File Download
There are no files associated with this item.
Links for fulltext
(May Require Subscription)
- Publisher Website: 10.1016/j.bmc.2021.116328
- Scopus: eid_2-s2.0-85111917940
- PMID: 34364223
- WOS: WOS:000704055700011
- Find via
Supplementary
- Citations:
- Appears in Collections:
Article: Identification of isoform/domain-selective fragments from the selection of DNA-encoded dynamic library
Title | Identification of isoform/domain-selective fragments from the selection of DNA-encoded dynamic library |
---|---|
Authors | |
Keywords | DNA-encoded library Dynamic combinatorial library High throughput screening Drug discovery Post-translational modification |
Issue Date | 2021 |
Publisher | Pergamon. The Journal's web site is located at http://www.elsevier.com/locate/bmc |
Citation | Bioorganic & Medicinal Chemistry, 2021, v. 45, p. article no. 116328 How to Cite? |
Abstract | DNA-encoded chemical library (DEL) has emerged to be a powerful ligand screening technology in drug discovery. Recently, we reported a DNA-encoded dynamic library (DEDL) approach that combines the principle of traditional dynamic combinatorial library (DCL) with DEL. DEDL has shown excellent potential in fragment-based ligand discovery with a variety of protein targets. Here, we further tested the utility of DEDL in identifying low molecular weight fragments that are selective for different isoforms or domains of the same protein family. A 10,000-member DEDL was selected against sirtuin-1, 2, and 5 (SIRT1, 2, 5) and the BD1 and BD2 domains of bromodomain 4 (BRD4), respectively. Albeit with modest potency, a series of isoform/domain-selective fragments were identified and the corresponding inhibitors were derived by fragment linking. |
Persistent Identifier | http://hdl.handle.net/10722/301717 |
ISSN | 2021 Impact Factor: 3.461 2020 SCImago Journal Rankings: 0.721 |
ISI Accession Number ID |
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Zhou, Y | - |
dc.contributor.author | SHEN, W | - |
dc.contributor.author | PENG, J | - |
dc.contributor.author | DENG, Y | - |
dc.contributor.author | Li, X | - |
dc.date.accessioned | 2021-08-09T03:43:11Z | - |
dc.date.available | 2021-08-09T03:43:11Z | - |
dc.date.issued | 2021 | - |
dc.identifier.citation | Bioorganic & Medicinal Chemistry, 2021, v. 45, p. article no. 116328 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://hdl.handle.net/10722/301717 | - |
dc.description.abstract | DNA-encoded chemical library (DEL) has emerged to be a powerful ligand screening technology in drug discovery. Recently, we reported a DNA-encoded dynamic library (DEDL) approach that combines the principle of traditional dynamic combinatorial library (DCL) with DEL. DEDL has shown excellent potential in fragment-based ligand discovery with a variety of protein targets. Here, we further tested the utility of DEDL in identifying low molecular weight fragments that are selective for different isoforms or domains of the same protein family. A 10,000-member DEDL was selected against sirtuin-1, 2, and 5 (SIRT1, 2, 5) and the BD1 and BD2 domains of bromodomain 4 (BRD4), respectively. Albeit with modest potency, a series of isoform/domain-selective fragments were identified and the corresponding inhibitors were derived by fragment linking. | - |
dc.language | eng | - |
dc.publisher | Pergamon. The Journal's web site is located at http://www.elsevier.com/locate/bmc | - |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry | - |
dc.subject | DNA-encoded library | - |
dc.subject | Dynamic combinatorial library | - |
dc.subject | High throughput screening | - |
dc.subject | Drug discovery | - |
dc.subject | Post-translational modification | - |
dc.title | Identification of isoform/domain-selective fragments from the selection of DNA-encoded dynamic library | - |
dc.type | Article | - |
dc.identifier.email | Zhou, Y: yuchow@hku.hk | - |
dc.identifier.email | Li, X: xiaoyuli@hku.hk | - |
dc.identifier.authority | Li, X=rp02080 | - |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1016/j.bmc.2021.116328 | - |
dc.identifier.pmid | 34364223 | - |
dc.identifier.scopus | eid_2-s2.0-85111917940 | - |
dc.identifier.hkuros | 324089 | - |
dc.identifier.volume | 45 | - |
dc.identifier.spage | article no. 116328 | - |
dc.identifier.epage | article no. 116328 | - |
dc.identifier.isi | WOS:000704055700011 | - |
dc.publisher.place | United Kingdom | - |