CRB3 Inhibitors

CRB3 inhibitors constitute a diverse class of compounds designed to modulate the activity of Crumbs homolog 3 (CRB3), a transmembrane protein involved in cell polarity and adhesion. Among these inhibitors, Neferine, Statins, Verteporfin, Simvastatin, Farnesylthiosalicylic acid (FTS), A-769662, GGTI-298, GGTI-2417, and others have been identified as potential agents to influence CRB3 function. These inhibitors act through various mechanisms, providing valuable insights into the regulation of CRB3-mediated cellular processes. Neferine, for instance, indirectly inhibits CRB3 by targeting components of the Hippo signaling pathway, such as MST1/2 or YAP/TAZ, disrupting the signaling cascade that impacts CRB3 activity. Statins, known cholesterol-lowering drugs, indirectly modulate CRB3 by interfering with the mevalonate pathway, affecting the prenylation of small GTPases crucial for CRB3 function. Verteporfin, a photosensitizer, indirectly inhibits CRB3 by disrupting the interaction between YAP/TAZ and TEAD transcription factors, key players in the Hippo pathway regulating CRB3.

Simvastatin and FTS interfere with the mevalonate pathway and protein farnesylation, respectively, indirectly influencing CRB3 activity by modulating the membrane association of small GTPases. A-769662, an AMPK activator, indirectly inhibits CRB3 by regulating cellular energy sensing pathways. GGTI-298 and GGTI-2417, inhibitors of geranylgeranyltransferase I, indirectly modulate CRB3 by disrupting the geranylgeranylation of small GTPases involved in CRB3 regulation. Collectively, these CRB3 inhibitors offer a molecular toolkit to investigate the consequences of altered CRB3 function, providing valuable insights into the regulation of cell polarity and adhesion processes. The diverse mechanisms employed by these inhibitors contribute to a nuanced understanding of the intricate pathways governing CRB3-mediated cellular functions.