R. V. van Montfort

发表

Structure-based drug design: aiming for a perfect fit

R. V. van Montfort, P. Workman, 2017, Essays in biochemistry.

Structure-based design of molecular cancer therapeutics.

R. V. van Montfort, P. Workman, 2009, Trends in biotechnology.

Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.

Ian Collins, C. E. Allen, Michelle D Garrett, 2010, Bioorganic & medicinal chemistry letters.

Application of fragment screening and fragment linking to the discovery of novel thrombin inhibitors.

Gianni Chessari, Chris Abell, Christopher W Murray, 2006, Journal of medicinal chemistry.

Analysis of water patterns in protein kinase binding sites

Caterina Barillari, Julian Blagg, Anna L. Duncan, 2011, Proteins.

Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.

R. V. van Montfort, K. Boxall, G. Aherne, 2011, Journal of medicinal chemistry.

Nucleotide sequence and X-ray structure of cyclodextrin glycosyltransferase from Bacillus circulans strain 251 in a maltose-dependent crystal form.

L. Dijkhuizen, K. H. Kalk, B. Dijkstra, 1994, Journal of molecular biology.

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.

R. V. van Montfort, A. Faisal, N. Cronin, 2016, Journal of medicinal chemistry.

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance.

R. V. van Montfort, P. Workman, A. Faisal, 2015, Cancer research.

Mutations in the DNA methyltransferase gene DNMT3A cause an overgrowth syndrome with intellectual disability.

S. Seal, N. Rahman, D. Baralle, 2014, Nature genetics.

Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition

R. V. van Montfort, R. Bayliss, D. Fearon, 2018, Bioorganic & medicinal chemistry.

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.

Privileged Structures and Polypharmacology within and between Protein Families

R. V. van Montfort, P. Workman, Y. Le Bihan, 2018, ACS medicinal chemistry letters.

An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

R. V. van Montfort, Y. Le Bihan, Marcella Widya, 2017, Angewandte Chemie.

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

S. Robinson, R. V. van Montfort, M. Lamers, 2016, Journal of medicinal chemistry.

Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.

C. E. Allen, R. V. van Montfort, J. Caldwell, 2013, Bioorganic & medicinal chemistry.

Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70

R. V. van Montfort, P. Workman, I. Collins, 2016, Journal of medicinal chemistry.

Mutations in the PP2A regulatory subunit B family genes PPP2R5B, PPP2R5C and PPP2R5D cause human overgrowth

N. Rahman, A. Renwick, Elise Ruark, 2015, Human molecular genetics.

Implementing a method for engineering multivalency to substantially enhance binding of clinical trial anti-SARS-CoV-2 antibodies to wildtype spike and variants of concern proteins

R. V. van Montfort, T. Rabbitts, Ami Miller, 2021, Scientific Reports.

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Journal of medicinal chemistry.

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Journal of medicinal chemistry.

Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2021, Journal of medicinal chemistry.

Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1

R. V. van Montfort, F. Raynaud, A. Hayes, 2021, Bioorganic & medicinal chemistry letters.

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Scientific Reports.

Synthesis of a Ribose‐Incorporating Medium Ring Scaffold via a Challenging Ring‐Closing Metathesis Reaction

R. V. van Montfort, N. Cronin, J. Caldwell, 2016, European journal of organic chemistry.

A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms

Ian Collins, Isaac M. Westwood, Paul Workman, 2016, Scientific Reports.

Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization†

Caterina Barillari, Ian Collins, Samantha Burns, 2010, Journal of medicinal chemistry.

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

R. V. van Montfort, P. Workman, R. Griffin, 2013, Oncotarget.

Drugging the PI3 kinome: from chemical tools to drugs in the clinic.

Paul Workman, R. V. van Montfort, P. Workman, 2010, Cancer research.

Structure and function of the small heat shock protein/alpha-crystallin family of molecular chaperones.

R. V. van Montfort, E. Vierling, C. Slingsby, 2001, Advances in protein chemistry.

Mutations in the DNA methyltransferase gene, DNMT3A, cause an overgrowth syndrome with intellectual disability

Katrina Tatton-Brown, Nazneen Rahman, Elise Ruark, 2014, Nature Genetics.

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen

R. V. van Montfort, P. Workman, R. T. te Poele, 2016, Journal of medicinal chemistry.

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2020, Journal of medicinal chemistry.

Insights into the Conformational Variability and Regulation of Human Nek2 Kinase

Mark W. Richards, Andrew M. Fry, Richard Bayliss, 2009, Journal of molecular biology.

EML4-ALK fusions: propelling cancer but creating exploitable chaperone dependence.

R. V. van Montfort, P. Workman, 2014, Cancer discovery.

The structure of the Escherichia coli phosphotransferase IIAmannitol reveals a novel fold with two conformations of the active site.

K. H. Kalk, G. Robillard, B. Dijkstra, 1998, Structure.

Pan RAS-binding compounds selected from a chemical library by inhibiting interaction between RAS and a reduced affinity intracellular antibody

R. V. van Montfort, T. Rabbitts, Ami Miller, 2021, Scientific Reports.

Structural and functional characterisation of human RNA helicase DHX8 provides insights into the mechanism of RNA-stimulated ADP release.

R. V. van Montfort, P. Workman, Y. Le Bihan, 2019, The Biochemical journal.

Dissecting mechanisms of resistance to targeted drug combination therapy in human colorectal cancer

Paul Workman, Rosemary Burke, R. V. van Montfort, 2019, Oncogene.

Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing

Gary Box, Ian Collins, Isaac M. Westwood, 2011, Journal of medicinal chemistry.

Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.

F. Holding, V. Berdini, M. Tortorici, 2016, ACS chemical biology.

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

R. V. van Montfort, A. Faisal, F. Raynaud, 2019, Molecular Cancer Therapeutics.

Fragment-Based Screening Maps Inhibitor Interactions in the ATP-Binding Site of Checkpoint Kinase 2

Ian Collins, Isaac M. Westwood, Nathan Brown, 2013, PloS one.

Identification of inhibitors of checkpoint kinase 1 through template screening.

Ian Collins, Samantha Burns, David Williams, 2009, Journal of medicinal chemistry.

The structure of an energy-coupling protein from bacteria, IIBcellobiose, reveals similarity to eukaryotic protein tyrosine phosphatases.

K. H. Kalk, M. Saier, G. Robillard, 1997, Structure.

PI(3) kinases: revealing the delta lady.

R. V. van Montfort, P. Workman, 2010, Nature chemical biology.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)

R. V. van Montfort, A. Faisal, N. Cronin, 2018, Journal of medicinal chemistry.

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.

The functional importance of structural differences between the mannitol‐specific IIAmannitol and the regulatory IIAnitrogen

B. Dijkstra, R. V. van Montfort, 1998, Protein science : a publication of the Protein Society.

Crystal structure of eta-crystallin: adaptation of a class 1 aldehyde dehydrogenase for a new role in the eye lens.

R. V. van Montfort, A. Purkiss, G. Wistow, 2003, Biochemistry.

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2023, Journal of medicinal chemistry.

Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70

Alan M. Jones, R. V. van Montfort, Y. Le Bihan, 2022, Molecules.

Identification of Autophosphorylation Inhibitors of the Inositol-Requiring Enzyme 1 Alpha (IRE1α) by High-Throughput Screening Using a DELFIA Assay

G. Morgan, R. V. van Montfort, A. Mirza, 2013, Journal of biomolecular screening.

Crystal structure of truncated human βB1‐crystallin

R. V. van Montfort, N. Lubsen, C. Slingsby, 2003 .

iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

T. Westbrook, R. V. van Montfort, Y. Le Bihan, 2023, iScience.

Determination of Ligand-Binding Affinity (Kd) Using Transverse Relaxation Rate (R2) in the Ligand-Observed 1H NMR Experiment and Applications to Fragment-Based Drug Discovery.

Benjamin R Bellenie, R. V. van Montfort, A. Mirza, 2023, Journal of medicinal chemistry.

Unveiling the secrets of the ancestral PI3 kinase Vps34.

R. V. van Montfort, P. Workman, 2010, Cancer cell.

Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein–ligand crystallography

R. V. van Montfort, J. Blagg, I. Westwood, 2012, Bioorganic & medicinal chemistry.

R. V. van Montfort, K. Boxall, G. Aherne, 2016, Journal of medicinal chemistry.

Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates

M. Tortorici, R. V. van Montfort, A. Mirza, 2018, ACS chemical biology.

Identification of inhibitors of checkpoint kinase 1 through template screening.

R. V. van Montfort, M. Walton, K. Boxall, 2009, Journal of medicinal chemistry.

Crystal structure of truncated human betaB1-crystallin.

R. V. van Montfort, N. Lubsen, C. Slingsby, 2004, Protein science : a publication of the Protein Society.