Overview

Protein-protein interactions (PPIs) regulate various physiological processes and are implicated in a wide range of diseases, which are effective targets for therapeutic drug interventions. The development of PPI inhibitors has a crucial role to play in PPI interactions and the study of new therapies and drugs targeting PPIs involved in cancer. PPI-based inhibitor discovery is challenging due to its potential for interfacial accessibility changes, event-driven conformational changes, and lack of a rational starting point for drug design. DNA-encoded glycan library (DEGL), an affinity-based selection process, is considered to be a powerful tool for PPI inhibitor discovery. CD BioGlyco offers innovative and customized DEGL screening solutions to discover PPI inhibitors. With in-depth knowledge of the mechanism of action of the target PPI and the rational design of compound libraries, DEGL provides selective hits with desirable mechanisms and potentially specified functions.

Revolutionize the PPI Inhibitor Study: Try our DEGL screening solutions!

We expand the selection to different interactions with different proteins and all possible conformational changes to facilitate a realistic simulation of the PPI process and maximize the chances of identifying PPI inhibitors with good affinity and properties. With an efficient DEGL screening protocol, a deep understanding of the mechanism of action of PPI targets, and various orders of magnitude of DEGL, the discovery of PPI inhibitors is designed to be more efficient and simple. The specific experimental procedure is as follows:

Library Design and Construction

We design and synthesize a diverse library of glycan structures based on the PPI mechanism of action, protein binding properties, etc., and bind each glycan to a unique DNA tag. The DEGL construction methods include solid-phase synthesis, liquid-phase synthesis, etc. Based on our industry-leading synthesis capabilities, we custom synthesize various quantities of DEGLs to maximize hit rates.

High-throughput Screening of DEGL

This process involves incubation of the target library, removal of unbound molecules, and recovery of bound molecules. Each step is critical to obtaining potential hits. Elution of unbound molecules is followed by polymerase chain reaction (PCR) amplification for sequencing. There must be a range of copy numbers in the sample to achieve high efficiency in data usage. We also monitor this by using quantitative real-time PCR (qPCR). After amplification, we use next-generation sequencing (NGS) for decoding.

Data Analysis

The screening data is essential information to further explore the potential of PPI targets and provide direction for compound optimization. We use efficient bioinformatics tools and match recognition algorithms to increase the rate of analysis of screening data.

Hit Validation and Evaluation

Our experienced chemists select representative DEGL theoretical end-product molecules for organic synthesis validation. This validation and evaluation include physical and biochemical analyses, potency analysis of PPI inhibitors, selectivity, lead compound optimization, and more.

Workflow

We synthesize diverse DEGLs and perform high-throughput screening targeting PPIs for potential therapeutic agents through medicinal chemistry optimization.

Applications

• The discovery of PPI inhibitors through DEGL screening contributes to a better understanding of the mechanism of PPI action.
• DEGL screening discovers and develops PPI inhibitors in a high-throughput manner, thereby facilitating the development of therapeutic drugs for cancer, and other therapeutic areas.
• Hit compounds identified through DEGL screening can be further optimized through medicinal chemistry studies to increase their potency, thereby contributing to the development of more potent PPI inhibitors and drugs.

Advantages

• Our larger and more diverse DEGL library increases the opportunity to discover novel PPI inhibitors with high potency and selectivity.
• We have extensive experience in DEGL screening and PPI inhibitor research, tailoring appropriate screening strategies to our client's research objectives.
• We communicate regularly on the progress of DEGL screening, and hit identification, and are always available to answer clients' various project-related questions.

Publication Data

Frequently Asked Questions

• What is the correlation between PPIs and disease?
  • PPI is the process by which two or more protein molecules form a protein complex through non-covalent bonds. It forms a major component of the cellular biochemical response network and is important in regulating the cell and its signaling. Several PPI networks have been shown to play a role in tumor development and are considered potential tumor targets. Screening of PPI inhibitors provides a structural basis for the design and development of PPI-based drugs.
• What studies is DEGL screening suitable for?
  • We customize DEGL to meet our client's research needs and offer DEGL screening solutions for the following studies:
  • DEGL Screening for Glycan-Protein Interaction Study
  • DEGL Screening for PPI Discovery
  • DEGL Screening for G Protein-coupled Receptor-Binding Compounds Discovery
  • DEGL Screening for Protein Ubiquitination Study
  • DEGL Screening for Bacterial Enzyme Study
  • DEGL Screening for Antibody Target Identification
  • DEGL Screening for Protein-templated Ligand Discovery

As an innovative approach, DEGL screening analyses large libraries of compounds in a high-throughput manner, potentially identifying novel PPI inhibitors with improved specificity. CD BioGlyco offers efficient, customized DEGL screening solutions for PPI inhibitor discovery to explore drug development. Welcome to contact us for customized DEGL and screening strategies for PPI inhibitor discovery.

• Magnetic Bead-based DEGL Affinity Screening
• Resin Tip-based DEGL Affinity Screening
• Interaction-dependent PCR (IDPCR)-based DEGL Screening
• DNA Photoaffinity Labeling-based DEGL Screening
• Microfluidic Processor-based DEGL Screening
• Cell-based DEGL Screening
• DNA Programmed Affinity Labelling (DPAL)-based DEGL Screening
• DEGL Screening for Glycan-Protein Interaction Study
• DEGL Screening for G Protein-coupled Receptor-Binding Compounds Discovery
• DEGL Screening for Protein Ubiquitination Study
• DEGL Screening for Bacterial Enzyme Study
• DEGL Screening for Antibody Target Identification
• DEGL Screening for Protein-templated Ligand Discovery