[HTML][HTML] Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy
In the past two decades, we have witnessed the discovery and development of many potent
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
Obesity and prostate cancer—microenvironmental roles of adipose tissue
A Saha, MG Kolonin, J DiGiovanni - Nature Reviews Urology, 2023 - nature.com
Obesity is known to have important roles in driving prostate cancer aggressiveness and
increased mortality. Multiple mechanisms have been postulated for these clinical …
increased mortality. Multiple mechanisms have been postulated for these clinical …
First clinical results for PSMA-targeted α-therapy using 225Ac-PSMA-I&T in advanced-mCRPC patients
MJ Zacherl, FJ Gildehaus, L Mittlmeier… - Journal of Nuclear …, 2021 - Soc Nuclear Med
Treatment of advanced metastatic castration-resistant prostate cancer after failure of
approved therapy options remains challenging. Prostate-specific membrane antigen (PSMA) …
approved therapy options remains challenging. Prostate-specific membrane antigen (PSMA) …
[HTML][HTML] 177 Lu-PSMA-617 radioligand therapy of metastatic castration-resistant prostate cancer: Initial 254-patient results from a prospective registry (REALITY Study)
F Khreish, Z Ghazal, RJ Marlowe, F Rosar… - European Journal of …, 2022 - Springer
Purpose Preliminary data from retrospective analyses and recent data from large
randomized controlled trials suggest safety and efficacy of radioligand therapy (RLT) …
randomized controlled trials suggest safety and efficacy of radioligand therapy (RLT) …
Effects of MTX-23, a novel PROTAC of androgen receptor splice variant-7 and androgen receptor, on CRPC resistant to second-line antiandrogen therapy
GT Lee, N Nagaya, J Desantis, K Madura… - Molecular cancer …, 2021 - AACR
Although second-line antiandrogen therapy (SAT) is the standard of care in men with
castration-resistant prostate cancer (CRPC), resistance inevitably occurs. One major …
castration-resistant prostate cancer (CRPC), resistance inevitably occurs. One major …
[HTML][HTML] Multiplexed functional genomic analysis of 5'untranslated region mutations across the spectrum of prostate cancer
The functional consequences of genetic variants within 5'untranslated regions (UTRs) on a
genome-wide scale are poorly understood in disease. Here we develop a high-throughput …
genome-wide scale are poorly understood in disease. Here we develop a high-throughput …
[HTML][HTML] The androgen receptor in prostate cancer: Effect of structure, ligands and spliced variants on therapy
EA Messner, TM Steele, MM Tsamouri, N Hejazi… - Biomedicines, 2020 - mdpi.com
The androgen receptor (AR) plays a predominant role in prostate cancer (PCa) pathology. It
consists of an N-terminal domain (NTD), a DNA-binding domain (DBD), a hinge region (HR) …
consists of an N-terminal domain (NTD), a DNA-binding domain (DBD), a hinge region (HR) …
Lutetium-177 PSMA for the treatment of metastatic castrate resistant prostate cancer: a systematic review
Introduction Metastatic castrate resistant prostate cancer (mCPRC) remains an aggressive
form of prostate cancer that no longer responds to traditional hormonal treatment alone …
form of prostate cancer that no longer responds to traditional hormonal treatment alone …
Computational drug discovery for castration-resistant prostate cancers through in vitro drug response modeling
Prostate cancer (PC) is the most frequently diagnosed malignancy and a leading cause of
cancer deaths in US men. Many PC cases metastasize and develop resistance to systemic …
cancer deaths in US men. Many PC cases metastasize and develop resistance to systemic …
Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer
L Chen, L Han, S Mao, P Xu, X Xu, R Zhao, Z Wu… - European Journal of …, 2021 - Elsevier
Androgen receptor (AR) is an effective therapeutic target for the treatment of prostate cancer.
We report herein the design, synthesis, and biological evaluation of highly effective …
We report herein the design, synthesis, and biological evaluation of highly effective …