Targeted degradation of CD147 proteins in melanoma
Copyright © 2020 Elsevier Inc. All rights reserved..
CD147 is a transmembrane glycoprotein and a member of immunoglobulin superfamily, is strongly expressed in melanoma cells. CD147 has a pivotal role in tumor development. Therefore, it is a potential drug target for melanoma. In this article, we report the discovery of the first CD147 protein proteolysis targeting chimeras (PROTACs) derived from the natural product pseudolaric acid B (PAB). The representative compound 6a effectively induced degradation of CD147 and inhibited melanoma cells in vitro and in vivo. 6a could be used as the novel type of anticancer agent or as a part of the molecular biology research toolkit used in the gain-of-function study of the dynamic roles of CD147 in cancer networks.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2020 |
|---|---|
| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:105 |
|---|---|
| Enthalten in: |
Bioorganic chemistry - 105(2020) vom: 13. Dez., Seite 104453 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Zhou, Zhe [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
136894-56-9 |
|---|
| Anmerkungen: |
Date Completed 19.03.2021 Date Revised 29.02.2024 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1016/j.bioorg.2020.104453 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM317652265 |
|---|
| LEADER | 01000caa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM317652265 | ||
| 003 | DE-627 | ||
| 005 | 20240229233650.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2020 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1016/j.bioorg.2020.104453 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1311.xml |
| 035 | |a (DE-627)NLM317652265 | ||
| 035 | |a (NLM)33197849 | ||
| 035 | |a (PII)S0045-2068(20)31751-X | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Zhou, Zhe |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Targeted degradation of CD147 proteins in melanoma |
| 264 | 1 | |c 2020 | |
| 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 Completed 19.03.2021 | ||
| 500 | |a Date Revised 29.02.2024 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2020 Elsevier Inc. All rights reserved. | ||
| 520 | |a CD147 is a transmembrane glycoprotein and a member of immunoglobulin superfamily, is strongly expressed in melanoma cells. CD147 has a pivotal role in tumor development. Therefore, it is a potential drug target for melanoma. In this article, we report the discovery of the first CD147 protein proteolysis targeting chimeras (PROTACs) derived from the natural product pseudolaric acid B (PAB). The representative compound 6a effectively induced degradation of CD147 and inhibited melanoma cells in vitro and in vivo. 6a could be used as the novel type of anticancer agent or as a part of the molecular biology research toolkit used in the gain-of-function study of the dynamic roles of CD147 in cancer networks | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a CD147 | |
| 650 | 4 | |a Degradation | |
| 650 | 4 | |a Melanoma | |
| 650 | 4 | |a PROTAC | |
| 650 | 4 | |a Pseudolaric Acid B | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Basigin |2 NLM | |
| 650 | 7 | |a 136894-56-9 |2 NLM | |
| 650 | 7 | |a Diterpenes |2 NLM | |
| 650 | 7 | |a pseudolaric acid B |2 NLM | |
| 650 | 7 | |a 82508-31-4 |2 NLM | |
| 700 | 1 | |a Long, Jing |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Yuan |e verfasserin |4 aut | |
| 700 | 1 | |a Li, YaYun |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Xu |e verfasserin |4 aut | |
| 700 | 1 | |a Tang, Ling |e verfasserin |4 aut | |
| 700 | 1 | |a Chang, Qi |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Zhuo |e verfasserin |4 aut | |
| 700 | 1 | |a Hu, GaoYun |e verfasserin |4 aut | |
| 700 | 1 | |a Hu, Shuo |e verfasserin |4 aut | |
| 700 | 1 | |a Li, QianBin |e verfasserin |4 aut | |
| 700 | 1 | |a Peng, Cong |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Xiang |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Bioorganic chemistry |d 1986 |g 105(2020) vom: 13. Dez., Seite 104453 |w (DE-627)NLM012846570 |x 1090-2120 |7 nnns |
| 773 | 1 | 8 | |g volume:105 |g year:2020 |g day:13 |g month:12 |g pages:104453 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1016/j.bioorg.2020.104453 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 105 |j 2020 |b 13 |c 12 |h 104453 | ||