Drug intelligence / Profile preview

RRD2

Development stage
Preclinical
Modality
Small Molecules
01

Overview

RRD2 is a platinum-based antitumor compound belonging to the phosphaplatin class. Unlike traditional platinum drugs like cisplatin, RRD2 primarily targets proteins rather than DNA, making it a promising candidate for cisplatin-resistant cancers. Its diverse antitumor properties include inhibiting human umbilical vein endothelial cell migration and tube formation, and suppressing tumor angiogenesis and growth. RRD2 achieves its effects by lowering gene expression of vascular endothelial growth factors (VEGFs) and the VEGFR-2 receptor, and by inhibiting VEGFR-2 through metal-ligand coordination. It also activates and upregulates death receptors such as FAS, DR5, and TNFR1, triggering apoptosis via the extrinsic pathway. Furthermore, RRD2 downregulates the PTEN-PI3K pathway (PI3K and p-AKT) and upregulates tumor suppression genes P53 and PTEN, leading to apoptosis through p53 signaling involving BCL-proteins (upregulation of BAX, PUMA, and downregulation of BCL2).

02

Targets

DNA

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