Drug intelligence / Profile preview

balanol

Development stage
Discontinued
Lead developer
Triangle Research Laboratories
Modality
Small Molecules
01

Overview

Balanol is a natural product isolated from the fungus Verticillium balanoides. It is a potent, non-selective ATP-competitive inhibitor of serine/threonine protein kinases, particularly protein kinase A (PKA) and protein kinase C (PKC), as well as other AGC family kinases. Balanol binds to the catalytic domain of these kinases in a manner similar to ATP, thereby preventing phosphorylation of target substrates and inhibiting downstream signaling pathways. It has also been reported to inhibit G protein-coupled receptor kinases (GRKs), with modest selectivity for GRK2 and GRK3. Balanol was originally discovered during efforts to find novel PKC inhibitors due to the role of PKC overactivation in diseases such as cancer. Preclinical studies have explored its anti-inflammatory, antifungal, and antineoplastic properties; however, development was discontinued for indications including cancer, inflammation, and psoriasis[3][5][6][7].

Other names
ophiocordinazepinostatin
02

Targets

PKA (Cyclic amp-dependent protein kinase)GRK3 (G protein-coupled receptor kinase 3)GRK2 (G protein-coupled receptor kinase 2)PKC (Protein kinase C family)

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