Drug intelligence / Profile preview

RTS-V5

Development stage
Preclinical
Lead developer
University of Bonn
Modality
Small Molecules
Administration
Unknown
01

Overview

**RTS-V5** is a first-in-class dual inhibitor targeting both **histone deacetylase (HDAC)**, primarily HDAC6 and HDAC8, and the **chymotrypsin-like activity of the proteasome**. Its mechanism of action is based on simultaneously blocking the ubiquitin-proteasome and aggresome pathways, thereby inducing apoptosis, endoplasmic reticulum stress, unfolded protein response (UPR), and autophagy in cancerous cells. RTS-V5 displays potent and selective anticancer activity against leukemia, multiple myeloma, and bladder cancer cell lines, including those resistant to chemotherapy, while showing low toxicity toward normal peripheral blood mononuclear cells. The drug is structurally validated by co-crystallization with both HDAC6 and the 20S proteasome, confirming its non-covalent binding and specificity. In preclinical studies, RTS-V5 acts synergistically with ritonavir, further enhancing ER stress and apoptosis in bladder cancer models[1][2][3][4].

Brand names
RTS-V5RTS-V-5RTS-V 5
Other names
RTS-V5RTS-V-5RTS-V 5
02

Targets

HDAC2 (Histone deacetylase 2)HDAC1 (Histone Deacetylase 1)HDAC6 (Histone deacetylase 6)HDAC8 (Histone Deacetylase 8)HDAC3 (Histone Deacetylase 3)PSMB5 (Proteasome subunit beta Type-5)

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