C
Christopher P. Tinworth
Researcher at GlaxoSmithKline
Publications - 9
Citations - 272
Christopher P. Tinworth is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Small molecule & Protein degradation. The author has an hindex of 5, co-authored 7 publications receiving 148 citations. Previous affiliations of Christopher P. Tinworth include University of Strathclyde.
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Journal ArticleDOI
PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase Is Inhibited by Covalent Binding.
Christopher P. Tinworth,Hannah Lithgow,Lars Dittus,Zuni I. Bassi,Sophie E. Hughes,Marcel Muelbaier,Han Dai,Ian Edward David Smith,William J. Kerr,Glenn A. Burley,Marcus Bantscheff,John D. Harling +11 more
TL;DR: Proteomics analysis determined that the use of a covalent bound PROTAC did not result in the degradation of covalently bound targets, while degradation was observed for some reversibly bound targets.
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Facts, Patterns, and Principles in Drug Discovery: Appraising the Rule of 5 with Measured Physicochemical Data.
TL;DR: This perspective explores the impact of various physicochemical descriptors and contemporary lipophilicity measurements on permeability and solubility, showing that the distribution coefficient log D7.4 (rather than log P) is the most impactful parameter.
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Structural Insights into PROTAC-Mediated Degradation of Bcl-xL
Chun-wa Chung,Han Dai,Esther Fernández,Christopher P. Tinworth,Ian Churcher,Jenni Cryan,Jane Denyer,John D. Harling,Agnieszka Konopacka,Markus A. Queisser,Christopher J. Tame,Gillian F. Watt,Fan Jiang,Dongming Qian,Andrew B. Benowitz +14 more
TL;DR: The design, characterization and X-ray structure of a VHL E3 ligase-recruiting Bcl-xL PROTAC degrader reveals an extensive network of neo-interactions, between the E3ligase and the target protein, and between non-cognate parts of the PROTAC and partner proteins.
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Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.
John Liddle,Jonathan P. Hutchinson,Semra Kitchen,Paul Rowland,Margarete Neu,Ted Cecconie,Duncan S. Holmes,Emma J. Jones,Justyna Korczynska,Despoina Koumantou,Jonathan D Lea,Leng Nickels,Michelle Pemberton,Alex Phillipou,Jessica L. Schneck,Hester Sheehan,Christopher P. Tinworth,Iain Uings,Justyna Wojno-Picon,Robert J. Young,Efstratios Stratikos +20 more
TL;DR: Crystallographic analysis confirmed that the compound targets the regulatory site of the enzyme that normally binds the C-terminus of the peptide substrate, which constitutes a novel starting point for the development of selective ERAP1 modulators that have potential for further clinical development.
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Small molecule-mediated protein knockdown as a new approach to drug discovery
TL;DR: Some of the recent advances in the design of small molecule chemical inducers of protein degradation are surveyed and the potential challenges that will need to be overcome in order to allow clinical evaluation are surveyed.