Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer
CBP/p300 are critical transcriptional coactivators of the androgen receptor (AR) and are
promising cancer therapeutic targets. Herein, we report the discovery of highly potent …
promising cancer therapeutic targets. Herein, we report the discovery of highly potent …
Discovery of CBPD-268 as an exceptionally potent and orally efficacious CBP/p300 PROTAC degrader capable of achieving tumor regression
CBP/p300 proteins are key epigenetic regulators and promising targets for the treatment of
castration-resistant prostate cancer and other types of human cancers. Herein, we report the …
castration-resistant prostate cancer and other types of human cancers. Herein, we report the …
Discovery of exceptionally potent, selective, and efficacious PROTAC degraders of CBP and p300 proteins
The histone acetyltransferase CREB-binding protein (CBP) and its paralogue p300 protein
are key transcriptional coactivators and attractive cancer therapeutic targets. We describe …
are key transcriptional coactivators and attractive cancer therapeutic targets. We describe …
[PDF][PDF] Characterisation of CCS1477: A novel small molecule inhibitor of p300/CBP for the treatment of castration resistant prostate cancer
N Pegg, N Brooks, J Worthington, B Young… - J. Clin …, 2017 - cellcentric.com
Bicalutamide resistant LNCaP tumour bearing athymic nude mice were treated with
Enzalutamide by oral gavage, once daily (4mg/kg), or CCS1477 by oral gavage, once daily …
Enzalutamide by oral gavage, once daily (4mg/kg), or CCS1477 by oral gavage, once daily …
Y08197 is a novel and selective CBP/EP300 bromodomain inhibitor for the treatment of prostate cancer
L Zou, Q Xiang, X Xue, C Zhang, C Li, C Wang… - Acta Pharmacologica …, 2019 - nature.com
In advanced prostate cancer, CREB (cAMP-responsive element-binding protein) binding
protein (CBP) and its homolog EP300 are highly expressed; targeting the bromodomain of …
protein (CBP) and its homolog EP300 are highly expressed; targeting the bromodomain of …
Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity
J Hu, H Xu, T Wu, C Zhang, H Shen… - Journal of Medicinal …, 2024 - ACS Publications
The transcriptional coactivator cAMP response element binding protein (CREB)-binding
protein (CBP) and its homologue p300 have emerged as attractive therapeutic targets for …
protein (CBP) and its homologue p300 have emerged as attractive therapeutic targets for …
Therapeutic targeting of the CBP/p300 bromodomain blocks the growth of castration-resistant prostate cancer
L Jin, J Garcia, E Chan, C de la Cruz, E Segal… - Cancer research, 2017 - AACR
Resistance invariably develops to antiandrogen therapies used to treat newly diagnosed
prostate cancers, but effective treatments for castration-resistant disease remain elusive …
prostate cancers, but effective treatments for castration-resistant disease remain elusive …
Targeting the p300/CBP axis in lethal prostate cancer
J Welti, A Sharp, N Brooks, W Yuan, C McNair… - Cancer Discovery, 2021 - AACR
Resistance to androgen receptor (AR) blockade in castration-resistant prostate cancer
(CRPC) is associated with sustained AR signaling, including through alternative splicing of …
(CRPC) is associated with sustained AR signaling, including through alternative splicing of …
Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma
Q Chang, J Li, Y Deng, R Zhou, B Wang… - Journal of Medicinal …, 2024 - ACS Publications
Adenoviral E1A binding protein 300 kDa (p300) and its closely related paralog CREB
binding protein (CBP) are promising therapeutic targets for human cancer. Here, we report …
binding protein (CBP) are promising therapeutic targets for human cancer. Here, we report …
CBP/p300: critical co-activators for nuclear steroid hormone receptors and emerging therapeutic targets in prostate and breast cancers
Simple Summary The CREB-binding protein (CBP) and p300 are paralogous lysine
acetyltransferases that serve as critical co-activators for transcription factors involved in …
acetyltransferases that serve as critical co-activators for transcription factors involved in …
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