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PubMed Publications| Keyword search (4,163 papers available) |  |
"Ayan S" Authored Publications:
| Title | Authors | PubMed ID | |
|---|---|---|---|
| 1 | A chloromethyl-triazole fluorescent chemosensor for O6-methylguanine DNA methyltransferase | Ayan S; Rotaru AM; Kaye EG; Juneau G; Das S; Wilds CJ; Beharry AA; | 38502038 CHEMBIOCHEM |
| Title: | A chloromethyl-triazole fluorescent chemosensor for O6-methylguanine DNA methyltransferase | ||||
| Authors: | Ayan S, Rotaru AM, Kaye EG, Juneau G, Das S, Wilds CJ, Beharry AA | ||||
| Link: | https://pubmed.ncbi.nlm.nih.gov/38502038/ | ||||
| DOI: | 10.1039/d4ob00120f | ||||
| Publication: | Organic & biomolecular chemistry | ||||
| Keywords: | |||||
| PMID: | 38502038 | Category: | Date Added: | 2024-03-19 | |
| Dept Affiliation: |
CHEMBIOCHEM
1 Department of Chemical and Physical Sciences, University of Toronto Mississauga, Mississauga, Ontario, L5L 1C6, Canada. andrew.beharry@utoronto.ca. 2 Department of Chemistry and Biochemistry, Concordia University, 7141 Sherbrooke St W., Montréal, Québec, H4B 1R6, Canada. 3 Keenan Chair in Surgery, Division of Neurosurgery, St Michael's Hospital, University of Toronto, Ontario, M5B 1W8, Canada. |
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Description: |
Fluorescent chemosensors offer a direct means of measuring enzyme activity for cancer diagnosis, predicting drug resistance, and aiding in the discovery of new anticancer drugs. O6-methylguanine DNA methyltransferase (MGMT) is a predictor of resistance towards anticancer alkylating agents such as temozolomide. Using the fluorescent molecular rotor, 9-(2-carboxy-2-cyanovinyl)julolidine (CCVJ), we synthesized, and evaluated a MGMT fluorescent chemosensor derived from a chloromethyl-triazole covalent inhibitor, AA-CW236, a non-pseudosubstrate of MGMT. Our fluorescence probe covalently labelled the MGMT active site C145, producing a 18-fold increase in fluorescence. Compared to previous fluorescent probes derived from a substrate-based inhibitor, our probe had improved binding and reaction rate. Overall, our chloromethyl triazole-based fluorescence MGMT probe is a promising tool for measuring MGMT activity to predict temozolomide resistance. |
