N
Nicholas C. O. Tomkinson
Researcher at University of Strathclyde
Publications - 165
Citations - 3934
Nicholas C. O. Tomkinson is an academic researcher from University of Strathclyde. The author has contributed to research in topics: Catalysis & Dihydroxylation. The author has an hindex of 31, co-authored 156 publications receiving 3366 citations. Previous affiliations of Nicholas C. O. Tomkinson include Dartmouth College & Research Triangle Park.
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Journal ArticleDOI
The Pregnane X Receptor: A Promiscuous Xenobiotic Receptor That Has Diverged during Evolution
Stacey A. Jones,Linda B. Moore,Jennifer L. Shenk,G. Bruce Wisely,Geraldine A. Hamilton,David D. McKee,Nicholas C. O. Tomkinson,Edward L. LeCluyse,Millard H. Lambert,Timothy M. Willson,Steven A. Kliewer,John T. Moore +11 more
TL;DR: In this paper, the mouse and human pregnane X receptor (PXR) were shown to be activated by compounds that induce CYP3A expression in primary hepatocytes, and the authors reported the cloning and characterization of PXR from these two species, with the rabbit, rat and human receptors sharing only approximately 80% amino acid identity in their ligand-binding domains.
Journal ArticleDOI
The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution
Stacey A. Jones,Linda B. Moore,Jennifer L. Shenk,G. Bruce Wisely,Geraldine A. Hamilton,David D. McKee,Nicholas C. O. Tomkinson,Edward L. LeCluyse,Millard H. Lambert,Timothy M. Willson,Steven A. Kliewer,John T. Moore +11 more
TL;DR: In this paper, the mouse and human pregnane X receptor (PXR) were shown to be activated by compounds that induce CYP3A expression in primary hepatocytes, and the authors reported the cloning and characterization of PXR from these two species, with the rabbit, rat and human receptors sharing only approximately 80% amino acid identity in their ligand-binding domains.
Journal ArticleDOI
A cluster of palmitoylated cysteines are essential for aggregation of cysteine-string protein mutants that cause neuronal ceroid lipofuscinosis
Cinta Diez-Ardanuy,Jennifer Greaves,Kevin R. Munro,Nicholas C. O. Tomkinson,Luke H. Chamberlain +4 more
TL;DR: Interestingly, palmitoylated monomers of ANCL CSP α mutants were shown to be short-lived compared with wild-type CSPα, suggesting that the mutants either have a faster rate of depalmitoylation or that they are consumed in a time-dependent manner into high molecular weight aggregates.
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Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
Natalie Hope Theodoulou,Paul Bamborough,Andrew J. Bannister,Isabelle Becher,Rino A. Bit,Ka Hing Che,Chun-wa Chung,Antje Dittmann,Gerard Drewes,David H. Drewry,Laurie J. Gordon,Paola Grandi,Melanie Leveridge,Matthew J Lindon,Anne-Marie Michon,Judit Molnar,Samuel Robson,Nicholas C. O. Tomkinson,Tony Kouzarides,Rab K. Prinjha,Philip G. Humphreys +20 more
TL;DR: I-BRD9 represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromidomain-containing protein 7 (BRD7).
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A public-private partnership to unlock the untargeted kinome
Stefan Knapp,Paulo Arruda,Julian Blagg,Stephen K. Burley,David H. Drewry,Aled M. Edwards,Doriano Fabbro,Paul Gillespie,Nathanael S. Gray,Bernhard Kuster,Karen Lackey,Paulo Mazzafera,Nicholas C. O. Tomkinson,Timothy M. Willson,Paul Workman,William J. Zuercher +15 more
TL;DR: A large-scale public-private partnership is proposed as a new approach that offers economies of scale, minimized redundancy and sharing of risk and cost.