Approximately 75% of breast cancers are estrogen receptor alpha-positive (ERα+), and targeting ERα directly with ERα antagonists/degraders or indirectly with aromatase inhibitors is a successful therapeutic strategy. However, such treatments are rarely curative and development of resistance is universal. We recently reported ErSO, a compound that induces ERα-dependent cancer cell death through a mechanism distinct from clinically approved ERα drugs, via hyperactivation of the anticipatory unfolded protein response. ErSO has remarkable tumor-eradicative activity in multiple ERα+ tumor models. While ErSO has promise as a new drug, it has effects on ERα-negative (ERα−) cells in certain contexts. Herein, we construct modified versions of ErSO and identify variants with enhanced differential activity between ERα+ and ERα– cells. We report ErSO-DFP, a compound that maintains antitumor efficacy, has enhanced selectivity for ERα+ cancer cells, and is well tolerated in rodents. ErSO-DFP and related compounds represent an intriguing new class for the treatment of ERα+ cancers.
Approximately 75% of breast cancers are of a certain type.
We know of ways to target this type of cancer directly and indirectly.
However, these methods rarely fully cure the problem, and the patient eventually develops a resistance to these treatments, which makes continued use less effective.
We recently examined and reported on a drug which targets this common cancer type in a novel way and is remarkably effective.
However, that drug also interacts with non-cancerous cells in certain contexts, which ideally you want a cancer-targeting drug to avoid wherever possible.
We examine and report on a variant of this drug that is similarly effective but is less likely to target non-cancerous cells.
It is tolerated well in rodents, and this drug and related drugs are worth exploring for treating this cancer type.
The abstract from that linked page:
Not that I have any idea what that says…