Histamine H3 receptor expression in triple negative breast cancer: therapeutic opportunity with pharmacological inhibition.

MONICA TAQUEZ DELGADO; MELISA N NICOUD; IGNACIO OSPITAL; MICHELLE F. CORRÊA; GUSTAVO A. B. FERNANDES; DANIELA SPEISKY; JOÃO P. S. FERNANDES; VANINA A MEDINA

Congreso; LXVII Reunión Anual de la SAIC, Sociedad Argentina de Investigación Clínica; 2022

Triple-negative breast cancer (TNBC) accounts for 10-15% of incident breast cancers and lacks specifically targeted and effective therapy, exhibiting the worst prognosis. We have previously reported the expression of the histamine H3 receptor (H3R) in benign and malignant lesions, and cell lines derived from human mammary glands. In this work, we aimed at evaluating the expression of H3R specifically in TNBC samples and cell lines and investigating the antitumoral properties of a series of 10 H3R antagonists, 1-(2,3-dihydro-1-benzofuran-2-yl)methylpiperazines (LINS01 compounds).1,2 Analysis of the TCGA Pan-Cancer Atlas data set showed that H3R mRNA expression was higher in the aggressive basal-like/TNBC tumors compared with the most favorable clinical outcome luminal subtype (P