Background of Drug Discovery Targeting Lysosomal Cathepsins
Lysosomal cathepsins are classified according to their catalytic sites into serines (cathepsins A and G), aspartic acids (cathepsins D and E), and 11 caspases that have been annotated in the human genome (proteases B, C, F, H, K, L, O, S, V, X and W). Currently cathepsins are the most abundant lysosomal proteases that are mainly found in acidic endo/lysosomal compartments where they play a vital role in intracellular protein degradation, energy metabolism, and immune responses among a host of other functions. Although the proteolytic functions of cathepsins in physiological processes show a certain degree of similarity, the consequences of cathepsin dysfunction in terms of clinical symptoms are very different. Dysregulation of cathepsin synthesis and activity is associated with a variety of diseases, including metabolic syndrome, cancer, and inflammatory neurological disorders. Furthermore, cathepsins are involved in tumor-associated growth, invasion, angiogenesis, and therapy resistance. Thus, the range and complexity of cathepsin-dependent biological activities make it a common concern for various diseases.
Fig. 1. Trafficking and targeting of lysosomal proteases. (Bose S J, et al., 2022)
Solutions
Lysosomal cathepsins have different functions under different pathological conditions and our scientists use cathepsins as highly relevant targets for therapeutic interventions in a range of diseases to develop appropriate targeting measures. Our goal is to help you design tailor-made selective cathepsins inhibitors. Based on an understanding of the structure, differential expression and localisation of cathepsins in a variety of pathologies, CD BioSciences is committed to providing our global clients with strategies for targeting lysosomal cathepsins in human disease.
Identifying Cathepsins for Targeting Diseases
- Breast, colon, lung, brain and head and neck cancers: Cathepsin B and L.
- Pancreatic and hepatocellular carcinomas: Cathepsin L.
- Lung, melanoma and colorectal cancer: Cathepsin H.
- Coronary artery disease, aneurysms, adiposity and peripheral artery disease: Cathepsin S, K and L.
- Liver metabolism: Cathepsin D.
- Type 2 diabetes: Plasma Cathepsin D.
- Osteoporosis: Cathepsin Z and K.
Cathepsins Fluorescent Probes
We use cathepsins as fluorescent probes for diagnostic non-invasive imaging, a method that has been successful in preclinical mouse models.
Cathepsins Enzyme Replacement Therapy
In diseases caused by histone inactivation or loss of function, we provide functional cathepsins to restore cellular function and ameliorate disease. We replace the defective lysosomal cathepsin D with recombinant proenzyme D and closely monitor the level of recombinant enzyme injected in mice.
Why Choose Us
- Multiple strategies to ensure effective lysosomal cathepsins targeting.
- Tailored targeting measures designed for different lysosomal cathepsins.
- Rapid experimental process to deliver results at an economical cost.
- Collaborate with experienced international technical staff.
CD BioSciences can meet any reasonable needs of our clients, taking time and budget into consideration for you. Our aim is to be customer-centric and to provide the highest quality services to customers. Our customer service representatives are enthusiastic and trustworthy 24 hours a day, 7 days a week. If you are interested in our services, please feel free to contact us for more information or a detailed discussion.
Reference
- Bose S J, Ayagama T, Burton R A B. (2022) Lysosomal proteases and their role in signaling pathways[M]//Proteolytic Signaling in Health and Disease. Academic Press, 41-61.