Skip to content

Home Search Authors Pakistan News Saved

SciRah

SciRah does not host or store research papers. Results come live from free, official scholarly APIs, and every paper links back to its original source.

Data sources

OpenAlex
Semantic Scholar
Crossref
CORE
arXiv
PubMed

Privacy policy Terms of service

T. Heightman · SciRah

Researcher profile · Semantic Scholar

T. Heightman

Share profile

T. Heightman — researcher profile on SciRah

h-index: 34
Works: 120
Citations: 8,760

Most-cited papers

Selective inhibition of BET bromodomains
P. Filippakopoulos, J. Qi, S. Picaud, Yao Shen +21 more
2010Nature4,051 citations Open access
Semantic Scholar
Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras
Honorine Lebraud, D. J. Wright, Christopher N. Johnson, T. Heightman
2016ACS Central Science341 citations Open access
Semantic Scholar
BRD4 assists elongation of both coding and enhancer RNAs guided by histone acetylation
T. Kanno, Y. Kanno, G. Leroy, E. Campos +9 more
2014Nature Structural &Molecular Biology295 citations Open access
Semantic Scholar
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.
T. G. Davies, W. Wixted, J. Coyle, C. Griffiths-Jones +21 more
2016Journal of Medicinal Chemistry272 citations Open access
Semantic Scholar
3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands
D. Hewings, Ming-Hua Wang, M. Philpott, O. Fedorov +8 more
2011Journal of Medicinal Chemistry211 citations Open access
Semantic Scholar
Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors
O. King, X. Li, Masaaki Sakurai, A. Kawamura +13 more
2010PLoS ONE210 citations Open access
Semantic Scholar
BRD4 Coordinates Recruitment of Pause Release Factor P-TEFb and the Pausing Complex NELF/DSIF To Regulate Transcription Elongation of Interferon-Stimulated Genes
Mira C. Patel, Maxime Debrosse, Matthew Smith, Anup Dey +5 more
2013Molecular and Cellular Biology173 citations Open access
Semantic Scholar
A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases
Xue-Lai Luo, Yong-Xian Liu, S. Kubicek, J. Myllyharju +8 more
2011Journal of the American Chemical Society149 citations Open access
Semantic Scholar
Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
M. Philpott, Jing Yang, Tony Tumber, O. Fedorov +8 more
2011Molecular Biosystems131 citations
Semantic Scholar
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.
J. Johannes, Amber Y. S. Balazs, D. Barratt, M. Biśta +39 more
2021Journal of Medicinal Chemistry127 citations Open access
Semantic Scholar
A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation–π Interaction
T. Rooney, P. Filippakopoulos, O. Fedorov, S. Picaud +16 more
2014Angewandte Chemie112 citations Open access
Semantic Scholar
Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors
J. Spencer, Jahangir Amin, Ming-Hua Wang, G. Packham +6 more
2011ACS Medicinal Chemistry Letters96 citations Open access
Semantic Scholar
Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
F. Ferguson, O. Fedorov, A. Chaikuad, M. Philpott +7 more
2013Journal of Medicinal Chemistry89 citations Open access
Semantic Scholar
Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds
Kai-Hsuan Chang, O. King, A. Tumber, E. Woon +4 more
2011ChemMedChem79 citations Open access
Semantic Scholar
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.
T. Heightman, J. Callahan, E. Chiarparin, J. Coyle +18 more
2019Journal of Medicinal Chemistry78 citations Open access
Semantic Scholar
WHSC1 links transcription elongation to HIRA‐mediated histone H3.3 deposition
Naoyuki Sarai, Keisuke Nimura, T. Tamura, T. Kanno +4 more
2013EMBO Journal66 citations Open access
Semantic Scholar
Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
E. Tamanini, I. Buck, G. Chessari, E. Chiarparin +15 more
2017Journal of Medicinal Chemistry63 citations Open access
Semantic Scholar
Development of homogeneous luminescence assays for histone demethylase catalysis and binding
A. Kawamura, A. Tumber, Nathan R. Rose, O. King +4 more
2010Analytical Biochemistry63 citations Open access
Semantic Scholar
Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.
D. Tisi, E. Chiarparin, E. Tamanini, P. Pathuri +20 more
2016ACS Chemical Biology58 citations
Semantic Scholar
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
T. Heightman, V. Berdini, Hannah Braithwaite, I. Buck +32 more
2018Journal of Medicinal Chemistry51 citations Open access
Semantic Scholar
Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates
Armin Thalhammer, Jasmin Mecinović, Christoph Loenarz, A. Tumber +3 more
2010Organic and biomolecular chemistry51 citations Open access
Semantic Scholar
The Cryptosporidium parvum Kinome
J. Artz, A. Wernimont, A. Allali‐Hassani, Yong Zhao +22 more
2011BMC Genomics47 citations Open access
Semantic Scholar
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains
D. Hay, O. Fedorov, P. Filippakopoulos, Sarah Martin +8 more
2013MedChemComm46 citations Open access
Semantic Scholar
Click JAHAs: Conformationally restricted ferrocene-based histone deacetylase inhibitors
J. Spencer, Jahangir Amin, R. Boddiboyena, G. Packham +11 more
201242 citations
Semantic Scholar
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
D. F. Corbett, T. Heightman, S. Moss, S. Bromidge +5 more
2005Bioorganic & Medicinal Chemistry Letters41 citations Open access
Semantic Scholar
Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines
R. Grainger, T. Heightman, S. Ley, Fabio H. B. Lima +1 more
2018Chemical Science40 citations Open access
Semantic Scholar
High-Affinity Inhibitors of Human NAD+-Dependent 15-Hydroxyprostaglandin Dehydrogenase: Mechanisms of Inhibition and Structure-Activity Relationships
F. Niesen, Lena Schultz, A. Jadhav, C. Bhatia +7 more
2010PLoS ONE39 citations Open access
Semantic Scholar
Fragment-based drug discovery: opportunities for organic synthesis
Jeffrey D. St-Denis, Richard J. Hall, C. Murray, T. Heightman +1 more
2020RSC Medicinal Chemistry36 citations Open access
Semantic Scholar
Development of a solid-phase 'asymmetric resin-capture-release' process: application of an ephedrine chiral resin in an approach to gamma-butyrolactones.
N. Kerrigan, Panee C. Hutchison, T. Heightman, D. Procter
2004Organic and biomolecular chemistry35 citations
Semantic Scholar
Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
J. Johannes, Amber Y. S. Balazs, Derek G. Barratt, M. Biśta +38 more
2024Journal of Medicinal Chemistry33 citations Open access
Semantic Scholar
Application of an ephedrine chiral linker in a solid-phase, ‘asymmetric catch-release’ approach to γ-butyrolactones
N. Kerrigan, Panee C. Hutchison, T. Heightman, D. Procter
200332 citations
Semantic Scholar
Application of a recyclable pseudoephedrine resin in asymmetric alkylations on solid phase.
Panee C. Hutchison, T. Heightman, D. Procter
2004Journal of Organic Chemistry30 citations
Semantic Scholar
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
E. Demont, Sandra Arpino, R. A. Bit, Colin A. Campbell +19 more
2011Journal of Medicinal Chemistry29 citations Open access
Semantic Scholar
Nonenzymatic biotinylation of histone H2A
S. Healy, T. Heightman, Laura Hohmann, D. Schriemer +1 more
2009Protein Science29 citations Open access
Semantic Scholar
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.
D. Norton, W. Bonnette, J. Callahan, M. Carr +15 more
2021Journal of Medicinal Chemistry28 citations Open access
Semantic Scholar
Protein degradation: a validated therapeutic strategy with exciting prospects.
Honorine Lebraud, T. Heightman
2017Essays in Biochemistry25 citations
Semantic Scholar
Therapeutic prospects for epigenetic modulation
T. Heightman
2011Expert opinion on therapeutic targets25 citations
Semantic Scholar
Terminal aziridines by alpha-deprotonation/electrophile trapping of N-protected aziridine.
D. M. Hodgson, S. Hughes, A. Thompson, T. Heightman
2008Organic Letters24 citations
Semantic Scholar
Isoxazole‐Derived Amino Acids are Bromodomain‐Binding Acetyl‐Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3
Angelina R. Sekirnik Née Measures, D. Hewings, N. H. Theodoulou, Lukass Jursins +5 more
2016Angewandte Chemie22 citations Open access
Semantic Scholar
Chemical Biology of Lysine Demethylases
T. Heightman
2011Current Chemical Genomics22 citations Open access
Semantic Scholar
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
J. Skidmore, J. Heer, Christopher N. Johnson, David Norton +20 more
2014Journal of Medicinal Chemistry21 citations Open access
Semantic Scholar
Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.
S. Howard, N. Amin, Andrew B. Benowitz, E. Chiarparin +15 more
2014ACS Medicinal Chemistry Letters20 citations Open access
Semantic Scholar
ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
J. Munck, V. Berdini, L. Bevan, J. Brothwood +23 more
2021Molecular Cancer Therapeutics19 citations
Semantic Scholar
Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.
E. Tamanini, Shin Miyamura, I. Buck, Benjamin D. Cons +24 more
2022ACS Medicinal Chemistry Letters17 citations Open access
Semantic Scholar
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
T. Heightman, V. Berdini, L. Bevan, I. Buck +31 more
2021Journal of Medicinal Chemistry15 citations Open access
Semantic Scholar
Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.
J. Witherington, L. Abberley, Michael A. Briggs, Katharine Collis +14 more
2008Bioorganic & Medicinal Chemistry Letters15 citations Open access
Semantic Scholar
Identification of small molecule agonists of the motilin receptor.
T. Heightman, E. Conway, D. F. Corbett, G. Macdonald +15 more
2008Bioorganic & Medicinal Chemistry Letters15 citations Open access
Semantic Scholar
In-gel activity-based protein profiling of a clickable covalent ERK1/2 inhibitor.
Honorine Lebraud, D. J. Wright, C. East, F. Holding +2 more
2016Molecular Biosystems14 citations
Semantic Scholar
Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.
T. Heightman, Jackie S. Scott, Mark J. Longley, V. Bordas +18 more
2007Bioorganic & Medicinal Chemistry Letters13 citations Open access
Semantic Scholar
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
S. Westaway, S. L. Brown, E. Conway, T. Heightman +24 more
2008Bioorganic & Medicinal Chemistry Letters12 citations Open access
Semantic Scholar

Frequent co-authors

Invite them to SciRah by sharing their profile.

S. Rich×8
Invite
S. Rich — researcher profile on SciRah
O. Fedorov×7
Invite
O. Fedorov — researcher profile on SciRah
C. Griffiths-Jones×7
Invite
C. Griffiths-Jones — researcher profile on SciRah
A. Woolford×7
Invite
A. Woolford — researcher profile on SciRah

×6

Invite

M. Philpott — researcher profile on SciRah

Invite

D. Norton — researcher profile on SciRah

P. Filippakopoulos×5

Invite

P. Filippakopoulos — researcher profile on SciRah

Invite

S. Picaud — researcher profile on SciRah

Invite

S. Knapp — researcher profile on SciRah

Christopher N. Johnson×5

Invite

Christopher N. Johnson — researcher profile on SciRah

C. Richardson×5

Invite

C. Richardson — researcher profile on SciRah

Ming-Hua Wang×5

Invite

Ming-Hua Wang — researcher profile on SciRah