I. Churcher

发表

Lead-oriented synthesis: a new opportunity for synthetic chemistry.

Channa K. Hattotuwagama, A. Nadin, I. Churcher, 2012, Angewandte Chemie.

Catalytic in vivo protein knockdown by small-molecule PROTACs.

I. E. Smith, Marcus Bantscheff, Kristoffer Famm, 2015, Nature chemical biology.

A practical drug discovery project at the undergraduate level.

J. Liddle, M. Fray, D. Coe, 2013, Drug discovery today.

Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2

Aditya R. Thawani, I. E. Smith, Carol A. Capriotti, 2020, Communications Biology.

Structural insights into PROTAC-mediated degradation of Bcl-xL.

F. Jiang, C. Chung, J. Harling, 2020, ACS chemical biology.

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

I. Churcher, 2017, Journal of medicinal chemistry.

Small molecule-mediated protein knockdown as a new approach to drug discovery

I. Churcher, Christopher P Tinworth, Hannah Lithgow, 2016 .

Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.

S. Pickett, C. Chung, C. Jamieson, 2016, Journal of medicinal chemistry.

Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: preparation of (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement.

Y. S. Tang, J. Castro, I. Churcher, 2003, Journal of medicinal chemistry.

Selected Non-steroidal Anti-inflammatory Drugs and Their Derivatives Target γ-Secretase at a Novel Site

A. Nadin, I. Churcher, D. Beher, 2004, Journal of Biological Chemistry.

In Vivo Characterization of Aβ(40) Changes in Brain and Cerebrospinal Fluid Using the Novel γ-Secretase Inhibitor N-[cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the Rat

J. Atack, Michael A. Reilly, J. Best, 2006, Journal of Pharmacology and Experimental Therapeutics.

4-Substituted cyclohexyl sulfones as potent, orally active γ-secretase inhibitors

Euan R. Kay, R. Mortishire-Smith, Michael A. Reilly, 2006 .

Intra- or intercomplex binding to the gamma-secretase enzyme. A model to differentiate inhibitor classes.

I. Churcher, D. Beher, M. Shearman, 2006, The Journal of biological chemistry.

The novel γ secretase inhibitor MRK-560 reduces amyloid plaque deposition without evidence of Notch-related pathology in the Tg 2576 mouse

T. Rosahl, Michael A. Reilly, J. Best, 2006 .

The rise and rise of protein degradation: opportunities and challenges ahead.

A. Testa, I. Churcher, S. Hughes, 2021, Drug discovery today.

A systematic approach to diverse, lead-like scaffolds from α,α-disubstituted amino acids.

Adam Nelson, Daniel J Foley, S. Marsden, 2015, Chemical communications.

A Systematic Approach to Diverse, Lead‐Like Scaffolds from α,α‐Disubstituted Amino Acids.

S. Marsden, Daniel J. Foley, A. Nelson, 2015 .

A unified lead-oriented synthesis of over fifty molecular scaffolds.

Adam Nelson, Mark Dow, David House, 2015, Organic & biomolecular chemistry.

Synthesis and Demonstration of the Biological Relevance of sp3‐rich Scaffolds Distantly Related to Natural Product Frameworks

Adam Nelson, Frank von Delft, Daniel J Foley, 2017, Chemistry.

The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.

S. Pickett, C. Chung, E. Nicodème, 2015, Journal of medicinal chemistry.

Optimization of a Series of RIPK2 PROTACs.

Aditya R. Thawani, I. E. Smith, R. Nagilla, 2021, Journal of medicinal chemistry.

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.

Martin C Fillmore, R. Prinjha, N. Galwey, 2018, ACS chemical biology.

4‐Substituted Cyclohexyl Sulfones as Potent, Orally Active γ‐Secretase Inhibitors.

I. Churcher, 2006 .

γ-Secretase as a Therapeutic Target for the Treatment of Alzheimers Disease

I. Churcher, D. Beher, 2005 .

Sigmatropic Rearrangement of Vinyl Aziridines: Expedient Synthesis of Cyclic Sulfoximines from Chiral Sulfinimines.

José A. Souto, Justine Dutton, W. Lewis, 2016, Angewandte Chemie.

Stereoselective aza-Darzens reactions of tert-butanesulfinimines: convenient access to chiral aziridines.

W. Lewis, I. Churcher, R. Stockman, 2011, Organic & biomolecular chemistry.

Asymmetric synthesis of trisubstituted aziridines via aza-Darzens reaction of chiral sulfinimines.

W. Lewis, I. Churcher, R. Stockman, 2014, Organic letters.

Organic synthesis provides opportunities to transform drug discovery

Anthony Wood, Andrew W. Thomas, David M. Wilson, 2018, Nature Chemistry.

On the utility of S-mesitylsulfinimines for the stereoselective synthesis of chiral amines and aziridines.

D. Macpherson, I. Churcher, R. Stockman, 2011, Chemical communications.

A divergent synthetic approach to diverse molecular scaffolds: assessment of lead-likeness using LLAMA, an open-access computational tool.

Adam Nelson, Ignacio Colomer, Christopher J. Empson, 2016, Chemical communications.

Dimerization of o-hydroxycyclohexadienones related to calicheamicinone: SN2 displacement of the 12α-hydroxyl group

D. Hallett, I. Churcher, P. Magnus, 1999 .

Tau therapeutic strategies for the treatment of Alzheimer's disease.

I. Churcher, 2006, Current topics in medicinal chemistry.

Synthesis of the Enediyne Aglycon (±)-Calicheamicinone

D. Hallett, I. Churcher, P. Magnus, 1998 .

Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2

Aditya R. Thawani, I. E. Smith, M. Bantscheff, 2020, Communications Biology.

A Phenotypic Screening Approach in Cord Blood–Derived Mast Cells to Identify Anti-Inflammatory Compounds

Janet L. Smith, G. Wayne, R. Kaur, 2013, Journal of biomolecular screening.

The Novel γ Secretase Inhibitor N-[cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) Reduces Amyloid Plaque Deposition without Evidence of Notch-Related Pathology in the Tg2576 Mouse

Timothy Harrison, J. Atack, T. Rosahl, 2007, Journal of Pharmacology and Experimental Therapeutics.

Small-molecule modulation of cellular chaperones to treat protein misfolding disorders.

Martin C Fillmore, I. Churcher, Lisa A. Sloan, 2009, Current opinion in drug discovery & development.

Gamma-secretase as a therapeutic target for the treatment of Alzheimer's disease.

I. Churcher, D. Beher, 2005, Current pharmaceutical design.

Synthesis of the potent potassium channel opener Ro 31-6930 via claisen rearrangement and tandem regiocontrolled cyclisation.

R. Dunsdon, I. Churcher, M. Attwood, 1991 .

Synthesis of the Antitumor Agent Aglycon (±)-Calicheamicinone Using an o-Quinone Monoketal Strategy

D. Hallett, I. Churcher, P. Magnus, 1998 .

Synthesis of the Antitumor Agent Aglycon (.+-.)-Calicheamicinone Using an o-Quinone Monoketal Strategy.

D. Hallett, I. Churcher, P. Magnus, 2010 .

4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.

R. Mortishire-Smith, Michael A. Reilly, E. Kay, 2006, Bioorganic & medicinal chemistry letters.

gamma-Secretase as a target for drug intervention in Alzheimer's disease.

I. Churcher, D. Beher, T. Harrison, 2004, Current opinion in drug discovery & development.

A new series of potent benzodiazepine γ-secretase inhibitors

I. Churcher, J. W. Butcher, H. Lewis, 2003 .

A new series of potent benzodiazepine gamma-secretase inhibitors.

I. Churcher, J. W. Butcher, H. Lewis, 2003, Bioorganic & Medicinal Chemistry Letters.