B. Atrash

发表

On the rational design of renin inhibitors: X-ray studies of aspartic proteinases complexed with transition-state analogues.

T L Blundell, M Szelke, J Cooper, 1987, Biochemistry.

High resolution X-ray analyses of renin inhibitor-aspartic proteinase complexes

T. L. Blundell, B. L. Sibanda, L. H. Pearl, 1987, Nature.

Inhibitors of aspartic proteinases and their relevance to the design of antihypertensive agents.

B. L. Sibanda, T. Blundell, J. Cooper, 1987, Biochemical Society transactions.

Design and synthesis of thrombin inhibitors

J. Deinum, M. Szelke, D. M. Jones, 1995, Letters in Peptide Science.

Inhibitors of thrombin containing arginine ketone derivatives

J. Deinum, M. Szelke, D. M. Jones, 1995 .

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

P. Workman, A. Faisal, M. Valenti, 2012, Leukemia.

4-cyanothiazolidides as very potent, stable inhibitors of dipeptidyl peptidase IV

M. Szelke, D. M. Jones, B. Atrash, 1996 .

The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo

S. Robinson, P. Workman, A. Faisal, 2011, Molecular Cancer Therapeutics.

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

G. F. Ruda, O. Fedorov, C. Bountra, 2016, Journal of medicinal chemistry.

New inhibitors of human renin tested in vitro and in vivo in the anaesthetized baboon.

J. Morton, D. M. Jones, B. Atrash, 1983, Journal of hypertension.

Crystallographic Studies of Reduced Bond Inhibitors Complexed with an Aspartic Proteinase

T. Blundell, L. Pearl, J. Cooper, 1987, Journal of cardiovascular pharmacology.

A transition-state analogue inhibitor of human renin (H.261): test in vitro and a comparison with captopril in the anaesthetized baboon.

M. Szelke, D. M. Jones, B. Atrash, 1985, Journal of hypertension.

Optimization of imidazo [4, 5-b] pyridine-based kinase inhibitors: identification of a dual FLT3/aur

Gary Box, Nathan Brown, Julian Blagg, 2012 .

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.

P. Workman, A. Faisal, R. Bayliss, 2010, Journal of medicinal chemistry.

Abstract B74: The dual FLT3-Aurora inhibitor CCT241736 overcomes resistance to selective FLT3 inhibition driven by FLT3 ligand and FLT3 point mutations in acute myeloid leukemia.

P. Workman, A. Faisal, M. Valenti, 2011 .

Synthesis of resorcinylic macrocycles related to radicicol via ring-closing metathesis

P. Workman, E. McDonald, B. Atrash, 2006 .

Development of synthetic routes to macrocyclic compounds based on the HSP90 inhibitor radicicol

P. Workman, E. McDonald, B. Atrash, 2006 .

Assessing histone demethylase inhibitors in cells: lessons learned

G. F. Ruda, O. Fedorov, C. Bountra, 2017, Epigenetics & Chromatin.

Renin inhibitors: their use in understanding the role of angiotensin II as a pressor hormone.

J. Morton, M. Szelke, D. M. Jones, 1985, Journal of cardiovascular pharmacology.

Thrombin inhibitors based on ketone derivatives of arginine and lysine.

H. Ryder, M. Szelke, D. M. Jones, 1995, Journal of enzyme inhibition.

Potent new inhibitors of human renin

M. Szelke, D. M. Jones, B. Atrash, 1982, Nature.

Aurora Isoform Selectivity: Design and Synthesis of Imidazo[4,5-b]pyridine Derivatives as Highly Selective Inhibitors of Aurora-A Kinase in Cells

P. Workman, A. Faisal, K. Boxall, 2013, Journal of medicinal chemistry.

Reusable resin plug-bound palladium catalysts for organic synthesis

M. Bradley, J. Reader, B. Atrash, 2003 .

Revolutionizing Resin Handling for Combinatorial Synthesis.

M. Bradley, J. Reader, B. Atrash, 2001, Angewandte Chemie.

A kinetic study of phosphinic carboxylic mixed anhydrides

B. Atrash, R. Ramage, D. Hopton, 1985 .

Evaluation of phosphinic acid derivatives as reagents for amine protection in peptide synthesis

B. Atrash, R. Ramage, D. Hopton, 1985 .

A new bio-compatible pH cleavable linker for solid-phase synthesis of a squalamine analogue

M. Bradley, B. Atrash, B. Chitkul, 2001 .

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

A. Faisal, R. Bayliss, Chongbo Sun, 2010, Bioorganic & medicinal chemistry letters.

Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.

Paul Workman, Peter M Fischer, Wayne Jackson, 2011, Bioorganic & medicinal chemistry.

Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer

P. Workman, D. Zheleva, D. Blake, 2020, PloS one.

Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design.

R. Bayliss, C. Dodson, J. Blagg, 2010, The Biochemical journal.

Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution

Y. Le Bihan, Alan T. Henley, F. Raynaud, 2016, Xenobiotica; the fate of foreign compounds in biological systems.

Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

Isaac M. Westwood, Julian Blagg, Florence I. Raynaud, 2013, Journal of medicinal chemistry.

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

G. F. Ruda, O. Fedorov, O. Rossanese, 2019, European journal of medicinal chemistry.

X-ray-crystallographic studies of complexes of pepstatin A and a statine-containing human renin inhibitor with endothiapepsin.

T. Blundell, J. Cooper, B. Veerapandian, 1993, The Biochemical journal.

MOARF, an Integrated Workflow for Multiobjective Optimization: Implementation, Synthesis, and Biological Evaluation

Nathan Brown, Julian Blagg, Nicholas C. Firth, 2015, J. Chem. Inf. Model..

Assessing histone demethylase inhibitors in cells: lessons learned

G. F. Ruda, O. Fedorov, C. Bountra, 2017, Epigenetics & Chromatin.

2-cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV

Paul D. Jenkins, Butrus Atrash, M. Szelke, 1996 .

Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species

A. Faisal, F. Raynaud, A. Hayes, 2019, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

A pH cleavable linker for zone diffusion assays and single bead solution screens in combinatorial chemistry

M. Bradley, B. Atrash, 1997 .

Dual Inhibition of Aurora and FLT3 Kinases by CCT137690: A Novel Treatment Strategy Against FLT3-ITD Positive AML In Vitro and In Vivo

P. Workman, A. Faisal, M. Valenti, 2010 .

Aurora Isoform Selectivity: Design and Synthesis of Imidazo [4, 5-b] pyridine Derivatives as Highly

A. Faisal, K. Boxall, Nathan Brown, 2013 .

Resistance to Selective FLT3 Inhibitors, Driven by FLT3 Ligand and FLT3 Point Mutations, Can Be Overcome with the Dual FLT3-Aurora Kinase Inhibitor CCT241736,

P. Workman, A. Faisal, M. Valenti, 2011 .

Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia

M. Valenti, A. K. de Haven Brandon, Alan T. Henley, 2012, Journal of Medicinal Chemistry.

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

P. Workman, A. Faisal, M. Valenti, 2012, Leukemia.