2020
DOI: 10.1016/j.bcp.2020.114224
|View full text |Cite
|
Sign up to set email alerts
|

Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
4
1

Citation Types

0
30
0
1

Year Published

2022
2022
2024
2024

Publication Types

Select...
9

Relationship

3
6

Authors

Journals

citations
Cited by 57 publications
(31 citation statements)
references
References 255 publications
0
30
0
1
Order By: Relevance
“…HATs catalyze the transfer of acetyl from donor-acetyl coenzyme A to lysine residues of the histone peptide, which could increase the level of histone acetylation to make the chromatin sustain an active transcription ( 78 ). In contrast, HDACs are responsible for catalyzing the removal of acetyl from ϵ-amino groups of conserved lysine residues at the histone amino terminal tail, thus leading to a low level of acetylation as well as heterochromatin and gene silence ( 82 , 83 ). There are 18 human HDACs identified and categorized into four classes: class I are Rpd3-like proteins and composed of HDAC1, HDAC2, HDAC3, and HDAC8; class II are Hda1-like proteins consisting of HDAC4~HDAC7 and HDAC9~10; class III are Sir2-like proteins including SIRT1~7; and class IV only contains HDAC11 ( 84 ).…”
Section: Immunity and Inflammation To Inflammatory Diseasementioning
confidence: 99%
“…HATs catalyze the transfer of acetyl from donor-acetyl coenzyme A to lysine residues of the histone peptide, which could increase the level of histone acetylation to make the chromatin sustain an active transcription ( 78 ). In contrast, HDACs are responsible for catalyzing the removal of acetyl from ϵ-amino groups of conserved lysine residues at the histone amino terminal tail, thus leading to a low level of acetylation as well as heterochromatin and gene silence ( 82 , 83 ). There are 18 human HDACs identified and categorized into four classes: class I are Rpd3-like proteins and composed of HDAC1, HDAC2, HDAC3, and HDAC8; class II are Hda1-like proteins consisting of HDAC4~HDAC7 and HDAC9~10; class III are Sir2-like proteins including SIRT1~7; and class IV only contains HDAC11 ( 84 ).…”
Section: Immunity and Inflammation To Inflammatory Diseasementioning
confidence: 99%
“…10,11 Other anticancer, hybrid molecule discovery toward multiple oncogenic pathways include either CRBN with HDAC, JAK with HDAC, and EGFR with NAMPT inhibitors. 12 All these case studies suggest the importance of hybrid molecules for the treatment of different types of diseases. Thus, based on these successful studies on multitargeting inhibitors encouraged us in the design of dual targeting (BCR-ABL and HDAC) hybrid molecules in an attempt to overcome the mutational resistance associated with single-targeted agents in CML.…”
Section: ■ Introductionmentioning
confidence: 99%
“…However, drug-induced adverse effects were seen in such cocktails, including drug–drug interactions, complex polypharmacokinetic properties, and poor patient compliance. , Thus, to overcome these adverse reactions, a single hybrid molecule designed by combining the key pharmacophores of clinically tested drugs has attracted attention in recent times. , In osteosarcoma, hybrid molecules were developed by combining cyclolignan related to podophyllic aldehyde and quinone fragments in diterpenylnaphtho hydroquinones through aliphatic or aromatic linkers (spacers) and were further evaluated successfully in specific tumor cell lines . Development of hybrid molecules CUDC-101 and CUDC-907 demonstrated effectively the progression of different kinase (EGFR or (HER2 or PI3K))/HDAC based dual inhibitors into different phases of clinical trials for cancer treatment. , Other anticancer, hybrid molecule discovery toward multiple oncogenic pathways include either CRBN with HDAC, JAK with HDAC, and EGFR with NAMPT inhibitors . All these case studies suggest the importance of hybrid molecules for the treatment of different types of diseases.…”
Section: Introductionmentioning
confidence: 99%
“…Our previous work in multi-targeting drug discovery 23 , 24 prompted us to design the hybrid molecules of β -elemene by incorporating HDACi pharmacophore (hydroxamic acid). Thus, compound 2 was designed for such a purpose ( Figure 3) .…”
Section: Introductionmentioning
confidence: 99%