L. Cutler

发表

Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.

C. Dingwall, J. Mosley, P. Rowland, 2009, Bioorganic & medicinal chemistry letters.

Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.

C. Dingwall, J. Mosley, P. Rowland, 2009, Bioorganic & medicinal chemistry letters.

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).

David M. Wilson, P. Bamborough, R. Prinjha, 2012, Bioorganic & medicinal chemistry letters.

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Christophe Simon, P. Bamborough, R. Prinjha, 2014, Journal of medicinal chemistry.

Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.

David M. Wilson, D. Pemberton, Frank T. Coppo, 2012, Bioorganic & medicinal chemistry letters.

Orexin-A, an hypothalamic peptide with analgesic properties

A. A. Parsons, E. Irving, A. Hunter, 2001, Pain.

Inhibition of colonic motility and defecation by RS‐127445 suggests an involvement of the 5‐HT2B receptor in rodent large bowel physiology

S. Summerfield, G. Sanger, L. Cutler, 2009, British journal of pharmacology.

Pharmacokinetics of the novel, high-affinity and selective dopamine D3 receptor antagonist SB-277011 in rat, dog and monkey: in vitro/in vivo correlation and the role of aldehyde oxidase

P. Jeffrey, K. Thewlis, G. Stemp, 2001, Xenobiotica; the fate of foreign compounds in biological systems.

Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.

P. Thomas, Jonathan D Goodacre, Lena Shukla, 2020, Bioorganic & medicinal chemistry letters.

BET Inhibition Improves NASH and Liver Fibrosis

Sarah A. Middleton, Pankaj Agarwal, D. Rajpal, 2018, Scientific Reports.

Oral administration of a potent and selective non‐peptidic BACE‐1 inhibitor decreases β‐cleavage of amyloid precursor protein and amyloid‐β production in vivo

P. Jeffrey, C. Dingwall, E. Demont, 2007 .

Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo.

P. Jeffrey, C. Dingwall, E. Demont, 2007, Journal of neurochemistry.

Development of a P-glycoprotein knockout model in rodents to define species differences in its functional effect at the blood-brain barrier.

P. Jeffrey, L. Cutler, C. Howes, 2006, Journal of pharmaceutical sciences.

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.

R. Prinjha, Baochau Le, O. Barbash, 2014, Blood.

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.

P. Bamborough, R. Prinjha, C. Chung, 2013, Journal of medicinal chemistry.

Improving the in Vitro Prediction of in Vivo Central Nervous System Penetration: Integrating Permeability, P-glycoprotein Efflux, and Free Fractions in Blood and Brain

Phil Jeffrey, Sac-Pham Tang, Scott G Summerfield, 2006, Journal of Pharmacology and Experimental Therapeutics.

Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.

R. Prinjha, P. Soden, C. Chung, 2021, Journal of medicinal chemistry.

Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists.

A. Naylor, L. Cutler, A. Hall, 2008, Bioorganic & medicinal chemistry letters.

Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.

Brian Clarke, Phil Jeffrey, P. Jeffrey, 2008, Journal of medicinal chemistry.

8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.

D. Middlemiss, C. Scott, G. W. Price, 2005, Bioorganic & medicinal chemistry letters.

BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.

C. Dingwall, J. Mosley, P. Rowland, 2010, Bioorganic & medicinal chemistry letters.

Bace-1 Inhibitors Using Novel Edge-to-Face Interaction with Arg-296

C. Howes, C. Dingwall, J. Mosley, 2010 .

Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.

James M. Woolven, P. Bamborough, R. Prinjha, 2020, Journal of medicinal chemistry.

BET Inhibition Improves NASH and Liver Fibrosis

Sarah A. Middleton, Pankaj Agarwal, D. Rajpal, 2018, Scientific Reports.

Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.

C. Dingwall, J. Mosley, P. Rowland, 2009, Bioorganic & medicinal chemistry letters.

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.

R. Prinjha, Baochau Le, O. Barbash, 2014, Blood.