CFTR modulators(Cystic fibrosis transmembrane conductance regulator modulators), Sodium-hydrogen exchangers modulators, chloride channel modulators(Chloride channel modulators)

Therapeutic Areas

Digestive System DisordersOther Diseases

Active Indication

Irritable Bowel SyndromeConstipation

Inactive Indication-

Originator Organization

University of Florida Research Foundation, Inc.

Active Organization

Nuvara Therapeutics

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with VS-013

100 Translational Medicine associated with VS-013

100 Patents (Medical) associated with VS-013

Literatures (Medical) associated with VS-013

01 Jan 2021·Journal of Enzyme Inhibition and Medicinal ChemistryQ2 · MEDICINE

Identification of histone deacetylase inhibitors with (arylidene)aminoxy scaffold active in uveal melanoma cell lines

Q2 · MEDICINE

ArticleOA

Author: Cuffaro, Doretta ; Orlandini, Elisabetta ; Fabbi, Marina ; Nuti, Elisa ; Ortore, Gabriella ; Campelli, Francesco ; Ciccone, Lidia ; Nencetti, Susanna ; Gangemi, Rosaria ; Ballante, Flavio ; Rossello, Armando ; Carbotti, Grazia ; Banti, Irene ; Marshall, Garland R.

Uveal melanoma (UM) represents an aggressive type of cancer and currently, there is no effective treatment for this metastatic disease. In the last years, histone deacetylase inhibitors (HDACIs) have been studied as a possible therapeutic treatment for UM, alone or in association with other chemotherapeutic agents. Here we synthesised a series of new HDACIs based on the SAHA scaffold bearing an (arylidene)aminoxy moiety. Their HDAC inhibitory activity was evaluated on isolated human HDAC1, 3, 6, and 8 by fluorometric assay and their binding mode in the catalytic site of HDACs was studied by molecular docking. The most promising hit was the quinoline derivative VS13, a nanomolar inhibitor of HDAC6, which exhibited a good antiproliferative effect on UM cell lines at micromolar concentration and a capability to modify the mRNA levels of HDAC target genes similar to that of SAHA.

01 Sep 2020·Journal of Molecular Graphics and ModellingQ4 · BIOLOGY

Identification of potential indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors by an FBG-based 3D QSAR pharmacophore model

Q4 · BIOLOGY

Article

Author: Zhang, Lu ; Chen, Xiaoguang ; Xiao, Zhiyan ; Lai, Fangfang

As a rate-limiting enzyme in the major pathway of l-tryptophan catabolism, indoleamine 2, 3-dioxygenase 1 (IDO1) has been regarded as a potential target for the treatment of a variety of diseases. To identify the key molecular features and extend the structural variety of IDO1 inhibitors, a ferrous binding group (FBG)-based 3D-QSAR pharmacophore model was constructed, validated and used for virtual screening herein. The Specs database was initially filtered based on drug-like rules, and was subsequently screened by the pharmacophore model. Molecular docking simulations and similarity analysis were then followed to prioritize twenty compounds for biological tests. Among them, compound VS-13 exhibited moderate inhibitory activity against IDO1, and could be subjected to further structure-activity relationship studies and structural optimization.

100 Deals associated with VS-013

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Irritable Bowel Syndrome	Preclinical	US	Nuvara Therapeutics	30 Jan 2022
Constipation	Preclinical	US	Nuvara Therapeutics	-

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