GlycoCLICK™-based Protein Tyrosine Phosphatase (PTP) Inhibitor Development Service

GlycoCLICK™-based Protein Tyrosine Phosphatase (PTP) Inhibitor Development Service

Your Satisfaction Is the Driving Force of Our Protein Tyrosine Phosphatase (PTP) Inhibitor Development Work

CD BioGlyco is skilled in the Development of Drugs such as Enzyme Inhibitors using a variety of click chemistry reactions. PTP catalyzes the dephosphorylation of phosphotyrosine residues in protein substrates and is an important class of signaling enzymes. We provide a high-quality GlycoCLICK™-based PTP inhibitor development service to support our client's research needs on PTP and its inhibitors. We use various click chemistry to synthesize glycoconjugates with different structures and develop inhibitors specific to the type of PTP. Our development strategies are as follows:

  • Galactosyl, triazolyl glucosyl, and mannosyl threonine and serine derivatives are found to be potent PTP inhibitors. We synthesize these derivatives by introducing alkyne amino acids onto different azido sugar templates via click chemistry.
  • We synthesize a library of benzyl 6-triazole (hydroxy)benzoic glucosides by copper(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). These glycoconjugates with sugar, (hydroxy)-benzoic derivatives, and alkyl chain are novel PTP inhibitors.
  • We synthesize triazole-linked phenylalanine and tyrosine-aryl C-glycoside hybrids by a microwave-assisted click reaction. The glycoconjugates partially containing benzyl and carboxylic acid portions are efficient and specific PTP inhibitors.
  • We incorporate one or two phenylalanines or tyrosines into the glucosyl scaffolds by methods such as microwave-assisted Cu. The ultimately synthesized tyrosine-based, mono- and bis-phenylalanine-based glucoside derivatives are potent PTP inhibitors.
  • We synthesize glycoconjugates of the triazolyl α-ketocarboxylic acids derivatives via CuAAC.
  • We synthesize a series of triazole-linked phenylalanyl, threonyl, serine, and tyrosyl 1-O-gluco- or galactosides by microwave-accelerated CuAAC. These glycopeptidotriazoles are potent PTP inhibitors.
  • Dimeric benzoylated β-C-D-glycosyl 1,4-dimethoxybenzenes or 1,4-benzoquinones are found to be good inhibitors of PTP1B. We synthesize various derivatives by click chemistry.

Strategies for PTP inhibitor development.

Publication Data

Technology: CuAAC

Journal: Journal of Heterocyclic Chemistry

IF: 0.873

Published: 2013

Results: In this study, several novel mono- or ditriazolyl, or bis-triazolyl amino acid derivatives were synthesized by microwave-assisted CuAAC, and their inhibitory activities against PTP were examined. The researchers found that some compounds had good inhibitory activity and specificity against PTP. This study provides an effective idea for the development of PTP inhibitors.

Fig.1 Reaction conditions and reagents used in the synthesis of PPT inhibitors.Fig.1 The synthesis of PPT inhibitors. (Cui, et al., 2013)

Applications

  • The developed PTP inhibitor is used to study the function of PTP in organisms.
  • The developed PTP inhibitor is used to study the mechanism of disease occurrence associated with PTP.
  • The developed PTP inhibitor plays an important role in the research of therapeutic approaches for diseases.

Advantages of Us

  • We synthesize highly efficient and well-specific PTP inhibitors through various click chemistry reactions.
  • Our PTP inhibitor syntheses are fast and easy to perform.
  • We use the highest quality reagents and follow strict quality control procedures to ensure the consistency and reproducibility of our PTP inhibitors.
  • We use various tools such as high-throughput screening and computer-aided drug design in the development of PTP inhibitors.

Frequently Asked Questions

  • What is the mechanism of action of PTP?

PTP is a signaling enzyme that controls several chemical processes. Its abnormalities lead to various diseases such as cancer, obesity, and diabetes. Phosphorylation of threonine, serine, tyrosine residues, etc. is found to be an important regulatory mechanism of PTP.

  • What are some ideas for PTP inhibitor development?
    • Screening of PTP inhibitors from natural compounds
    • Design and synthesis of compounds that bind to the PTP active site to exert inhibitory effects
    • Design and synthesis of compounds with dual affinity for the PTP active site and related sites
    • Design and synthesis of non-competitive inhibitors of PTP
    • Other ideas

At CD BioGlyco, our highly skilled research team utilizes state-of-the-art technology and equipment to deliver high-quality click chemistry solutions. Please feel free to contact us to learn more about PTP inhibitor development. Our team of scientists will be the first to respond to all your questions.

Reference

  1. Cui, L.; et al. Click synthesis of triazolyl phenylalaninyl and tyrosinyl derivatives as new protein tyrosine phosphatase inhibitors. Journal of Heterocyclic Chemistry. 2013, 50(3): 684-688.
For research use only. Not intended for any clinical use.
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