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Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs). / Bakulina, Olga; Sapegin, Alexander; Bunev, Alexander S.; Krasavin, Mikhail.

In: Mendeleev Communications , Vol. 32, No. 4, 01.07.2022, p. 419-432.

Research output: Contribution to journal › Review article › peer-review

Harvard

Bakulina, O, Sapegin, A, Bunev, AS & Krasavin, M 2022, 'Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs)', Mendeleev Communications , vol. 32, no. 4, pp. 419-432. https://doi.org/10.1016/j.mencom.2022.07.001, https://doi.org/10.1016/j.mencom.2022.07.001

APA

Bakulina, O., Sapegin, A., Bunev, A. S., & Krasavin, M. (2022). Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs). Mendeleev Communications , 32(4), 419-432. https://doi.org/10.1016/j.mencom.2022.07.001, https://doi.org/10.1016/j.mencom.2022.07.001

Vancouver

Bakulina O, Sapegin A, Bunev AS, Krasavin M. Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs). Mendeleev Communications . 2022 Jul 1;32(4):419-432. https://doi.org/10.1016/j.mencom.2022.07.001, https://doi.org/10.1016/j.mencom.2022.07.001

Author

Bakulina, Olga ; Sapegin, Alexander ; Bunev, Alexander S. ; Krasavin, Mikhail. / Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs). In: Mendeleev Communications . 2022 ; Vol. 32, No. 4. pp. 419-432.

BibTeX

@article{d9926989104e4a23a84c751cc3b07dbb,
title = "Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs)",
abstract = "The development of various heterobifunctional constructs dubbed PRoteolysis-TArgeting Chimeras (PROTACs) has gained a significant impetus in the last few years. A viable alternative to the traditional occupancy-based inhibition of aberrantly hyperactive proteins, PROTACs operate by an event-based catalytic mechanism bringing together the protein of interest (POI, to be degraded) and E3 ubiquitin ligases. The formation of the ternary complex {\textquoteleft}POI–PROTAC–E3 ubiquitin ligase{\textquoteright} is the critical step which leads to the ubiquitination of the POI and its proteasomal degradation. The current Focused Review aims to highlight the syntheses of selected innovative PROTAC-type degraders of the therapeutically important protein targets as well as some notable chemical aspects of PROTAC construction. The overview is focusing on PROTACs aimed at recruiting Cereblon, the most exploited E3 ligase for targeted protein degradation.",
keywords = "cereblon, E3 ubiquitin ligase, linkers, proteolysis-targeting chimeras, recruiter ligands, targeted protein degradation",
author = "Olga Bakulina and Alexander Sapegin and Bunev, {Alexander S.} and Mikhail Krasavin",
note = "Publisher Copyright: {\textcopyright} 2022",
year = "2022",
month = jul,
day = "1",
doi = "10.1016/j.mencom.2022.07.001",
language = "English",
volume = "32",
pages = "419--432",
journal = "Mendeleev Communications",
issn = "0959-9436",
publisher = "Elsevier",
number = "4",

}

RIS

TY - JOUR

T1 - Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs)

AU - Bakulina, Olga

AU - Sapegin, Alexander

AU - Bunev, Alexander S.

AU - Krasavin, Mikhail

N1 - Publisher Copyright: © 2022

PY - 2022/7/1

Y1 - 2022/7/1

N2 - The development of various heterobifunctional constructs dubbed PRoteolysis-TArgeting Chimeras (PROTACs) has gained a significant impetus in the last few years. A viable alternative to the traditional occupancy-based inhibition of aberrantly hyperactive proteins, PROTACs operate by an event-based catalytic mechanism bringing together the protein of interest (POI, to be degraded) and E3 ubiquitin ligases. The formation of the ternary complex ‘POI–PROTAC–E3 ubiquitin ligase’ is the critical step which leads to the ubiquitination of the POI and its proteasomal degradation. The current Focused Review aims to highlight the syntheses of selected innovative PROTAC-type degraders of the therapeutically important protein targets as well as some notable chemical aspects of PROTAC construction. The overview is focusing on PROTACs aimed at recruiting Cereblon, the most exploited E3 ligase for targeted protein degradation.

AB - The development of various heterobifunctional constructs dubbed PRoteolysis-TArgeting Chimeras (PROTACs) has gained a significant impetus in the last few years. A viable alternative to the traditional occupancy-based inhibition of aberrantly hyperactive proteins, PROTACs operate by an event-based catalytic mechanism bringing together the protein of interest (POI, to be degraded) and E3 ubiquitin ligases. The formation of the ternary complex ‘POI–PROTAC–E3 ubiquitin ligase’ is the critical step which leads to the ubiquitination of the POI and its proteasomal degradation. The current Focused Review aims to highlight the syntheses of selected innovative PROTAC-type degraders of the therapeutically important protein targets as well as some notable chemical aspects of PROTAC construction. The overview is focusing on PROTACs aimed at recruiting Cereblon, the most exploited E3 ligase for targeted protein degradation.

KW - cereblon

KW - E3 ubiquitin ligase

KW - linkers

KW - proteolysis-targeting chimeras

KW - recruiter ligands

KW - targeted protein degradation

UR - http://www.scopus.com/inward/record.url?scp=85135522317&partnerID=8YFLogxK

UR - https://www.mendeley.com/catalogue/8a9a57f4-d9fb-3324-a952-57b581021124/

U2 - 10.1016/j.mencom.2022.07.001

DO - 10.1016/j.mencom.2022.07.001

M3 - Review article

AN - SCOPUS:85135522317

VL - 32

SP - 419

EP - 432

JO - Mendeleev Communications

JF - Mendeleev Communications

SN - 0959-9436

IS - 4

ER -

ID: 97843400