Last update 21 Nov 2024

Fosfosal

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fosfosal (INN)

+ [2]

Target-

Mechanism-

Therapeutic Areas

Nervous System Diseases

Active Indication

Pain

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure

Molecular FormulaC7H7O6P

InChIKeyFFKUDWZICMJVPA-UHFFFAOYSA-N

CAS Registry6064-83-1

100 Clinical Results associated with Fosfosal

100 Translational Medicine associated with Fosfosal

100 Patents (Medical) associated with Fosfosal

Literatures (Medical) associated with Fosfosal

17 Aug 2020·ChemBioChemQ4 · BIOLOGY

The Selectivity of Fosfosal for STAT5b over STAT5a is Mediated by Arg566 in the Linker Domain

Q4 · BIOLOGY

Article

Author: Gräb, Julian ; Berg, Thorsten

AbstractFosfosal is the O‐phosphorylated derivative of salicylic acid, with documented clinical use as a prodrug for the treatment of inflammatory diseases. We recently discovered that fosfosal itself inhibits the protein‐protein interaction domain, the SH2 domain, of the tumor‐related transcription factor STAT5b. Here, we demonstrate that fosfosal is selective for STAT5b over its close homologue STAT5a. This selectivity is mediated by the STAT5b residue Arg566, located in the SH2 domain‐adjacent linker domain. Our data provide further evidence for the role of the STAT linker domain in determining the activity of small molecules against the SH2 domain. We present a refined binding model for fosfosal and STAT5b, which can serve as the basis for the development of fosfosal‐based STAT5b inhibitors.

22 Jul 2016·ACS SensorsQ1 · CHEMISTRY

Detection of Alkaline Phosphatase Enzyme Activity with a CatalyCEST MRI Biosensor

Q1 · CHEMISTRY

Article

Author: Mohammadebrahim Ghaffari, Mahsa ; Jones, Kyle M. ; Pagel, Mark D. ; Daryaei, Iman

Responsive CEST MRI biosensors offer good sensitivity and excellent specificity for detection of biomarkers with great potential for clinical translation. We report the application of fosfosal, a phosphorylated form of salicylic acid, for the detection of alkaline phosphatase (AP) enzyme. We detected conversion of fosfosal to salicylic acid in the presence of the enzyme by CEST MRI. Importantly the technique was able to detect AP enzyme expressed in cells in the presence of other cell components, which improves specificity. Various isoforms of the enzyme showed different Michaelis-Menten kinetics and yet these kinetics studies indicated very efficient catalytic rates. Our results with the fosfosal biosensor encourage further in vivo studies.

21 Oct 2011·ACS Chemical BiologyQ2 · BIOLOGY

Selective Targeting of Disease-Relevant Protein Binding Domains byO-Phosphorylated Natural Product Derivatives

Q2 · BIOLOGY

Letter

Author: Elumalai, Nagarajan ; Janczyk, Weronika ; Gräber, Martin ; Hausch, Felix ; Kozany, Christian ; Sperl, Bianca ; Holak, Tad A. ; Berg, Thorsten

Phosphorylation-dependent protein binding domains are crucially important for intracellular signaling pathways and thus highly relevant targets in chemical biology. By screening of chemical libraries against 12 structurally diverse phosphorylation-dependent protein binding domains, we have identified fosfosal and dexamethasone-21-phosphate as selective inhibitors of two antitumor targets: the SH2 domain of the transcription factor STAT5b and the substrate-binding domain of the peptidyl-prolyl isomerase Pin1, respectively. Both compounds are phosphate prodrugs with documented clinical use as anti-inflammatory agents in humans and were discovered with a high hit rate from a small subgroup within the screening library. Our study indicates O-phosphorylation of appropriately preselected natural products or natural product derivatives as a generally applicable strategy for the identification of non-reactive and non-peptidic ligands of phosphorylation-dependent protein binding domains. Moreover, our data indicate that it would be advisable to monitor the bioactivities of clinically used prodrugs in their uncleaved state against phosphorylation-dependent protein binding domains.

100 Deals associated with Fosfosal

External Link

KEGG	Wiki	ATC	Drug Bank
D07991	-	N02	-

R&D Status

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Indication	Country/Location	Organization	Date
Pain	-	-	-

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