zhang, Ralph R. Minter, James Hunt, Sandrine Legg
Publikováno v:
Communications Biology, Vol 7, Iss 1, Pp 1-17 (2024)
Abstract Proteins can be targeted for degradation by engineering biomolecules that direct them to the eukaryotic ubiquitination machinery. For instance, the fusion of an E3 ubiquitin ligase to a suitable target binding domain creates a ‘biological
Externí odkaz:
https://doaj.org/article/82c3864e38134c29b42485f93454e6e6
Autor:
Jeffrey W. Johannes, Fiona Pachl, Amber Balazs, Tieguang Yao, C. Larner, Lisa McWilliams, Marianne Schimpl, Scott W. Martin, Kevin J. Embrey, Tom D. Heightman, Paul Hemsley, Jonathan P. Orme, Derek Barratt, Giuditta Illuzzi, Andrew Madin, Paolo Di Fruscia, Avipsa Ghosh, Martin J. Packer, Scott D. Edmondson, Elisabetta Leo, Xiaolan Zheng, Matthew D. Chuba, Xiaohui Pei, Mark J. O'Connor, Verity Talbot, Ke Zhang, Stephen Fawell, Elizabeth Underwood, Anna Staniszewska, Lina Liu, Lin Xue, Sonja J. Gill, Anders Gunnarsson, Andrew Pike, Susan E. Critchlow, Jeffrey G. Varnes, Andrew X. Zhang, Sébastien L. Degorce, J. Lane, Sudhir M. Hande, Hongyao She, Sabina Cosulich, Michal Bista
Publikováno v:
Journal of Medicinal Chemistry. 64:14498-14512
Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA mutation. However, some have failed in combination with first-line chemotherapies, usually
Publikováno v:
SLAS Discovery. 26:518-523
Mass spectrometry-based proteomics profiling is a discovery tool that enables researchers to understand the mechanisms of action of drug candidates. When applied to proteolysis targeting chimeras (PROTACs) such approaches provide unbiased perspective
Autor:
Pieter Giesbertz, Hannelore Daniel, Theresa Schöttl, Martin Klingenspor, Bernhard Kuster, Tobias Fromme, Fiona Pachl
Publikováno v:
Obesity. 28:590-600
Objective Previous studies have revealed decreased mitochondrial respiration in adipocytes of obese mice. This study aimed to identify the molecular underpinnings of altered mitochondrial metabolism in adipocytes. Methods Untargeted proteomics of mit
Autor:
Avipsa Ghosh, Sudhir M. Hande, Amber Balazs, Derek Barratt, Sabina Cosulich, Barry Davies, Sébastien Degorce, Kevin Embrey, Sonja Gill, Anders Gunnarsson, Giuditta Illuzzi, Peter Johnström, Jordan Lane, Carrie Larner, Rachel Lawrence, Elisabetta Leo, Andrew Madin, Elizabeth Martin, Lisa McWilliams, Lenka O’Connor, Mark O’Connor, Jonathan Orme, Fiona Pachl, Martin Packer, Andy Pike, Philip Rawlins, Marianne Schimpl, Magnus Schou, Anna Staniszewska, Wenzhan Yang, James Yates, Andrew Zhang, XiaoLa Zheng, Stephen Fawell, Petra Hamerlik, Jeffrey Johannes
Publikováno v:
Cancer Research. 82:6302-6302
PARP inhibitors exploit defects in DNA repair pathways to selectively target cancerous cells via PARP1 catalytic inhibition and PARP1 trapping onto the DNA. All known clinical PARP1 inhibitors bind at the same site at the catalytic center of the enzy
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase
Autor:
Claire Crafter, Erica Banks, Yumeng Mao, Omid Tavana, Bin Yang, David Kouvchinov, Viia Valge-Archer, Fiona Pachl, Sébastien L. Degorce, Anisha Solanki, Lakshmaiah Gingipalli, Scott D. Edmondson
Publikováno v:
Journal of medicinal chemistry. 63(18)
We report the first disclosure of IRAK3 degraders in the scientific literature. Taking advantage of an opportune byproduct obtained during our efforts to identify IRAK4 inhibitors, we identified ready-to-use, selective IRAK3 ligands in our compound c
Autor:
Pete Newham, Helen Boyd, M. Paola Castaldi, Fiona Pachl, Clay W Scott, Andrew X. Zhang, Kevin Moreau, Göran Dahl, Muireann Coen
Publikováno v:
Br J Pharmacol
Proteolysis-targeting chimeras are a new drug modality that exploits the endogenous ubiquitin proteasome system to degrade a protein of interest for therapeutic benefit. As the first-generation of proteolysis-targeting chimeras have now entered clini
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fcd7a568c229ff314cd00bfa85807cce
http://hdl.handle.net/10044/1/77454
http://hdl.handle.net/10044/1/77454
Autor:
Mark J. O'Connor, Philip B. Rawlins, Kevin J. Embrey, Anders Gunnarsson, Sudhir M. Hande, Anna Staniszewska, Fiona Pachl, Andrew X. Zhang, Jonathan P. Orme, Giuditta Illuzzi, Lisa McWilliams, Sonja J. Gill, Jeffrey W. Johannes, J. Lane, Sébastien L. Degorce, Amber Balazs, Martin J. Packer, Andrew Madin, Marianne Schimpl, Andrew Pike, Elisabetta Leo, Xiaolan Zheng, Avipsa Ghosh, C. Larner
Publikováno v:
Cancer Research. 81:296-296
Since the approval of olaparib in 2014 for BRCA mutated (BRCAm) ovarian cancer, many PARP inhibitors have been developed and have seen widespread success. However, as a class, these drugs are not without adverse events which have limited their abilit
Autor:
Bernhard Kuster, Nancy L. Brackett, Dominic Helm, Fiona Pachl, Jürgen Schiller, Barbara Ferreira da Silva, Emad Ibrahim, Chen Meng, Charles M. Lynne, Ricardo Pimenta Bertolla
Publikováno v:
Molecular & Cellular Proteomics. 15:1424-1434
The study of male infertility after spinal cord injury (SCI) has enhanced the understanding of seminal plasma (SP) as an important regulator of spermatozoa function. However, the most important factors leading to the diminished sperm motility and via
Autor:
Sameer Kawatkar, Philip B. Rawlins, Ning Gao, S. Bagal, Ronald Tomlinson, David Matthew Wilson, Elisabetta Chiarparin, James Robinson, Jessie Hao-Ru Hsu, Erin Code, Emma Bednarski, Lisa Drew, Kelly Jacques, Stephen Fawell, Andrew Bloecher, Xiahui Zhu, M. Paola Castaldi, Timothy Rasmusson, Haley Woods, Jon Read, Argyrides Argyrou, Minhui Shen, Daniel H. O' Donovan, Fiona Pachl
Publikováno v:
Cell Chemical Biology. 27:41-46.e17
Summary Deregulation of the PRC2 complex, comprised of the core subunits EZH2, SUZ12, and EED, drives aberrant hypermethylation of H3K27 and tumorigenicity of many cancers. Although inhibitors of EZH2 have shown promising clinical activity, preclinic