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- Publisher Website: 10.1016/j.ejmech.2020.113120
- Scopus: eid_2-s2.0-85098856655
- PMID: 33422982
- WOS: WOS:000629622800023
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Article: Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions
Title | Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions |
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Authors | |
Keywords | Single-step Fluorescent probe Decrotonylation Histone deacetylases Sirtuin |
Issue Date | 2020 |
Publisher | Elsevier France, Editions Scientifiques et Medicales. The Journal's web site is located at http://www.elsevier.com/locate/ejmech |
Citation | European Journal of Medicinal Chemistry, 2020, v. 212, p. article no. 113120 How to Cite? |
Abstract | Lysine crotonylation plays vital roles in gene transcription and cellular metabolism. Nevertheless, methods for dissecting the molecular mechanisms of decrotonyaltion remains limited. So far, there is no single-step fluorescent method developed for enzymatic decrotonylation activity detection. The major difficulty is that the aliphatic crotonylated lysine doesn’t allow π-conjugation to a fluorophore and decrotonylation can not modulate the electronic state directly. Herein, we have designed and synthesized two activity-based single-step fluorogenic probes KTcr-I and KTcr-II for detecting enzymatic decrotonylation activity. These two probes can be recognized by histone deacetylases and undergo intramolecular nucleophilic exchange reaction to generate fluorescence signal. Notably, peptide sequence-dependent effect was observed. KTcr-I can be recognized by Sirt2 more effectively, while KTcr-II with LGKcr peptide sequence preferentially reacted with HDAC3. Compared to other methods of studying enzymatic decrotonylation activity, our single-step fluorescent method has a number of advantages, such as facileness, high sensitivity, cheap facility and little material consumed. We envision that the probes developed in this study will provide useful tools to screen inhibitors which suppress the decrotonylation activity of HDACs. Such probes will be useful for further delineating the roles of decrotonylation enzyme and aid in biomarker identification and drug discovery. |
Persistent Identifier | http://hdl.handle.net/10722/295543 |
ISSN | 2023 Impact Factor: 6.0 2023 SCImago Journal Rankings: 1.151 |
ISI Accession Number ID |
DC Field | Value | Language |
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dc.contributor.author | Xie, Y | - |
dc.contributor.author | Yang, L | - |
dc.contributor.author | Chen, Q | - |
dc.contributor.author | Zhang, J | - |
dc.contributor.author | Feng, L | - |
dc.contributor.author | Chen, JL | - |
dc.contributor.author | Hao, Q | - |
dc.contributor.author | Zhang, L | - |
dc.contributor.author | Sun, H | - |
dc.date.accessioned | 2021-01-25T11:16:22Z | - |
dc.date.available | 2021-01-25T11:16:22Z | - |
dc.date.issued | 2020 | - |
dc.identifier.citation | European Journal of Medicinal Chemistry, 2020, v. 212, p. article no. 113120 | - |
dc.identifier.issn | 0223-5234 | - |
dc.identifier.uri | http://hdl.handle.net/10722/295543 | - |
dc.description.abstract | Lysine crotonylation plays vital roles in gene transcription and cellular metabolism. Nevertheless, methods for dissecting the molecular mechanisms of decrotonyaltion remains limited. So far, there is no single-step fluorescent method developed for enzymatic decrotonylation activity detection. The major difficulty is that the aliphatic crotonylated lysine doesn’t allow π-conjugation to a fluorophore and decrotonylation can not modulate the electronic state directly. Herein, we have designed and synthesized two activity-based single-step fluorogenic probes KTcr-I and KTcr-II for detecting enzymatic decrotonylation activity. These two probes can be recognized by histone deacetylases and undergo intramolecular nucleophilic exchange reaction to generate fluorescence signal. Notably, peptide sequence-dependent effect was observed. KTcr-I can be recognized by Sirt2 more effectively, while KTcr-II with LGKcr peptide sequence preferentially reacted with HDAC3. Compared to other methods of studying enzymatic decrotonylation activity, our single-step fluorescent method has a number of advantages, such as facileness, high sensitivity, cheap facility and little material consumed. We envision that the probes developed in this study will provide useful tools to screen inhibitors which suppress the decrotonylation activity of HDACs. Such probes will be useful for further delineating the roles of decrotonylation enzyme and aid in biomarker identification and drug discovery. | - |
dc.language | eng | - |
dc.publisher | Elsevier France, Editions Scientifiques et Medicales. The Journal's web site is located at http://www.elsevier.com/locate/ejmech | - |
dc.relation.ispartof | European Journal of Medicinal Chemistry | - |
dc.subject | Single-step | - |
dc.subject | Fluorescent probe | - |
dc.subject | Decrotonylation | - |
dc.subject | Histone deacetylases | - |
dc.subject | Sirtuin | - |
dc.title | Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions | - |
dc.type | Article | - |
dc.identifier.email | Hao, Q: qhao@hku.hk | - |
dc.identifier.authority | Hao, Q=rp01332 | - |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1016/j.ejmech.2020.113120 | - |
dc.identifier.pmid | 33422982 | - |
dc.identifier.scopus | eid_2-s2.0-85098856655 | - |
dc.identifier.hkuros | 320941 | - |
dc.identifier.volume | 212 | - |
dc.identifier.spage | article no. 113120 | - |
dc.identifier.epage | article no. 113120 | - |
dc.identifier.isi | WOS:000629622800023 | - |
dc.publisher.place | France | - |