ArticleMolecular immunology2011
Novel analogues of the therapeutic complement inhibitor compstatin with significantly improved affinity and potency.
Article in Molecular immunology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
37 citing papers in PubMed, 67 citations in OpenAlex.
- New Analogs of the Compstatin Family of Clinical Complement Inhibitors with Low Picomolar Target Affinity.Journal of medicinal chemistry · 2026Article
- Fucoidan alginate and sulfated alginate microbeads induce distinct coagulation, inflammatory and fibrotic responses.Materials today. Bio · 2025Article
- Inflammation-Driven Plaque Erosion in Atherosclerosis: A Focus on Complement System Pathways.Current atherosclerosis reports · 2025Review
- Reconstitution of the alternative pathway of the complement system enables rapid delineation of the mechanism of action of novel inhibitors.The Journal of biological chemistry · 2024Article
- The complement alternative pathway in paroxysmal nocturnal hemoglobinuria: From a pathogenic mechanism to a therapeutic target.Immunological reviews · 2023Review
- Insight into mode-of-action and structural determinants of the compstatin family of clinical complement inhibitors.Nature communications · 2022Article
- Compstatins: the dawn of clinical C3-targeted complement inhibition.Trends in pharmacological sciences · 2022Review
- How we('ll) treat paroxysmal nocturnal haemoglobinuria: diving into the future.British journal of haematology · 2022Review
- Computational analysis of complement inhibitor compstatin using molecular dynamics.Journal of molecular modeling · 2020Article
- Distinct roles of the anaphylatoxin receptors C3aR, C5aR1 and C5aR2 in experimental meningococcal infections.Virulence · 2019Article
- Cholesterol Crystals Induce Coagulation Activation through Complement-Dependent Expression of Monocytic Tissue Factor.Journal of immunology (Baltimore, Md. : 1950) · 2019Article
- Alginate microbeads are coagulation compatible, while alginate microcapsules activate coagulation secondary to complement or directly through FXII.Acta biomaterialia · 2017Article
- Factor H C-Terminal Domains Are Critical for Regulation of Platelet/Granulocyte Aggregate Formation.Frontiers in immunology · 2017Article
- Iron oxide nanoparticles induce cytokine secretion in a complement-dependent manner in a human whole blood model.International journal of nanomedicine · 2017Article
- Complement component C3 - The "Swiss Army Knife" of innate immunity and host defense.Immunological reviews · 2016Review
- Properdin-Mediated C5a Production Enhances Stable Binding of Platelets to Granulocytes in Human Whole Blood.Journal of immunology (Baltimore, Md. : 1950) · 2016Article
- Using an in vitro xenoantibody-mediated complement-dependent cytotoxicity model to evaluate the complement inhibitory activity of the peptidic C3 inhibitor Cp40.Clinical immunology (Orlando, Fla.) · 2016Article
- Compstatin: a C3-targeted complement inhibitor reaching its prime for bedside intervention.European journal of clinical investigation · 2015Review
- Therapeutic C3 inhibitor Cp40 abrogates complement activation induced by modern hemodialysis filters.Immunobiology · 2015Article
- Tumor necrosis-initiated complement activation stimulates proliferation of medulloblastoma cells.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2015Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Compstatin is a 13-residue disulfide-bridged peptide that inhibits a key step in the activation of the human complement system. Compstatin and its derivatives have shown great promise for the treatment of many clinical disorders associated with unbalanced complement activity. To obtain more potent compstatin analogues, we have now performed an N-methylation scan of the peptide backbone and amino acid substitutions at position 13. One analogue (Ac-I[CVW(Me)QDW-Sar-AHRC](NMe)I-NH(2)) displayed a 1000-fold increase in both potency (IC(50) = 62 nM) and binding affinity for C3b (K(D) = 2.3 nM) over that of the original compstatin. Biophysical analysis using surface plasmon resonance and isothermal titration calorimetry suggests that the improved binding originates from more favorable free conformation and stronger hydrophobic interactions. This study provides a series of significantly improved drug leads for therapeutic applications in complement-related diseases, and offers new insights into the structure-activity relationships of compstatin analogues.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.