Society for Endocrinology - a world-leading authority on hormones


Issue 143 Spring 2022

Endocrinologist > Spring 2022 > Hot topics


ACT001 REVERSES DRUG RESISTANCE OF PROLACTINOMAS

| Hot topics



Prolactinomas are a leading type of pituitary adenoma. Dopamine agonists provide the current mainstay of treatment, in the form of cabergoline or bromocriptine. Unfortunately, approximately 20% of patients do not respond well to these treatment options.

A new study from Zhu et al. shows that ACT001, a derivative of the promising anti-cancer treatment parthenolide, can reverse the resistance of prolactinoma cells to both cabergoline and bromocriptine. More importantly, this has been shown both in cell line studies and in vivo in a mouse model. The proposed method of action includes an increase in reactive oxygen species and inhibition of mTOR to induce cell death in prolactinoma cells through apoptosis.

Parthenolide is a natural product isolated from medicinal herbs, which has already been shown to have a variety of important pharmacological activities, such as anti-cancer roles in breast and prostate cancer. The new structural arrangement improved stability, bioavailability and water solubility to allow crossing of the blood brain barrier, opening up new avenues for treatment options for a wide range of diseases.

Read the full article in Endocrine-Related Cancer 29 33–46




This Issue:

Spring 2022

Spring 2022

The Endocrinologist

...

Autumn 2022

Autumn 2022