Current status in the discovery of dual BET/HDAC inhibitors
Copyright © 2021 Elsevier Ltd. All rights reserved..
The development of desired multitarget agents may provide an attractive and cost-effective complement or alternative to drug combinations. Bromodomain and extraterminal domain (BET) and histone deacetylase (HDAC), as important epigenetic modulators, are attractive targets in drug discovery and development. Considering the fact that BET and HDAC inhibitors exert a synergistic effect on cellular processes in cancer cells, the design of dual BET/HDAC inhibitors may be a rational strategy to improve the efficacy of their single-target drugs for tumor treatment. In the current review, we depict the development of dual BET/HDAC inhibitors and particularly highlight their structure-activity relationships (SARs), binding modes, and biological functions with the aim to facilitate rational drug design and develop more dual BET/HDAC inhibitors.
| Errataetall: |
ErratumFor: Bioorg Med Chem Lett. 2021 Jan 1;31:127671. - PMID 33229136 |
|---|---|
| Medienart: |
E-Artikel |
| Erscheinungsjahr: |
2021 |
|---|---|
| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:38 |
|---|---|
| Enthalten in: |
Bioorganic & medicinal chemistry letters - 38(2021) vom: 15. Apr., Seite 127829 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Ren, Qinghua [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
|---|
| Anmerkungen: |
Date Revised 02.04.2021 published: Print-Electronic ErratumFor: Bioorg Med Chem Lett. 2021 Jan 1;31:127671. - PMID 33229136 Citation Status PubMed-not-MEDLINE |
|---|
| doi: |
10.1016/j.bmcl.2021.127829 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM322429765 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM322429765 | ||
| 003 | DE-627 | ||
| 005 | 20231225182025.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2021 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1016/j.bmcl.2021.127829 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1074.xml |
| 035 | |a (DE-627)NLM322429765 | ||
| 035 | |a (NLM)33685790 | ||
| 035 | |a (PII)S0960-894X(21)00055-X | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Ren, Qinghua |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Current status in the discovery of dual BET/HDAC inhibitors |
| 264 | 1 | |c 2021 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Revised 02.04.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a ErratumFor: Bioorg Med Chem Lett. 2021 Jan 1;31:127671. - PMID 33229136 | ||
| 500 | |a Citation Status PubMed-not-MEDLINE | ||
| 520 | |a Copyright © 2021 Elsevier Ltd. All rights reserved. | ||
| 520 | |a The development of desired multitarget agents may provide an attractive and cost-effective complement or alternative to drug combinations. Bromodomain and extraterminal domain (BET) and histone deacetylase (HDAC), as important epigenetic modulators, are attractive targets in drug discovery and development. Considering the fact that BET and HDAC inhibitors exert a synergistic effect on cellular processes in cancer cells, the design of dual BET/HDAC inhibitors may be a rational strategy to improve the efficacy of their single-target drugs for tumor treatment. In the current review, we depict the development of dual BET/HDAC inhibitors and particularly highlight their structure-activity relationships (SARs), binding modes, and biological functions with the aim to facilitate rational drug design and develop more dual BET/HDAC inhibitors | ||
| 650 | 4 | |a Published Erratum | |
| 650 | 4 | |a BET | |
| 650 | 4 | |a HDAC | |
| 650 | 4 | |a Inhibitors | |
| 700 | 1 | |a Gao, Wenqian |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Bioorganic & medicinal chemistry letters |d 1992 |g 38(2021) vom: 15. Apr., Seite 127829 |w (DE-627)NLM09063828X |x 1464-3405 |7 nnns |
| 773 | 1 | 8 | |g volume:38 |g year:2021 |g day:15 |g month:04 |g pages:127829 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1016/j.bmcl.2021.127829 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 38 |j 2021 |b 15 |c 04 |h 127829 | ||