Hit Identification and Screening
Protheragen conducts high-throughput screening (HTS) to identify initial hits that interact with MyD88 and further improve them by employing fragment-based (FBDD) and structure-based (SBDD) drug design.
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Small Molecule Inhibitors Development
Protheragen provides a broad set of services for the development of small molecule inhibitors that target the MyD88 pathway. These inhibitors are central in blocking MyD88 signalling and have great potential in the treatment of inflammatory, autoimmune, infectious, and oncological diseases.
Small Molecule Inhibitors of MyD88
Small molecule inhibitors targeting MyD88 primarily function by targeting its TIR domain and interfering with the interactions between MyD88 and its upstream/downstream molecules. Several representative compounds have been developed, such as T5910047, which inhibits MyD88 dimerization, and ST2825, which blocks MyD88-MyD88 interactions. These drugs show promising applications in treating autoimmune diseases, inflammatory conditions, and certain tumors dependent on MyD88 signaling pathways.
Fig.1 Design principle of the MyD88 inhibitor. (Liu, M., et al., 2023)Advances in MyD88-Targeted Small Molecule Development
Considerable strides have been made in the creation of small molecule inhibitors that target MyD88. In particular, MyD88 protein-protein interactions (PPIs) have been the target in attempts to block and prevent any further signalling events further downstream.
MyD88 PPIs
Recent developments have dealt with small molecules that inhibit MyD88 binding in particular by preventing Myddosome complex formation as well as targeting the TIR domain. They are effective in selectively suppressing the NF-κB signalling cascade together with other mechanisms and have the potential of treating inflammation and immune diseases.
Allosteric Inhibitors
Advancements in structural biology and cheminformatics have enabled the design of allosteric inhibitors that bind to atypical sites on MyD88; these inhibitors are effective against some cancers due to this unique mechanism. They lower MyD88's conformation, preventing interaction with downstream signalling proteins.
L265P Mutation
The MyD88 L265P mutation which is a strong oncogenic driver of lymphoma has been extensively targeted by small molecules as well. Likewise, small molecule inhibitors designed to target specific mutations are being hailed as the future of therapy for individuals with lymphoma that harbours such a mutation.
Our Services
Protheragen is integral to enhancing the therapeutics of MyD88-related diseases as it aims to strengthen the development of MyD88-targeted small molecule inhibitors in the biotechnology field. Our experience covers the whole spectrum of preclinical research development with attention to MyD88-oriented drug discovery.
Workflow of MyD88-Targeted Small Molecule Inhibitors Development
Lead Optimization
Lead optimization is conducted via medicinal chemistry and molecular modelling for increasing potency, selectivity, and favourable pharmacokinetic properties.
Preclinical Development
The compounds of interest for MyD88-related diseases are first evaluated for their safety and efficacy through PK/PD studies, allergy tests, and other preclinical studies before they advance to human testing.
Investigator-Initiated Trials (IIT) Services
Protheragen offers additional concern for IITs like trial structure, regulatory preparation, and other leading structures to assist in progressing MyD88-targeted therapies from preclinical stages to higher clinical stages.
Types of MyD88-Targeted Diseases
- Autoimmune Diseases
- Inflammatory Diseases
- Transplant Rejection
- Ischemia-Reperfusion
- Allergic Diseases
- Cancers
- Neurodegenerative
- Metabolic Diseases
Protheragen takes an aggressive approach to the treatment of MyD88 related diseases and offers a comprehensive range of services, including small molecular inhibitor development, disease model development, pharmacokinetics and drug safety evaluation. We also focus on the initiation of investigator-sponsored trials enabling us to fast-track the preliminary testing process and facilitate the development of new therapies.
If you are interested in our services, please don't hesitate to contact us.
Reference
- Liu, M., et al. "Targeting Myd88: Therapeutic Mechanisms and Potential Applications of the Specific Inhibitor St2825." Inflamm Res 72.10-11 (2023): 2023-36.
All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.