269 results on '"Heightman, Tom"'
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2. The Cryptosporidium parvum Kinome
3. Supplementary Tables 1-6 from ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
4. Supplementary Figures 1-7 from ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
5. Data from ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
6. Supplementary Methods from ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
7. Animal Models of Epigenetic Regulation in Neuropsychiatric Disorders
8. Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor
9. Targeting DNA Methylation
10. Development of homogeneous luminescence assays for histone demethylase catalysis and binding
11. 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
12. WHSC1 links transcription elongation to HIRA‐mediated histone H3.3 deposition
13. 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
14. Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2
15. ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
16. 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
17. Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe
18. Fragment-based drug discovery: opportunities for organic synthesis
19. Animal Models of Epigenetic Regulation in Neuropsychiatric Disorders
20. Chemical Biology of Histone Modifications
21. Targeting Methyl Lysine
22. A structural view of the action of Escherichia coli (lacZ) beta-galactosidase
23. Selective inhibition of BET bromodomains
24. Transcriptional regulation of interferon stimulated genes: Role of chromatin binding protein Brd4: SS3-7
25. Nonenzymatic biotinylation of histone H2A
26. Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines
27. 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.
28. Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methyl-pyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
29. 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
30. Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines
31. Abstract 5781: A novel ERK1/2 inhibitor has potent activity in KRAS-mutant non-small cell lung cancer models
32. Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition
33. Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2
34. Abstract B161: Fragment-based discovery of a highly potent, orally bioavailable ERK1/2 inhibitor that modulates the phosphorylation and catalytic activity of ERK1/2
35. Abstract B154: Characterization of a novel ERK1/2 inhibitor, which modulates the phosphorylation and catalytic activity of ERK1/2
36. Fragment-based drug discovery: opportunities for organic synthesis
37. Protein degradation: a validated therapeutic strategy with exciting prospects
38. Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP)
39. Visualization of Endogenous ERK1/2 in Cells with a Bioorthogonal Covalent Probe
40. Application of a recyclable pseudoephedrine resin in asymmetric alkylations on solid phase
41. The discovery of the benzazepine class of histamine H3 receptor antagonists
42. Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras
43. Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives
44. Isoxazole‐Derived Amino Acids are Bromodomain‐Binding Acetyl‐Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3
45. 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
46. In-gel activity-based protein profiling of a clickable covalent ERK1/2 inhibitor
47. Optimization of Sphingosine-1-phosphate-1 Receptor Agonists: Effects of Acidic, Basic, and Zwitterionic Chemotypes on Pharmacokinetic and Pharmacodynamic Profiles
48. BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones
49. Abstract SY05-01: Fragment-based drug discovery: Less is more
50. A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation-π Interaction
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