Chemical degradation of androgen receptor (Ar) using bicalutamide analog–thalidomide protacs

Ga Yeong Kim; Chae Won Song; Yo Sep Yang; Na Rae Lee; Hyung Seok Yoo; Seung Hwan Son; Soo Jin Lee; Jong Seon Park; Jong Kil Lee; Kyung Soo Inn; Nam Jung Kim

doi:10.3390/molecules26092525

Chemical degradation of androgen receptor (Ar) using bicalutamide analog–thalidomide protacs

Ga Yeong Kim, Chae Won Song, Yo Sep Yang, Na Rae Lee, Hyung Seok Yoo, Seung Hwan Son, Soo Jin Lee, Jong Seon Park, Jong Kil Lee, Kyung Soo Inn, Nam Jung Kim

Research output: Contribution to journal › Article › peer-review

27 Citations (Scopus)

Abstract

A series of PROTACs (PROteolysis-TArgeting Chimeras) consisting of bicalutamide analogs and thalidomides were designed, synthesized, and biologically evaluated as novel androgen receptor (AR) degraders. In particular, we found that PROTAC compound 13b could successfully demonstrate a targeted degradation of AR in AR-positive cancer cells and might be a useful chemical probe for the investigation of AR-dependent cancer cells, as well as a potential therapeutic candidate for prostate cancers.

Original language	English
Article number	2525
Journal	Molecules
Volume	26
Issue number	9
DOIs	https://doi.org/10.3390/molecules26092525
Publication status	Published - 2021

Bibliographical note

Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.

Keywords

Androgen receptor (AR)
Bicalutamide
PROTAC
Prostate cancer
Protein degradation

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3390/molecules26092525

Cite this

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title = "Chemical degradation of androgen receptor (Ar) using bicalutamide analog–thalidomide protacs",

abstract = "A series of PROTACs (PROteolysis-TArgeting Chimeras) consisting of bicalutamide analogs and thalidomides were designed, synthesized, and biologically evaluated as novel androgen receptor (AR) degraders. In particular, we found that PROTAC compound 13b could successfully demonstrate a targeted degradation of AR in AR-positive cancer cells and might be a useful chemical probe for the investigation of AR-dependent cancer cells, as well as a potential therapeutic candidate for prostate cancers.",

keywords = "Androgen receptor (AR), Bicalutamide, PROTAC, Prostate cancer, Protein degradation",

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year = "2021",

doi = "10.3390/molecules26092525",

language = "English",

volume = "26",

journal = "Molecules",

issn = "1420-3049",

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AU - Kim, Ga Yeong

AU - Song, Chae Won

AU - Yang, Yo Sep

AU - Lee, Na Rae

AU - Yoo, Hyung Seok

AU - Son, Seung Hwan

AU - Lee, Soo Jin

AU - Park, Jong Seon

AU - Lee, Jong Kil

AU - Inn, Kyung Soo

AU - Kim, Nam Jung

PY - 2021

Y1 - 2021

N2 - A series of PROTACs (PROteolysis-TArgeting Chimeras) consisting of bicalutamide analogs and thalidomides were designed, synthesized, and biologically evaluated as novel androgen receptor (AR) degraders. In particular, we found that PROTAC compound 13b could successfully demonstrate a targeted degradation of AR in AR-positive cancer cells and might be a useful chemical probe for the investigation of AR-dependent cancer cells, as well as a potential therapeutic candidate for prostate cancers.

AB - A series of PROTACs (PROteolysis-TArgeting Chimeras) consisting of bicalutamide analogs and thalidomides were designed, synthesized, and biologically evaluated as novel androgen receptor (AR) degraders. In particular, we found that PROTAC compound 13b could successfully demonstrate a targeted degradation of AR in AR-positive cancer cells and might be a useful chemical probe for the investigation of AR-dependent cancer cells, as well as a potential therapeutic candidate for prostate cancers.

KW - Androgen receptor (AR)

KW - Bicalutamide

KW - PROTAC

KW - Prostate cancer

KW - Protein degradation

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DO - 10.3390/molecules26092525

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SN - 1420-3049

VL - 26

JO - Molecules

JF - Molecules

IS - 9

M1 - 2525

ER -

Chemical degradation of androgen receptor (Ar) using bicalutamide analog–thalidomide protacs

Abstract

Bibliographical note

Keywords

UN SDGs

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