Identifying chemogenetic interactions from CRISPR screens with drugZ

Autor: Medina Colic, Gang Wang, Michal Zimmermann, Keith Mascall, Megan McLaughlin, Lori Bertolet, W. Frank Lenoir, Jason Moffat, Stephane Angers, Daniel Durocher, Traver Hart

Publikováno v: Genome Medicine, Vol 11, Iss 1, Pp 1-12 (2019)

Abstract Background Chemogenetic profiling enables the identification of gene mutations that enhance or suppress the activity of chemical compounds. This knowledge provides insights into drug mechanism of action, genetic vulnerabilities, and resistan

Externí odkaz: https://doaj.org/article/0660691297e4473f951c2f4ee9ed5f00

Data from RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors

Autor: W. Cameron Black, Michael Zinda, Jordan T.F. Young, Zuomei Li, Yael Mamane, Rino Stocco, Martine Hamel, Artur Veloso, Victoria Rimkunas, Amina Mulani, Kathryn Skorey, Sabrina Vignini-Hammond, Chloe Fugère-Desjardins, William Yang, Hunain Alam, Amandine Chefson, Shou Yun Yin, Marie-Eve Leclaire, Li Li, Sara Fournier, Lee D. Fader, Stéphane Dorich, Valerie Dumais, Émilie Dumas-Bérube, Charles Pellerin, Alexander Skeldon, Robert Papp, Michal Zimmermann, Anne Roulston

Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA replication. RP-3500 is a novel, orally bioavailable clinical-stage ATR kinase inhibitor (NCT04497116). RP-3500 is highly potent with IC50 values of 1.0 and 0.33

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a51beae2425d617ba7d0ef61e96c7e6
https://doi.org/10.1158/1535-7163.c.6651330.v1

RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors

Autor: Anne Roulston, Michal Zimmermann, Robert Papp, Alexander Skeldon, Charles Pellerin, Émilie Dumas-Bérube, Valerie Dumais, Stéphane Dorich, Lee D. Fader, Sara Fournier, Li Li, Marie-Eve Leclaire, Shou Yun Yin, Amandine Chefson, Hunain Alam, William Yang, Chloe Fugère-Desjardins, Sabrina Vignini-Hammond, Kathryn Skorey, Amina Mulani, Victoria Rimkunas, Artur Veloso, Martine Hamel, Rino Stocco, Yael Mamane, Zuomei Li, Jordan T.F. Young, Michael Zinda, W. Cameron Black

Publikováno v: Molecular Cancer Therapeutics. 21:245-256

Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA replication. RP-3500 is a novel, orally bioavailable clinical-stage ATR kinase inhibitor (NCT04497116). RP-3500 is highly potent with IC50 values of 1.0 and 0.33

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5c5c2c693c809fd51b04d00ce59692a4
https://doi.org/10.1158/1535-7163.mct-21-0615

Control of homologous recombination by the HROB–MCM8–MCM9 pathway

Autor: Yuichiro Saito, Masato T. Kanemaki, Yichao Zhao, Michele Olivieri, Dheva Setiaputra, Salomé Adam, Andrea Jurisicova, Jing Yi Yuan, Daniel Durocher, Michal Zimmermann, Nicole Hustedt, Andrea McEwan, Alejandro Álvarez-Quilón

Publikováno v: Genes & Development. 33:1397-1415

DNA repair by homologous recombination (HR) is essential for genomic integrity, tumor suppression, and the formation of gametes. HR uses DNA synthesis to repair lesions such as DNA double-strand breaks and stalled DNA replication forks, but despite h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7b2a0db3611e8b4b54b9b32ffac9e28
https://doi.org/10.1101/gad.329508.119

CRISPR screens identify genomic ribonucleotides as a source of PARP-trapping lesions

Autor: Andrea McEwan, Megha Chandrashekhar, Olga Murina, Maryou B. Lambros, Valerie G. Brunton, Daniel Durocher, Angelo Agathanggelou, Martin A M Reijns, Jason Moffat, Tatjana Stankovic, Michal Zimmermann, Stephane Angers, Traver Hart, Adeline Fluteau, Michael Aregger, Paul Moss, Morwenna Muir, Wei Yuan, Rachel C. Challis, Matthew Clarke, Andrew P. Jackson, Shankara Paneesha, Johann S. de Bono, Žygimantė Tarnauskaitė

Publikováno v: Zimmermann, M, Murina, O, Reijns, M A M, Agathanggelou, A, Challis, R, Tarnauskaite, Z, Muir, M, Fluteau, A, Aregger, M, McEwan, A, Yuan, W, Clarke, M, Lambros, M B, Paneesha, S, Moss, P, Chandrashekhar, M, Angers, S, Moffat, J, Brunton, V G, Hart, T, de Bono, J, Stankovic, T, Jackson, A P & Durocher, D 2019, ' CRISPR screens identify genomic ribonucleotides as a source of PARP-trapping lesions ', Nature, vol. 559, no. 7713, pp. 285–289 . https://doi.org/10.1038/s41586-018-0291-z

The observation that BRCA1- and BRCA2-deficient cells are sensitive to inhibitors of poly(ADP–ribose) polymerase (PARP) has spurred the development of cancer therapies that use these inhibitors to target deficiencies in homologous recombination. Th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c31459b4e5a8c1168b596ef85f70c55
https://doi.org/10.1038/s41586-018-0291-z