C4BPα Inhibitors

C4BPα, also known as C4b-binding protein alpha chain, is a key regulator of the complement system, which is a part of the innate immune response responsible for recognizing and eliminating pathogens. C4BPα plays a crucial role in controlling the activation of the complement cascade by regulating the formation and stability of the C3 convertase enzyme complex. This complex is involved in the cleavage of C3 into its active forms, C3a and C3b, initiating downstream effector functions such as opsonization, chemotaxis, and cell lysis. C4BPα achieves its regulatory function by binding to C4b, a component of the complement cascade, and acting as a cofactor for factor I-mediated cleavage of C4b into inactive fragments. By inhibiting the formation of the C3 convertase complex, C4BPα prevents excessive activation of the complement system and helps maintain immune homeostasis.

Inhibition of C4BPα can be achieved through various mechanisms targeting its interaction with C4b and other complement components. One approach is the use of small molecule inhibitors that disrupt the binding interface between C4BPα and C4b, preventing the formation of the C4BPα-C4b complex. Alternatively, antibodies or peptide-based inhibitors can be designed to specifically target C4BPα, blocking its regulatory function and allowing for uncontrolled activation of the complement cascade. Additionally, modulating the expression or activity of factors involved in the synthesis or secretion of C4BPα can indirectly inhibit its function in complement regulation. By targeting C4BPα inhibition, these strategies offer potential avenues for modulating the immune response and investigating the role of the complement system in various pathological conditions.