T. Heightman

发表

Selective inhibition of BET bromodomains

William B. Smith, S. Knapp, M. McKeown, 2010, Nature.

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.

S. Knapp, O. Fedorov, P. Brennan, 2013, MedChemComm.

Development of a solid-phase 'asymmetric resin-capture-release' process: application of an ephedrine chiral resin in an approach to gamma-butyrolactones.

T. Heightman, D. Procter, N. Kerrigan, 2004, Organic & biomolecular chemistry.

Click JAHAs: Conformationally restricted ferrocene-based histone deacetylase inhibitors

J. Bradner, G. Packham, Jahangir Amin, 2012 .

Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors

J. Bradner, G. Packham, Jahangir Amin, 2011, ACS medicinal chemistry letters.

In-gel activity-based protein profiling of a clickable covalent ERK1/2 inhibitor.

F. Holding, M. O’Reilly, T. Heightman, 2016, Molecular bioSystems.

SB‐272183, a selective 5‐HT1A, 5‐HT1B and 5‐HT1D receptor antagonist in native tissue

C. Davies, D. Middlemiss, C. Scott, 2001, British journal of pharmacology.

Fragment-based drug discovery: opportunities for organic synthesis

Richard J. Hall, C. Murray, T. Heightman, 2020, RSC medicinal chemistry.

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

Chris Abell, Stefan Knapp, Frank von Delft, 2013, Journal of medicinal chemistry.

Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).

G. Chessari, P. Williams, E. Chiarparin, 2017, Journal of medicinal chemistry.

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

A. Jadhav, A. Simeonov, R. Klose, 2010, PloS one.

Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe

P. Nordlund, O. Surova, M. O’Reilly, 2019 .

Visualization of Endogenous ERK1/2 in Cells with a Bioorthogonal Covalent Probe.

S. Cook, S. Meloche, Rebecca H. Gilley, 2017, Bioconjugate chemistry.

Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c8sc04789h

S. Ley, T. Heightman, Christopher N. Johnson, 2018, Chemical science.

Synthesis of Fused Triazoles as Probes for the Active Site of Retaining β‐Glycosidases: From Which Direction Is the Glycoside Protonated?

A. Vasella, T. Heightman, M. Locatelli, 1996 .

Application of an ephedrine chiral linker in a solid-phase, 'asymmetric catch-release' approach to gamma-butyrolactones.

T. Heightman, D. Procter, N. Kerrigan, 2003, Chemical communications.

2. G-Protein-Coupled Receptors

T. Heightman, S. Garland, 2008 .

Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates.

T. Heightman, C. Schofield, A. Tumber, 2011, Organic & biomolecular chemistry.

Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition.

J. Lunec, J. Castro, S. Wedge, 2018, Bioconjugate chemistry.

Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.

S. Bromidge, T. Heightman, D. F. Corbett, 2005, Bioorganic & medicinal chemistry letters.

Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.

K. Kondo, A. Woolford, T. Heightman, 2022, ACS medicinal chemistry letters.

A structural view of the action of Escherichia coli (lacZ) beta-galactosidase.

B. Matthews, S. Withers, J. McCarter, 2001, Biochemistry.

The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.

Jackie S. Scott, A. Muir, G. Sanger, 2009, Bioorganic & medicinal chemistry letters.

Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.

A. Muir, Benjamin R Bellenie, G. Sanger, 2009, Bioorganic & medicinal chemistry letters.

Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.

Michael A. Briggs, A. Muir, G. Sanger, 2008, Bioorganic & medicinal chemistry letters.

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

S. Knapp, O. Fedorov, B. Marsden, 2011, Journal of medicinal chemistry.

The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.

Michael A. Briggs, G. Macdonald, G. Sanger, 2008, Bioorganic & medicinal chemistry letters.

Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.

S. Dowell, K. Philpott, T. Heightman, 2011, Journal of medicinal chemistry.

Enantiopure bicyclic piperidinones: stereoselectivity in lactam enolate alkylations.

T. Heightman, M. Moloney, S. Hermitage, 2004, Organic & biomolecular chemistry.

INHIBITION OF GLYCOSIDASES BY LACTAM OXIMES : INFLUENCE OF THE AGLYCON IN DISACCHARIDE ANALOGUES

A. Vasella, T. Heightman, S. Vonhoff, 1998 .

A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation–π Interaction**

Stefan Knapp, Robert S Paton, Susanne Müller, 2014, Angewandte Chemie.

Recent Insights into Inhibition, Structure, and Mechanism of Configuration-Retaining Glycosidases.

A. Vasella, T. Heightman, Tom D Heightman, 1999, Angewandte Chemie.

Synthesis of Galactose‐ and N‐Acetylglucosamine‐Derived Tetrazoles and their evaluation as β‐glycosidase inhibitors

A. Vasella, T. Heightman, P. Ermert, 1995 .

Isoxazole‐Derived Amino Acids are Bromodomain‐Binding Acetyl‐Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3

T. Heightman, D. Hewings, Timothy P. C. Rooney, 2016, Angewandte Chemie.

Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.

Jackie S. Scott, Alan Wise, A. Muir, 2007, Bioorganic & medicinal chemistry letters.

CONVENIENT PREPARATIONS OF RACEMIC AND ENANTIOPURE METHYL 6-OXOPIPECOLATE

T. Heightman, M. Moloney, S. Hermitage, 1996 .

Animal models of epigenetic regulation in neuropsychiatric disorders.

C. Bountra, U. Oppermann, T. Heightman, 2011, Current topics in behavioral neurosciences.

Nonenzymatic biotinylation of histone H2A

D. Schriemer, S. Healy, T. Heightman, 2009, Protein science : a publication of the Protein Society.

Stereospecific α-Deprotonation of N-ProtectedAziridines

T. Heightman, D. M. Hodgson, Steven P Hughes, 2008 .

Terminal aziridines by alpha-deprotonation/electrophile trapping of N-protected aziridine.

T. Heightman, D. M. Hodgson, Steven P Hughes, 2008, Organic letters.

Cooperative Interactions of the Catalytic Nucleophile and the Catalytic Acid in the Inhibition of β-Glycosidases. Calculations and their validation by comparative kinetic and structural studies of the inhibition of glycogen phosphorylase b

Spyros E. Zographos, Katerina E. Tsitsanou, S. Zographos, 1998 .

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.

H. Willems, G. Saxty, T. Davies, 2016, Journal of medicinal chemistry.

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

T. Heightman, Christopher N. Johnson, Honorine Lebraud, 2016, ACS central science.

A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.

S. Schreiber, U. Oppermann, S. Kubicek, 2011, Journal of the American Chemical Society.

BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones

D. Reinberg, B. Garcia, J. O’Shea, 2014, Nature Structural &Molecular Biology.

WHSC1 links transcription elongation to HIRA‐mediated histone H3.3 deposition

K. Ozato, T. Tamura, T. Heightman, 2013, The EMBO journal.

Targeting Methyl Lysine

S. Frye, T. Heightman, Jian Jin, 2010 .

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.

Fiona Pachl, A. Pike, M. O’Connor, 2021, Journal of medicinal chemistry.

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.

S. Knapp, O. Fedorov, P. Filippakopoulos, 2011, Molecular bioSystems.

High-resolution native and complex structures of thermostable beta-mannanase from Thermomonospora fusca - substrate specificity in glycosyl hydrolase family 5.

W. Zimmermann, K. Piontek, S. Gloor, 1998, Structure.

BRD4 Coordinates Recruitment of Pause Release Factor P-TEFb and the Pausing Complex NELF/DSIF To Regulate Transcription Elongation of Interferon-Stimulated Genes

K. Ozato, A. Dey, T. Tamura, 2013, Molecular and Cellular Biology.

ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK

C. Murray, V. Berdini, J. Lyons, 2021, Molecular Cancer Therapeutics.

Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.

I. Wall, K. Philpott, T. Heightman, 2014, Journal of medicinal chemistry.

Therapeutic prospects for epigenetic modulation

T. Heightman, 2011, Expert opinion on therapeutic targets.

Chemical Biology of Lysine Demethylases

T. Heightman, 2011, Current chemical genomics.

Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.

C. Murray, V. Berdini, L. Fazal, 2021, Journal of medicinal chemistry.

Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.

C. Murray, V. Berdini, J. Castro, 2018, Journal of medicinal chemistry.

Development of homogeneous luminescence assays for histone demethylase catalysis and binding.

U. Oppermann, T. Heightman, C. Schofield, 2010, Analytical biochemistry.

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

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

Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.

Paul N. Mortenson, E. Chiarparin, T. Heightman, 2014, ACS medicinal chemistry letters.

High-Affinity Inhibitors of Human NAD+-Dependent 15-Hydroxyprostaglandin Dehydrogenase: Mechanisms of Inhibition and Structure-Activity Relationships

A. Jadhav, A. Simeonov, U. Oppermann, 2010, PloS one.

Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.

Paul N. Mortenson, W. Rumsey, H. Willems, 2019, Journal of medicinal chemistry.

Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.

M. Verdonk, W. Rumsey, H. Willems, 2021, 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.

8‐Piperazinyl‐2,3‐dihydropyrrolo[3,2‐g]isoquinolines: Potent, Selective, Orally Bioavailable 5‐HT1 Receptor Ligands.

T. Heightman, 2005 .

Epigenetic-Targeted Drug Discovery

T. Heightman, A. Pope, 2011, Journal of biomolecular screening.

Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c8sc02754d

P. Nordlund, O. Surova, M. O’Reilly, 2018, Chemical science.

The discovery of the benzazepine class of histamine H3 receptor antagonists.

Michael A. Briggs, Robert P. Davis, David M. Wilson, 2013, Bioorganic & medicinal chemistry letters.

Identification of small molecule agonists of the motilin receptor.

Alan Wise, G. Macdonald, A. Muir, 2008, Bioorganic & medicinal chemistry letters.

Inhibition of Histone Demethylases by 4‐Carboxy‐2,2′‐Bipyridyl Compounds

T. Heightman, C. Schofield, A. Tumber, 2011, ChemMedChem.

Protein degradation: a validated therapeutic strategy with exciting prospects.

T. Heightman, Honorine Lebraud, 2017, Essays in biochemistry.

Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.

S. Bromidge, F. King, G. Riley, 2001, Bioorganic & medicinal chemistry letters.

Recent Insights into Inhibition, Structure, and Mechanism of Configuration-Retaining Glycosidases.

A. Vasella, T. Heightman, 1999, Angewandte Chemie.