PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
durability of their effectiveness can be limited. Resistance to these therapies is often related …
Recent advances in prostate cancer treatment and drug discovery
E Nevedomskaya, SJ Baumgart… - International journal of …, 2018 - mdpi.com
Novel drugs, drug sequences and combinations have improved the outcome of prostate
cancer in recent years. The latest approvals include abiraterone acetate, enzalutamide and …
cancer in recent years. The latest approvals include abiraterone acetate, enzalutamide and …
Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer
We report herein the discovery of highly potent PROTAC degraders of androgen receptor
(AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein …
(AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein …
Strategies toward discovery of potent and orally bioavailable proteolysis targeting chimera degraders of androgen receptor for the treatment of prostate cancer
Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a
promising new type of therapeutic agents, but the design of PROTAC degraders with …
promising new type of therapeutic agents, but the design of PROTAC degraders with …
Genomic alterations in cell-free DNA and enzalutamide resistance in castration-resistant prostate cancer
Importance The molecular landscape underpinning response to the androgen receptor (AR)
antagonist enzalutamide in patients with metastatic castration-resistant prostate cancer …
antagonist enzalutamide in patients with metastatic castration-resistant prostate cancer …
Functional analysis of androgen receptor mutations that confer anti-androgen resistance identified in circulating cell-free DNA from prostate cancer patients
Background The androgen receptor (AR) is a pivotal drug target for the treatment of prostate
cancer, including its lethal castration-resistant (CRPC) form. All current non-steroidal AR …
cancer, including its lethal castration-resistant (CRPC) form. All current non-steroidal AR …
Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation: Miniperspective
S Xie, J Zhu, J Li, F Zhan, H Yao, J Xu… - Journal of Medicinal …, 2023 - ACS Publications
Targeted protein degradation (TPD) technologies have catalyzed a paradigm shift in
therapeutic strategies and offer innovative avenues for drug design. Hydrophobic tags …
therapeutic strategies and offer innovative avenues for drug design. Hydrophobic tags …
[HTML][HTML] Targeting androgen receptor degradation with PROTACs from bench to bedside
X Jia, X Han - Biomedicine & Pharmacotherapy, 2023 - Elsevier
Highlights•AR is a clinically fully validated target for treatment of human prostate
cancer.•PROTAC AR degraders overcome common resistance mechanisms developed …
cancer.•PROTAC AR degraders overcome common resistance mechanisms developed …
Therapeutic strategies to target the androgen receptor
The androgen receptor (AR) plays a key role in the maintenance of muscle and bone and
the support of male sexual-related functions, as well as in the progression of prostate …
the support of male sexual-related functions, as well as in the progression of prostate …
Best practices of computer-aided drug discovery: lessons learned from the development of a preclinical candidate for prostate cancer with a new mechanism of action
Small-molecule drug design is a complex and iterative decision-making process relying on
pre-existing knowledge and driven by experimental data. Low-molecular-weight chemicals …
pre-existing knowledge and driven by experimental data. Low-molecular-weight chemicals …