Drug intelligence / Profile preview

arylpiperazine 5k

Development stage
Preclinical
Lead developer
University of Zurich
Modality
Small Molecules
Administration
Oral
01

Overview

Arylpiperazine 5k is a small molecule inhibitor specifically targeting the fatty acid transporter SLC27A1, also known as Fatty Acid Transport Protein 1 (FATP1). Identified through pharmacological screening, this compound blocks the uptake of long-chain fatty acids into cells. In preclinical models of chronic lymphocytic leukemia (CLL), arylpiperazine 5k has been shown to disrupt metabolic fitness by reducing intracellular fatty acid levels and neutral lipid storage, which in turn impairs mitochondrial respiration and ATP production. This metabolic disruption leads to a significant reduction in leukemic cell proliferation. Furthermore, arylpiperazine 5k exhibits synergistic activity when combined with established CLL therapies such as the BTK inhibitor ibrutinib and the BCL-2 inhibitor venetoclax, highlighting its potential as a novel metabolic-targeted approach to enhance drug sensitivity in high-risk leukemia subsets.

Other names
SLC27A1 inhibitor 5kSLC-27A1 inhibitor 5kSLC 27A1 inhibitor 5kFATP1 inhibitor 5kFATP-1 inhibitor 5kFATP 1 inhibitor 5k
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))SLC27A1 (Long-chain fatty acid transport protein 1)HTR7 (5-hydroxytryptamine receptor 7)ADRA1A (α1A)

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