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Related Experiment Video

Updated: Jun 20, 2026

In Vitro Methods for Comparing Target Binding and CDC Induction Between Therapeutic Antibodies: Applications in Biosimilarity Analysis

In Vitro Methods for Comparing Target Binding and CDC Induction Between Therapeutic Antibodies: Applications in Biosimilarity Analysis

Published on: May 4, 2017

Structure-activity relationships for substrate-based inhibitors of human complement factor B.

Gloria Ruiz-Gómez¹, Junxian Lim, Maria A Halili

¹Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland, Australia.

Journal of Medicinal Chemistry

|September 12, 2009

Summary

Researchers developed novel peptide inhibitors for Factor B, a key protein in the human complement system. These inhibitors show potential for treating complement-mediated immune diseases.

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Protein WISDOM: A Workbench for In silico De novo Design of BioMolecules

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Published on: July 25, 2013

Area of Science:

Immunology
Biochemistry

Background:

Human complement system is crucial for immune defense but dysregulation causes disease.
Key complement proteases, like Factor B, are challenging to study due to their properties.

Purpose of the Study:

To investigate Factor B as a target for therapeutic intervention.
To develop and characterize novel inhibitors of Factor B activity.

Main Methods:

Structure-activity relationship studies were performed on 63 substrate-based peptide inhibitors.
Factor B activity was assessed under alkaline conditions (pH 9.5) and its inhibitory effects at neutral pH (pH 7) were evaluated.

Main Results:

A potent hexpeptide inhibitor, Ac-RLTbaLAR-H, was identified with an IC50 of 250 nM at pH 9.5.
This inhibitor blocked membrane attack complex formation and human complement-mediated lysis of erythrocytes at pH 7.

Conclusions:

Factor B inhibitors can be effective probes and potential drug leads for complement-mediated immunity and diseases.
Targeting Factor B offers a promising therapeutic strategy for immunoinflammatory conditions.