Browsing Cancer Therapeutics by author "Carmichael, LeAnne"
Now showing items 1-3 of 3
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Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch, SB; Yapp, C; Montenegro, RC; Savitsky, P; Gamble, V; et al. (BIOMED CENTRAL LTD, 2017-03-01)BACKGROUND: Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders. The ... -
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.
Le Bihan, Y-V; Lanigan, RM; Atrash, B; McLaughlin, MG; Velupillai, S; et al. (ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2019-09-01)Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit ... -
Identification and characterisation of drug-tolerant persister cells arising in response to targeted CHK1 inhibition
Rossanese O; Carmichael, L; Rossanese, O (Institute of Cancer Research (University Of London), 2024-01-05)Drug-tolerant persisters (DTPs) are a subpopulation of slow-cycling cells that have been identified in several cancer cell lines following lethal exposure to targeted and cytotoxic therapeutics and shown to precede acquisition ...