Advances in targeting 'undruggable'transcription factors with small molecules
MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
Induced protein degradation for therapeutics: past, present, and future
The concept of induced protein degradation by small molecules has emerged as a
promising therapeutic strategy that is particularly effective in targeting proteins previously …
promising therapeutic strategy that is particularly effective in targeting proteins previously …
Discovery of ARD-2585 as an exceptionally potent and orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer
We report herein the discovery of exceptionally potent and orally bioavailable PROTAC AR
degraders with ARD-2585 being the most promising compound. ARD-2585 achieves DC50 …
degraders with ARD-2585 being the most promising compound. ARD-2585 achieves DC50 …
The IUPHAR/BPS Guide to PHARMACOLOGY in 2020: extending immunopharmacology content and introducing the IUPHAR/MMV Guide to MALARIA …
JF Armstrong, E Faccenda, SD Harding… - Nucleic acids …, 2020 - academic.oup.com
Abstract The IUPHAR/BPS Guide to PHARMACOLOGY (www. guidetopharmacology. org) is
an open-access, expert-curated database of molecular interactions between ligands and …
an open-access, expert-curated database of molecular interactions between ligands and …
Discovery of ARD-1676 as a highly potent and orally efficacious AR PROTAC degrader with a broad activity against AR mutants for the treatment of AR+ human …
We report herein the discovery and extensive characterization of ARD-1676, a highly potent
and orally efficacious PROTAC degrader of the androgen receptor (AR). ARD-1676 was …
and orally efficacious PROTAC degrader of the androgen receptor (AR). ARD-1676 was …
Gender differences in the pathogenesis and risk factors of hepatocellular carcinoma
Simple Summary Significant gender disparities have been highlighted in the incidence,
aggressiveness, and prognosis of HCC. A different epidemiological distribution of the risk …
aggressiveness, and prognosis of HCC. A different epidemiological distribution of the risk …
Inhibiting androgen receptor splice variants with cysteine-selective irreversible covalent inhibitors to treat prostate cancer
T Thiyagarajan, S Ponnusamy… - Proceedings of the …, 2023 - National Acad Sciences
Androgen receptor (AR) and its splice variants (AR-SVs) promote prostate cancer (PCa)
growth by orchestrating transcriptional reprogramming. Mechanisms by which the low …
growth by orchestrating transcriptional reprogramming. Mechanisms by which the low …
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 …
A comprehensive overview of small-molecule androgen receptor degraders: Recent progress and future perspectives
S Ha, G Luo, H Xiang - Journal of medicinal chemistry, 2022 - ACS Publications
Prostate cancer (PC), the second most prevalent malignancy in men worldwide, has been
proven to depend on the aberrant activation of androgen receptor (AR) signaling. Long-term …
proven to depend on the aberrant activation of androgen receptor (AR) signaling. Long-term …
An overview of next-generation androgen receptor-targeted therapeutics in development for the treatment of prostate cancer
Traditional endocrine therapy for prostate cancer (PCa) has been directed at suppression of
the androgen receptor (AR) signaling axis since Huggins et al. discovered that …
the androgen receptor (AR) signaling axis since Huggins et al. discovered that …