Delving into the Latest Updates on CBB-3001 with Synapse

Overview

Basic Info

Drug Type

Chemical drugs

Synonyms

Target

KDM1A

Mechanism

KDM1A inhibitors(Lysine-specific histone demethylase 1 inhibitors)

Therapeutic Areas

NeoplasmsOther Diseases

Active Indication-

Inactive Indication

Embryonal CarcinomaTeratocarcinoma

Originator Organization

University of Nevada

Active Organization-

Inactive Organization

University of Nevada

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

LSD1/KDM1 is a histone demethylase that preferentially removes methyl groups from the mono- and di-methylated lysine 4 in histone H3 (H3K4), key marks for active chromatin for transcriptional activation. LSD1 is essential for pluripotent embryonic stem cells and embryonic teratocarcinoma/carcinoma cells and its expression is often elevated in various cancers. We developed a new LSD1 inhibitor, CBB3001, which potently inhibited LSD1 activity both in vitro and in vivo. CBB3001 also selectively inhibited the growth of human ovarian teratocarcinoma PA-1 and mouse embryonic carcinoma F9 cells, caused the downregulation of pluripotent stem cell proteins SOX2 and OCT4. However, CBB3001 does not have significant inhibition on the growth of human colorectal carcinoma HCT116 cells or mouse fibroblast NIH3T3 cells that do not express these stem cell proteins. Our studies strongly indicate that CBB3001 is a specific LSD1 inhibitor that selectively inhibits teratocarcinoma and embryonic carcinoma cells that express SOX2 and OCT4.

100 Deals associated with CBB-3001

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