BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR FAPalpha

The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of fibroblast activation protei...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: WALKER ERIC, STACE CATHERINE, L. CHEN
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung:The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of fibroblast activation protein a (FAPalpha). The invention also includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by FAPalpha. 本发明涉及多肽,其与分子支架共价结合,使得在支架的连接点之间对向存在两个或更多个肽环。特别地,本发明描述了作为成纤维细胞激活蛋白a(FAPα)的高亲和力结合物的肽。本发明还包括包含与一个或多个效应子和/或官能团偶联的所述肽的药物偶联物,包含所述肽配体和药物偶联物的药物组合物,以及所述肽配体和药物偶联物在预防、抑制或治疗FAPα介导的疾病或疾患中的用途。