Drug intelligence / Profile preview

prolame

Development stage
Preclinical
Lead developer
Linnaeus Therapeutics, Inc.
Modality
Small Molecules
01

Overview

Prolame is a synthetic 17β-aminoestrogen and an analog of 17β-estradiol (E2) that acts as a ligand for the G-protein-coupled receptor for estrogen (GPER1), also known as GPR30. It is part of a series of aminoestrogens, including butolame and pentolame, being investigated for potential use in hormone replacement therapy (HRT). Molecular docking studies indicate that prolame binds to a hydrophobic cavity within GPER1, similar to the natural ligand E2 and the specific agonist G1. Unlike some of its analogs, prolame has been shown to induce cell proliferation in breast (MCF-7) and cervical (SIHA) cancer cell lines, which may limit its therapeutic profile due to the risk of promoting tumor growth.

Other names
17β-aminoestrogenN-propyl-1,3,5(10)-estratrien-3-ol-17β-amineN-propyl-17β-aminoestradiol
02

Targets

GPER1 (G protein-coupled estrogen receptor 1)ER (Estrogen receptor)

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