Elastase Serine Protease Targeted Library

Elastases are a type of serine proteases produced by the pancreas. Elastase catalyzes the cleavage of carboxyl groups present in small hydrophobic amino acids such as glycine, alanine and valine. Its main role is to break down elastin, a protein that imparts elasticity to connective tissue. Elastase not only cleaves the important connective tissue protein elastin, but also promotes the degradation of extracellular matrix such as fibronectin; laminin; collagens III, IV and VI; and proteoglycans. Activation of elastase-type serine proteases can lead to acute pancreatitis, chronic inflammatory lung disease, and cancer. Mammalian elastase occurs mainly in the pancreas and phagocytes. Among non-mammalian elastases, there are a variety of bacterial metallo and serine elastases. Elastolytic activity varies from elastase to elastase and is usually independent of the catalytic efficiency of these proteases. A large number of natural (protein) and synthetic elastase inhibitors are available. Elastases play a pathological role in emphysema, cystic fibrosis, infections, inflammation and atherosclerosis.

BOC Sciences can produce 500 potential elastase inhibitors via establishing an elastase serine protease targeted library.

Figure 1. Design of ultrasensitive probes for human neutrophil elastase. (Kasperkiewicz, P.; et al. 2014)

Library Design

BOC Sciences has developed a receptor-based library of potential elastase serine protease inhibitors by employing docking approach.

1. A receptor-based virtual screening workflow is carefully built based on X-ray data for the complexes: 2V0B
2. The compounds in the HTS compound collection have been pre-filtered using BOC Sciences' internal filters and then docked at the active site
3. Finally, 1,600 potential Elastase serine protease inhibitors can be selected with computational chemistry and virtual screening techniques are generated successfully

Elastase Serine Protease Targeted 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

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 Elastase Serine Protease Targeted Library design at competitive prices for global customers. Personalized and customized services of Elastase Serine Protease Targeted 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!