PROTACS: A technology with a gold rush-like atmosphere
YW Wang, L Lan, M Wang, JY Zhang, YH Gao… - European Journal of …, 2023 - Elsevier
Abnormally expressed or malfunctioning proteins may affect or even damage cells, leading
to the onset of diseases. Proteolysis targeting chimera (PROTAC) technology has been …
to the onset of diseases. Proteolysis targeting chimera (PROTAC) technology has been …
The application of PROTAC in HDAC
S Chen, Y Zheng, B Liang, Y Yin, J Yao, Q Wang… - European Journal of …, 2023 - Elsevier
Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great
opportunities for scientific research and industrial applications. Histone deacetylase (HDAC) …
opportunities for scientific research and industrial applications. Histone deacetylase (HDAC) …
Discovery of ERD-3111 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader with Strong Antitumor Activity
Estrogen receptor α (ERα) is a prime target for the treatment of ER-positive (ER+) breast
cancer. Despite the development of several effective therapies targeting ERα signaling …
cancer. Despite the development of several effective therapies targeting ERα signaling …
Application and challenges of nitrogen heterocycles in PROTAC linker
Y Li, J Qu, L Jiang, X Peng, K Wu, M Chen… - European Journal of …, 2024 - Elsevier
The absence of effective active pockets makes traditional molecularly targeted drug
strategies ineffective against 80% of human disease-related proteins. The PROTAC …
strategies ineffective against 80% of human disease-related proteins. The PROTAC …
[HTML][HTML] MAF amplification licenses ERα through epigenetic remodelling to drive breast cancer metastasis
A Llorente, MT Blasco, I Espuny, M Guiu, C Ballaré… - Nature Cell …, 2023 - nature.com
MAF amplification increases the risk of breast cancer (BCa) metastasis through mechanisms
that are still poorly understood yet have important clinical implications. Oestrogen-receptor …
that are still poorly understood yet have important clinical implications. Oestrogen-receptor …
PROTACs: A novel strategy for cancer drug discovery and development
Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …
[HTML][HTML] Synthesis and biological activity of a VHL-based PROTAC specific for p38α
M Cubillos-Rojas, G Loren, YZ Hakim, X Verdaguer… - Cancers, 2023 - mdpi.com
Simple Summary The compounds named PROTACs are formed by two fragments, which
bring together a particular protein with a ubiquitinating enzyme. This allows ubiquitination …
bring together a particular protein with a ubiquitinating enzyme. This allows ubiquitination …
The crosstalk between ubiquitination and endocrine therapy
Y Ge, Z Zhan, M Ye, X Jin - Journal of Molecular Medicine, 2023 - Springer
Endocrine therapy (ET), also known as hormone therapy, refers to the treatment of tumors by
regulating and changing the endocrine environment and hormone levels. Its related …
regulating and changing the endocrine environment and hormone levels. Its related …
Click Chemistry and Targeted Degradation: A Winning Combination for Medicinal Chemists?
A Pasieka, E Diamanti, E Uliassi… - …, 2023 - Wiley Online Library
Click chemistry is universally recognized as a powerful strategy for the fast and precise
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …
Estrogen receptor alpha mutations, truncations, heterodimers, and therapies
GR Hancock, J Gertz, R Jeselsohn… - Endocrinology, 2024 - academic.oup.com
Annual breast cancer (BCa) deaths have declined since its apex in 1989 concomitant with
widespread adoption of hormone therapies that target estrogen receptor alpha (ERα), the …
widespread adoption of hormone therapies that target estrogen receptor alpha (ERα), the …