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NRTKs Inhibitor Development
Non-receptor tyrosine kinases (NRTKs) play a key role in the development of several cancers, including prostate cancer. They are involved in regulating processes such as cell proliferation, differentiation and survival. At Alfa Cytology, we provide a comprehensive one-stop service for the development of NRTKs inhibitor for prostate cancer.
Introduction to NRTKs Inhibitor
NRTKs are non-receptor tyrosine kinases, and they play key roles in cell signaling, especially in promoting cell proliferation and survival. In prostate cancer, aberrant activation of NRTKs is associated with tumor progression and drug resistance; therefore, the development of inhibitors targeting NRTKs is important for the treatment of prostate cancer.
Fig. 1 Therapeutic
strategies that target key kinases in CRPC. (Zhong, S., et al. 2022)
Structure of NRTKs
NRTKs are a family of proteins that contain multiple members, including ABL, SRC, FAK, and others. These kinases typically have similar structural domains, including a catalytically active tyrosine kinase domain (TKD), and regulatory structural domains that regulate kinase activity.
Tyrosine Kinase Domain (TKD)
- Catalytically active pocket is the core part of the kinase structural domain and contains the ATP binding site and the substrate (usually tyrosine residue) binding site.
- Activation loop, located near the pocket of catalytic activity, is a flexible ring structure whose conformational change is critical for kinase activity.
- Regulatory helix interacts with the activation loop and is involved in kinase activation and inhibition. In some kinases, conformational changes in the regulatory helix can affect the position of the activation loop and thus regulate kinase activity.
Regulatory Domains
- Src homology 2 domain recognizes and binds peptides containing phosphotyrosine. This binding event is usually associated with kinase activation or substrate recognition.
- Src homology 3 domain is often involved in protein-protein interactions and recognizes and binds proline-rich sequences.
- Pleckstrin homology domain binds phosphoinositides and other membrane-associated molecules and is involved in regulating the membrane localization and activity of kinases.
Our Services
In the field of prostate cancer treatment, the development of Nonreceptor Tyrosine Kinases (NRTKs) inhibitors represents a new therapeutic strategy aimed at targeting signaling pathways in tumor cells to inhibit tumor growth and spread. With a specialized platform that provides one-stop NRTKs inhibitor development services from basic research to preclinical development, Alfa Cytology is committed to translating scientific discoveries into effective therapies.
Workflow for NRTKs Inhibitor Development
Utilize the latest biological and pharmacological studies to design highly effective inhibitors against NRTKs targets.
Optimize lead compounds through structure-activity relationship studies to improve potency and selectivity.
Conduct in-depth in vitro and in vivo experiments to evaluate the safety and efficacy of inhibitors.
One-stop Solutions for NRTKs Inhibitor Development
Offer complete development of small molecule inhibitors, from discovering lead compounds to enhancing their chemistry, screening, and adjusting them for better performance.
Develop ADCs means linking a toxic drug to a monoclonal antibody with a chemical linker for precise delivery, targeting tumor cells strongly while minimizing harm to healthy ones.
Specific cells are modified, cultured and expanded, and finally the resulting cells are characterized to develop cellular drugs for the therapy of prostate cancer.
Prostate cancer modeling services provide researchers with reliable, reproducible and physiologically relevant models.
Alfa Cytology is a company dedicated to the development of prostate cancer therapies. Our company aims to provide customized one-stop NRTKs inhibitors development services in the field of prostate cancer therapy. If you are interested in our services, please don't hesitate to contact us for further information and pricing details.
Reference
- Zhong, S., et al. Choosing Kinase Inhibitors for Androgen Deprivation Therapy-Resistant Prostate Cancer. Pharmaceutics. 2022, 14(3): 498.
For research use only.