Current status in the discovery of dual BET/HDAC inhibitors
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 devel...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Ren, Qinghua [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2021transfer abstract |
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| Schlagwörter: |
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| Übergeordnetes Werk: |
Enthalten in: Feeding European sea bass ( - Torrecillas, S. ELSEVIER, 2018, a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Amsterdam [u.a.] |
|---|---|
| Übergeordnetes Werk: |
volume:38 ; year:2021 ; day:15 ; month:04 ; pages:0 |
| Links: |
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| DOI / URN: |
10.1016/j.bmcl.2021.127829 |
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| 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. | ||
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10.1016/j.bmcl.2021.127829 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001329.pica (DE-627)ELV053431596 (ELSEVIER)S0960-894X(21)00055-X DE-627 ger DE-627 rakwb eng 630 VZ 22 ssgn 46.00 bkl Ren, Qinghua verfasserin aut Current status in the discovery of dual BET/HDAC inhibitors 2021transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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. 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. BET Elsevier Inhibitors Elsevier HDAC Elsevier Gao, Wenqian oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:38 year:2021 day:15 month:04 pages:0 https://doi.org/10.1016/j.bmcl.2021.127829 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 38 2021 15 0415 0 |
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10.1016/j.bmcl.2021.127829 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001329.pica (DE-627)ELV053431596 (ELSEVIER)S0960-894X(21)00055-X DE-627 ger DE-627 rakwb eng 630 VZ 22 ssgn 46.00 bkl Ren, Qinghua verfasserin aut Current status in the discovery of dual BET/HDAC inhibitors 2021transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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. 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. BET Elsevier Inhibitors Elsevier HDAC Elsevier Gao, Wenqian oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:38 year:2021 day:15 month:04 pages:0 https://doi.org/10.1016/j.bmcl.2021.127829 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 38 2021 15 0415 0 |
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10.1016/j.bmcl.2021.127829 doi /cbs_pica/cbs_olc/import_discovery/elsevier/einzuspielen/GBV00000000001329.pica (DE-627)ELV053431596 (ELSEVIER)S0960-894X(21)00055-X DE-627 ger DE-627 rakwb eng 630 VZ 22 ssgn 46.00 bkl Ren, Qinghua verfasserin aut Current status in the discovery of dual BET/HDAC inhibitors 2021transfer abstract nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier 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. 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. BET Elsevier Inhibitors Elsevier HDAC Elsevier Gao, Wenqian oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:38 year:2021 day:15 month:04 pages:0 https://doi.org/10.1016/j.bmcl.2021.127829 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 38 2021 15 0415 0 |
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Current status in the discovery of dual BET/HDAC inhibitors |
| abstract |
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. |
| abstractGer |
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. |
| abstract_unstemmed |
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. |
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GBV_USEFLAG_U GBV_ELV SYSFLAG_U |
| title_short |
Current status in the discovery of dual BET/HDAC inhibitors |
| url |
https://doi.org/10.1016/j.bmcl.2021.127829 |
| remote_bool |
true |
| author2 |
Gao, Wenqian |
| author2Str |
Gao, Wenqian |
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| doi_str |
10.1016/j.bmcl.2021.127829 |
| up_date |
2024-07-06T18:56:09.423Z |
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