Protein-protein interactions (PPIs) play a key role in cellular signaling, the most common of which is the PDZ structural domain. PDZ domains are abundant protein interaction modules that enable to recognize short amino acid motifs at the C-termini of target proteins. These domains can recognize short C-terminal peptide ligands due to their well-defined binding sites. In addition to this, aberrant PPIs have a non-negligible role and PDZ domains are associated with diseases such as cancer, cystic fibrosis, schizophrenia, Alzheimer's disease, Parkinson's disease, avian influenza, pain and stroke. Thus, the involvement of the PDZ domain in disease pathways provides an important reference for the development of inhibitors capable of targeting PDZ-mediated interactions to inhibit PPI selectively.
BOC Sciences has fully considered the involvement of the PDZ domain in disease pathways, and established the PDZ PPI library by expanding on current efforts to modulate their interaction using modified peptides and small molecules as selective PDZ inhibitors.
Figure 1. Structure of the PDZ domain and mechanism of peptide recognition. (Harris, B. Z.; Wendell, A. 2001)
Library Design
We provide more than 200 structures of PDZ domains:
- The N- and C-termini of canonical PDZ domains are in proximity to each other on the opposite side form the peptide-binding site in a groove between the αB-helix and βB-strand structures
- The binding site in the groove shares a highly conserved carboxylate-binding loop
- A highly conserved positively charged residue
PDZ PPI Library Characteristics
- No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
- Bioactivity and safety confirmed by preclinical studies and clinical trials
- Structural diversity, medicinal activity, and cellular penetration
- Structural document, IC50, and other chemical and biological data are provided
- All compounds are continually updated
- All of these compounds with Tanimoto index ≥ 0.85
- Compound cherry-picking service is provided
Figure 2. The same PDZ domain can recognize two structurally distinct ligands. (Harris, B. Z.; Wendell, A. 2001)
What We Deliver
- Delivered within 2 weeks in any customer-preferred format
- Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
- All compounds have a minimum purity of 90% assessed by 1H NMR and HPLC
- Analytical data is provided
BOC Sciences provides professional, rapid and high-quality services of PDZ PPI Library design at competitive prices for global customers. Personalized and customized services of PDZ PPI Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!
Reference
- Harris, B. Z.; Wendell, A. LimMechanism and role of PDZ domains in signaling complex assembly. Journal of Cell Science. 2001. 114(18): 3219-3231.
