Proprotein Convertase Subtilisin/Kexin Type 1 Inhibitor Human Recombinant
PCSK1N Human Recombinant produced in E.coli is a single, non-glycosylated polypeptide chain containing 251 amino acids (34-260) and having a molecular mass of 26.6 kDa.
PCSK1N is fused to a 23 amino acid His-Tag at N-terminus and purified by proprietary chromatographic techniques.
Proprotein Convertase Subtilisin/Kexin (PCSK) is a family of serine proteases that play a crucial role in the activation of various proteins by cleaving their inactive precursors. The PCSK family consists of nine members, each with distinct functions and tissue distributions. These enzymes are involved in the processing of peptide hormones, growth factors, cell surface receptors, and other proteins essential for cellular homeostasis .
Key Biological Properties: PCSK enzymes are synthesized as inactive zymogens and undergo autocatalytic cleavage to become active. They are involved in the proteolytic maturation of secreted proteins such as hormones, cytokines, and growth factors .
Expression Patterns and Tissue Distribution: PCSK enzymes are ubiquitously expressed in various tissues, including the liver, brain, kidneys, and vascular walls. For instance, PCSK9, a well-studied member of this family, is predominantly expressed in the liver but also found in the brain and kidneys .
Primary Biological Functions: PCSK enzymes are essential for the activation of numerous bioactive proteins. They play a significant role in cholesterol metabolism by regulating the degradation of low-density lipoprotein receptors (LDLR), thereby influencing plasma cholesterol levels .
Role in Immune Responses and Pathogen Recognition: PCSK enzymes are involved in the regulation of immune responses. For example, PCSK9 has been shown to modulate the immune system by affecting the levels of major histocompatibility complex class I proteins, which are crucial for antigen presentation .
Mechanisms with Other Molecules and Cells: PCSK enzymes interact with various molecules and cells through their proteolytic activity. PCSK9, for instance, binds to LDLR on hepatocytes, leading to its degradation and subsequently increasing plasma LDL cholesterol levels .
Binding Partners and Downstream Signaling Cascades: PCSK enzymes have several binding partners, including LDLR and other cell surface receptors. The binding of PCSK9 to LDLR triggers a signaling cascade that results in the lysosomal degradation of LDLR, reducing its availability on the cell surface .
Regulatory Mechanisms Controlling Expression and Activity: The expression and activity of PCSK enzymes are tightly regulated at multiple levels. Transcriptional regulation involves various transcription factors that bind to the promoter regions of PCSK genes. Post-translational modifications, such as phosphorylation and glycosylation, also play a role in modulating the activity of these enzymes .
Transcriptional Regulation and Post-Translational Modifications: Specific transcription factors regulate the expression of PCSK genes, while post-translational modifications can alter the stability, localization, and activity of the enzymes .
Biomedical Research: PCSK enzymes are valuable targets in biomedical research due to their involvement in various physiological processes and diseases. Inhibitors of PCSK9, for example, have been developed as therapeutic agents to lower cholesterol levels in patients with hypercholesterolemia .
Diagnostic Tools and Therapeutic Strategies: PCSK enzymes serve as biomarkers for certain diseases and are used in diagnostic assays. Therapeutically, PCSK inhibitors are employed to treat conditions such as cardiovascular diseases and certain cancers .
Role Throughout the Life Cycle: PCSK enzymes play a role throughout the life cycle, from development to aging and disease. During development, they are involved in the maturation of various proteins essential for growth and differentiation. In aging and disease, dysregulation of PCSK activity can contribute to pathological conditions such as cardiovascular diseases and neurodegenerative disorders .
From Development to Aging and Disease: The activity of PCSK enzymes is crucial for maintaining cellular homeostasis throughout life. Their dysregulation can lead to various diseases, highlighting their importance in both health and disease .