Discovery of APL-1030, a Novel, High-Affinity Nanofitin Inhibitor of C3-Mediated Complement Activation.


Journal

Biomolecules
ISSN: 2218-273X
Titre abrégé: Biomolecules
Pays: Switzerland
ID NLM: 101596414

Informations de publication

Date de publication:
11 03 2022
Historique:
received: 13 12 2021
revised: 11 02 2022
accepted: 07 03 2022
entrez: 25 3 2022
pubmed: 26 3 2022
medline: 30 4 2022
Statut: epublish

Résumé

Uncontrolled complement activation contributes to multiple immune pathologies. Although synthetic compstatin derivatives targeting C3 and C3b are robust inhibitors of complement activation, their physicochemical and molecular properties may limit access to specific organs, development of bifunctional moieties, and therapeutic applications requiring transgenic expression. Complement-targeting therapeutics containing only natural amino acids could enable multifunctional pharmacology, gene therapies, and targeted delivery for underserved diseases. A Nanofitin library of hyperthermophilic protein scaffolds was screened using ribosome display for C3/C3b-targeting clones mimicking compstatin pharmacology. APL-1030, a recombinant 64-residue Nanofitin, emerged as the lead candidate. APL-1030 is thermostable, binds C3 (K

Identifiants

pubmed: 35327625
pii: biom12030432
doi: 10.3390/biom12030432
pmc: PMC8946527
pii:
doi:

Substances chimiques

Amino Acids 0
Complement C3 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

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Auteurs

Joshua Garlich (J)

Apellis Pharmaceuticals, Waltham, MA 02451, USA.

Mathieu Cinier (M)

Affilogic SAS, 44200 Nantes, France.

Anne Chevrel (A)

Affilogic SAS, 44200 Nantes, France.

Anaëlle Perrocheau (A)

Affilogic SAS, 44200 Nantes, France.

David J Eyerman (DJ)

Apellis Pharmaceuticals, Waltham, MA 02451, USA.

Mark Orme (M)

Apellis Pharmaceuticals, Waltham, MA 02451, USA.

Olivier Kitten (O)

Affilogic SAS, 44200 Nantes, France.

Lukas Scheibler (L)

Apellis Pharmaceuticals, Waltham, MA 02451, USA.

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Classifications MeSH