Synthesis of Lysine Methyltransferase Inhibitors
Lysine methyltransferase which catalyze methylation of histone and nonhistone proteins, play a crucial role in diverse biological processes and has emerged as a promising target for the development of various human diseases, including cancer, inflammation, and psychiatric disorders. However, inhibit...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2015-07-01
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| Series: | Frontiers in Chemistry |
| Subjects: | |
| Online Access: | http://journal.frontiersin.org/Journal/10.3389/fchem.2015.00044/full |
| _version_ | 1828824468226572288 |
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| author | Tao eYe Chunngai eHui |
| author_facet | Tao eYe Chunngai eHui |
| author_sort | Tao eYe |
| collection | DOAJ |
| description | Lysine methyltransferase which catalyze methylation of histone and nonhistone proteins, play a crucial role in diverse biological processes and has emerged as a promising target for the development of various human diseases, including cancer, inflammation, and psychiatric disorders. However, inhibiting Lysine methyltransferases selectively has presented many challenges to medicinal chemists. During the past decade, lysine methyltransferase inhibitors covering many different structural classes have been designed and developed. In this review, we describe the development of selective, small-molecule inhibitors of lysine methyltransferases with an emphasis on their discovery and chemical synthesis. We highlight the current state of lysine methyltransferase inhibitors and discuss future directions and opportunities for lysine methyltransferase inhibitor discovery. |
| first_indexed | 2024-12-12T13:57:48Z |
| format | Article |
| id | doaj.art-78fb4c6e6d8849ce8021d9bab432f673 |
| institution | Directory Open Access Journal |
| issn | 2296-2646 |
| language | English |
| last_indexed | 2024-12-12T13:57:48Z |
| publishDate | 2015-07-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Chemistry |
| spelling | doaj.art-78fb4c6e6d8849ce8021d9bab432f6732022-12-22T00:22:26ZengFrontiers Media S.A.Frontiers in Chemistry2296-26462015-07-01310.3389/fchem.2015.00044153269Synthesis of Lysine Methyltransferase InhibitorsTao eYe0Chunngai eHui1The Hong Kong Polytechnic UniversityThe Hong Kong Polytechnic UniversityLysine methyltransferase which catalyze methylation of histone and nonhistone proteins, play a crucial role in diverse biological processes and has emerged as a promising target for the development of various human diseases, including cancer, inflammation, and psychiatric disorders. However, inhibiting Lysine methyltransferases selectively has presented many challenges to medicinal chemists. During the past decade, lysine methyltransferase inhibitors covering many different structural classes have been designed and developed. In this review, we describe the development of selective, small-molecule inhibitors of lysine methyltransferases with an emphasis on their discovery and chemical synthesis. We highlight the current state of lysine methyltransferase inhibitors and discuss future directions and opportunities for lysine methyltransferase inhibitor discovery.http://journal.frontiersin.org/Journal/10.3389/fchem.2015.00044/fullepigeneticsSynthesisinhibitorsS-Adenosyl-l-methionineLysine methyltransferase |
| spellingShingle | Tao eYe Chunngai eHui Synthesis of Lysine Methyltransferase Inhibitors Frontiers in Chemistry epigenetics Synthesis inhibitors S-Adenosyl-l-methionine Lysine methyltransferase |
| title | Synthesis of Lysine Methyltransferase Inhibitors |
| title_full | Synthesis of Lysine Methyltransferase Inhibitors |
| title_fullStr | Synthesis of Lysine Methyltransferase Inhibitors |
| title_full_unstemmed | Synthesis of Lysine Methyltransferase Inhibitors |
| title_short | Synthesis of Lysine Methyltransferase Inhibitors |
| title_sort | synthesis of lysine methyltransferase inhibitors |
| topic | epigenetics Synthesis inhibitors S-Adenosyl-l-methionine Lysine methyltransferase |
| url | http://journal.frontiersin.org/Journal/10.3389/fchem.2015.00044/full |
| work_keys_str_mv | AT taoeye synthesisoflysinemethyltransferaseinhibitors AT chunngaiehui synthesisoflysinemethyltransferaseinhibitors |