Publications by authors named "Pascal D Fortin"

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Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Andreas Varkaris, Ermira Pazolli, Hakan Gunaydin, Qi Wang, Levi Pierce, Pascal D Fortin

Cancer Discov· February 2024

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Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.
Matthew J LaMarche, Michael Acker, Andreea Argintaru, Daniel Bauer, Julie Boisclair, Pascal D Fortin

J Med Chem· November 2020

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Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Julian R Levell, Thomas Caferro, Gregg Chenail, Ina Dix, Julia Dooley, Pascal D Fortin

ACS Med Chem Lett· February 2017

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Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor.
Jorge Garcia Fortanet, Christine Hiu-Tung Chen, Ying-Nan P Chen, Zhouliang Chen, Zhan Deng, Pascal D Fortin

J Med Chem· September 2016

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Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.
Ying-Nan P Chen, Matthew J LaMarche, Ho Man Chan, Peter Fekkes, Jorge Garcia-Fortanet, Pascal D Fortin

Nature· July 2016

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Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2.
Jonathan R LaRochelle, Michelle Fodor, Xiang Xu, Izabela Durzynska, Lixin Fan, Pascal D Fortin

Biochemistry· April 2016

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The novolactone natural product disrupts the allosteric regulation of Hsp70.
A Quamrul Hassan, Christina A Kirby, Wenlai Zhou, Tim Schuhmann, Roman Kityk, Pascal D Fortin

Chem Biol· January 2015

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Enzyme-dependent lysine deprotonation in EZH2 catalysis.
D Randal Kipp, Christopher M Quinn, Pascal D Fortin

Biochemistry· October 2013

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Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.
Michael D Shultz, Dyuti Majumdar, Donovan N Chin, Pascal D Fortin, Yun Feng

J Med Chem· September 2013

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Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.
Michael D Shultz, Atwood K Cheung, Christina A Kirby, Brant Firestone, Jianmei Fan, Pascal D Fortin

J Med Chem· August 2013

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[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.
Michael D Shultz, Christina A Kirby, Travis Stams, Donovan N Chin, Jutta Blank, Pascal D Fortin

J Med Chem· February 2012

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beta-Hydroxylation of the aspartyl residue in the phytotoxin syringomycin E: characterization of two candidate hydroxylases AspH and SyrP in Pseudomonas syringae.
Gitanjali M Singh, Pascal D Fortin, Alexander Koglin, Christopher T Walsh

Biochemistry· October 2008

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Gatekeeping versus promiscuity in the early stages of the andrimid biosynthetic assembly line.
Nathan A Magarvey, Pascal D Fortin, Paul M Thomas, Neil L Kelleher, Christopher T Walsh

ACS Chem Biol· September 2008

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Andrimid producers encode an acetyl-CoA carboxyltransferase subunit resistant to the action of the antibiotic.
Xinyu Liu, Pascal D Fortin, Christopher T Walsh

Proc Natl Acad Sci U S A· September 2008

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A transglutaminase homologue as a condensation catalyst in antibiotic assembly lines.
Pascal D Fortin, Christopher T Walsh, Nathan A Magarvey

Nature· August 2007

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Characterization of a C-C bond hydrolase from Sphingomonas wittichii RW1 with novel specificities towards polychlorinated biphenyl metabolites.
Stephen Y K Seah, Jiyuan Ke, Geoffroy Denis, Geoff P Horsman, Pascal D Fortin

J Bacteriol· June 2007

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FenF: servicing the Mycosubtilin synthetase assembly line in trans.
Zachary D Aron, Pascal D Fortin, Christopher T Calderone, Christopher T Walsh

Chembiochem· April 2007

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Structures of ternary complexes of BphK, a bacterial glutathione S-transferase that reductively dechlorinates polychlorinated biphenyl metabolites.
Elitza I Tocheva, Pascal D Fortin, Lindsay D Eltis, Michael E P Murphy

J Biol Chem· October 2006

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A glutathione S-transferase catalyzes the dehalogenation of inhibitory metabolites of polychlorinated biphenyls.
Pascal D Fortin, Geoff P Horsman, Hao M Yang, Lindsay D Eltis

J Bacteriol· June 2006

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Molecular basis for the substrate selectivity of bicyclic and monocyclic extradiol dioxygenases.
Frédéric H Vaillancourt, Pascal D Fortin, Geneviève Labbé, Nathalie M Drouin, Zamil Karim

Biochem Biophys Res Commun· December 2005

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Directed evolution of a ring-cleaving dioxygenase for polychlorinated biphenyl degradation.
Pascal D Fortin, Iain MacPherson, David B Neau, Jeffrey T Bolin, Lindsay D Eltis

J Biol Chem· December 2005

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Evolutionarily divergent extradiol dioxygenases possess higher specificities for polychlorinated biphenyl metabolites.
Pascal D Fortin, Andy T-F Lo, María-Amparo Haro, Stefan R Kaschabek, Walter Reineke

J Bacteriol· January 2005

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Synthesis and evaluation of keto-glutamine analogues as potent inhibitors of severe acute respiratory syndrome 3CLpro.
Rajendra P Jain, Hanna I Pettersson, Jianmin Zhang, Katherine D Aull, Pascal D Fortin

J Med Chem· December 2004

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High-throughput screening identifies inhibitors of the SARS coronavirus main proteinase.
Jan E Blanchard, Nadine H Elowe, Carly Huitema, Pascal D Fortin, Jonathan D Cechetto

Chem Biol· October 2004

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The mechanism-based inactivation of 2,3-dihydroxybiphenyl 1,2-dioxygenase by catecholic substrates.
Frederic H Vaillancourt, Genevieve Labbe, Nathalie M Drouin, Pascal D Fortin, Lindsay D Eltis

J Biol Chem· January 2002

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