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Primary Target

Ubiquitin carboxyl-terminal hydrolase 14

2

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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Investigational

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Phase I

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Refractory cancer

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Primary

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Originator

Karolinska Institute|Vivolux

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Vivolux

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Chemical

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VLX-1570

K6067N5M6N

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

19S-Proteasome Deubiquitinase

Ubiquitin carboxyl-terminal hydrolase 14

Ubiquitin carboxyl-terminal hydrolase isozyme L5

Vivolux developed VLX-1570 as a small molecule proteasome 19S proteasome deubiquitinase (DUB) inhibitor. In addition, VLX1570 shows selectivity for ubiquitin-specific protease-14 and induces apoptosis of multiple myeloma cells. VLX-1570 participated ...

in phase I/II clinical trial in patients with myeloma. However, this study was terminated because of the dose-limiting toxicity was observed. Thus, the full clinical trial was put on hold. VLX1570 also inhibits ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5). Besides, was shown that VLX1570 modulated bio-cellular pathways that were essential for Waldenstrom macroglobulinemia (WM) cell survival. Thus, VLX1570 can be further studied for clinical use in patients with WM.

VLX-600

YZO6DG19MG

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ubiquitin carboxyl-terminal hydrolase 14

Ubiquitin carboxyl-terminal hydrolase isozyme L5

mitochondrial respiratory chain complex IV

Conditions:

Refractory cancer

VLX600 - is a lipophilic cation-based triazinoindolyl-hydrazone compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. VLX600 is designed to increase the efficacy of radiotherapy and to kill c...

ancer cells that survive traditional chemotherapy. VLX 600 is a small molecule that inhibits deubiquitinating enzymes USP14 (a ubiquitin thiolesterase) and UCHL5 (a carboxypeptidase). Upon infusion, in normal cells and proliferating tumor cells where glucose is readily available, inhibition of OxPhos by VLX600 induces a hypoxia-inducible factor 1-alpha (HIF-1alpha)-dependent shift to, and an increase in glycolysis. Glycolysis alone does not produce enough energy to support the growth of tumor cells in this environment, and the induction of autophagy occurs. In the metabolically compromised tumor microenvironment, the availability of oxygen and glucose is limited due to poor vascularization and perfusion of tumor micro-areas. Tumor cells growing in this environment are thus unable to compensate for decreased mitochondrial function by increasing glycolysis. This leads to nutrient depletion, decreased energy production, induction of autophagy, tumor cell death and an inhibition of cell proliferation in quiescent tumor cells. Mitochondrial OxPhos, which is hyperactivated in cancer cells, plays a key role in the promotion of cancer cell proliferation. VLX-600 is in phase I clinical trials for the treatment of solid tumours. This compound was originally jointly discovered and developed by Vivolux and Karolinska Institute.

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