Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021
Q Wu, W Qian, X Sun, S Jiang - Journal of hematology & oncology, 2022 - Springer
Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …
Emerging mechanisms of resistance to androgen receptor inhibitors in prostate cancer
PA Watson, VK Arora, CL Sawyers - Nature Reviews Cancer, 2015 - nature.com
During the past 10 years, preclinical studies implicating sustained androgen receptor (AR)
signalling as the primary driver of castration-resistant prostate cancer (CRPC) have led to …
signalling as the primary driver of castration-resistant prostate cancer (CRPC) have led to …
Targeting androgen receptor phase separation to overcome antiandrogen resistance
Patients with castration-resistant prostate cancer inevitably acquire resistance to
antiandrogen therapies in part because of androgen receptor (AR) mutations or splice …
antiandrogen therapies in part because of androgen receptor (AR) mutations or splice …
SOX2 promotes lineage plasticity and antiandrogen resistance in TP53- and RB1-deficient prostate cancer
Some cancers evade targeted therapies through a mechanism known as lineage plasticity,
whereby tumor cells acquire phenotypic characteristics of a cell lineage whose survival no …
whereby tumor cells acquire phenotypic characteristics of a cell lineage whose survival no …
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 …
Tumor microenvironment-derived NRG1 promotes antiandrogen resistance in prostate cancer
Despite the development of second-generation antiandrogens, acquired resistance to
hormone therapy remains a major challenge in treating advanced prostate cancer. We find …
hormone therapy remains a major challenge in treating advanced prostate cancer. We find …
AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer
Background The androgen-receptor isoform encoded by splice variant 7 lacks the ligand-
binding domain, which is the target of enzalutamide and abiraterone, but remains …
binding domain, which is the target of enzalutamide and abiraterone, but remains …
Prospective genomic profiling of prostate cancer across disease states reveals germline and somatic alterations that may affect clinical decision making
Purpose A long natural history and a predominant osseous pattern of metastatic spread are
impediments to the adoption of precision medicine in patients with prostate cancer. To …
impediments to the adoption of precision medicine in patients with prostate cancer. To …
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 …
Androgen receptor signaling pathway in prostate cancer: from genetics to clinical applications
Around 80–90% of prostate cancer (PCa) cases are dependent on androgens at initial
diagnosis; hence, androgen ablation therapy directed toward a reduction in serum …
diagnosis; hence, androgen ablation therapy directed toward a reduction in serum …