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An Alkynylpyrimidine-Based Covalent Inhibitor That Targets a Unique Cysteine in NF-κB-Inducing Kinase.
J Med Chem. 2021 Jul 22;64(14):10001-10018. doi: 10.1021/acs.jmedchem.0c01249. Epub 2021 Jul 2.
J Med Chem. 2021.
PMID: 34212719
Recent advances in CDK inhibitors for cancer therapy.
Heptinstall AB, Adiyasa I, Cano C, Hardcastle IR.
Heptinstall AB, et al.
Future Med Chem. 2018 Jun 1;10(11):1369-1388. doi: 10.4155/fmc-2017-0246. Epub 2018 May 30.
Future Med Chem. 2018.
PMID: 29846081
Review.
Item in Clipboard
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C.
Myers SM, et al. Among authors: heptinstall ab.
Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25.
Eur J Med Chem. 2019.
PMID: 31212132
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Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C.
Miller DC, et al.
J Med Chem. 2022 May 12;65(9):6513-6540. doi: 10.1021/acs.jmedchem.1c01756. Epub 2022 Apr 25.
J Med Chem. 2022.
PMID: 35468293
Free PMC article.
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Cyclizations and fragmentations in the alkylation of 6-chloro-5-hydroxy-4-aminopyrimidines with aminoalkyl chlorides.
Picazo EMH, Heptinstall AB, Wilson DM, Cano C, Golding BT, Waring MJ.
Picazo EMH, et al. Among authors: heptinstall ab.
J Heterocycl Chem. 2021 Apr;58(4):947-951. doi: 10.1002/jhet.4228. Epub 2021 Feb 10.
J Heterocycl Chem. 2021.
PMID: 34824482
Free PMC article.
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Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach.
Miller DC, Martin MP, Adhikari S, Brennan A, Endicott JA, Golding BT, Hardcastle IR, Heptinstall A, Hobson S, Jennings C, Molyneux L, Ng Y, Wedge SR, Noble MEM, Cano C.
Miller DC, et al.
Org Biomol Chem. 2018 Mar 14;16(11):1843-1850. doi: 10.1039/c8ob00099a.
Org Biomol Chem. 2018.
PMID: 29469144
Free PMC article.
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The Underestimated and Overlooked Burden of Diarrhea and Constipation in Cancer Patients.
Moschen AR, Sammy Y, Marjenberg Z, Heptinstall AB, Pooley N, Marczewska AM.
Moschen AR, et al. Among authors: heptinstall ab.
Curr Oncol Rep. 2022 Jul;24(7):861-874. doi: 10.1007/s11912-022-01267-3. Epub 2022 Mar 24.
Curr Oncol Rep. 2022.
PMID: 35325401
Review.
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Mapping Ligand Interactions of Bromodomains BRD4 and ATAD2 with FragLites and PepLites─Halogenated Probes of Druglike and Peptide-like Molecular Interactions.
Davison G, Martin MP, Turberville S, Dormen S, Heath R, Heptinstall AB, Lawson M, Miller DC, Ng YM, Sanderson JN, Hope I, Wood DJ, Cano C, Endicott JA, Hardcastle IR, Noble MEM, Waring MJ.
Davison G, et al. Among authors: heptinstall ab.
J Med Chem. 2022 Nov 24;65(22):15416-15432. doi: 10.1021/acs.jmedchem.2c01357. Epub 2022 Nov 11.
J Med Chem. 2022.
PMID: 36367089
Free PMC article.
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