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Ian Churcher
Researcher at GlaxoSmithKline
Publications - 69
Citations - 4154
Ian Churcher is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Gamma secretase & Amyloid precursor protein. The author has an hindex of 27, co-authored 69 publications receiving 3283 citations. Previous affiliations of Ian Churcher include University of Texas at Austin & University of Hertfordshire.
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Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson,Alina Mares,Ian Edward David Smith,Ko Eunhwa,Sebastien Andre Campos,Afjal Hussain Miah,Katie E Mulholland,Natasha Routly,Dennis L. Buckley,Jeffrey L. Gustafson,Nico Zinn,Paola Grandi,Satoko Shimamura,Giovanna Bergamini,Maria Faelth-Savitski,Marcus Bantscheff,Carly S. Cox,Deborah A. Gordon,Ryan R. Willard,John J. Flanagan,Linda N. Casillas,Bartholomew J. Votta,Willem den Besten,Kristoffer Famm,Laurens Kruidenier,Paul S. Carter,John D. Harling,Ian Churcher,Craig M. Crews +28 more
TL;DR: Major improvements to the proteolysis targeting chimeras (PROTACs) method are described, a chemical knockdown strategy in which a heterobifunctional molecule recruits a specific protein target to an E3 ubiquitin ligase, resulting in the target's ubiquitination and degradation.
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Organic synthesis provides opportunities to transform drug discovery
David C. Blakemore,Luis Castro,Ian Churcher,David C. Rees,Andrew Thomas,David Matthew Wilson,Anthony Wood +6 more
TL;DR: This Perspective highlights some of the most pressing challenges to be overcome from the industrial viewpoint — such as the development of reactions tolerating specific functionalities — and encourages stronger industry–academia relationships.
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Lead-oriented synthesis: a new opportunity for synthetic chemistry.
TL;DR: Data is presented suggesting that much synthetic methodology is unintentionally predisposed to producing molecules with poorer drug-like properties, which may have ramifications to the early hit- and lead-finding phases of the drug discovery process when larger numbers of compounds from array techniques are prepared.
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Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?
TL;DR: The brief history of the field is surveyed from a drug discovery perspective with a focus on the key advances in knowledge which have led to the definition and exemplification of protein degradation concepts and their resulting applications to medicine discovery.
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Selected Non-steroidal Anti-inflammatory Drugs and Their Derivatives Target γ-Secretase at a Novel Site EVIDENCE FOR AN ALLOSTERIC MECHANISM
Dirk Beher,Earl E. Clarke,Jonathan D.J. Wrigley,Agnes C.L. Martin,Alan Nadin,Ian Churcher,Mark S. Shearman +6 more
TL;DR: It is demonstrated that in cell-free systems the mode of action of selected NSAIDs and their derivatives, depending on the concentrations used, can either be classified as modulatory or inhibitory.