An efficient mRNA display protocol yields potent bicyclic peptide inhibitors for FGFR3c: outperforming linear and monocyclic formats in affinity and stability
Camille Villequey, Silvana S. Zurmühl, Christian N. Cramer, Bhaskar Bhusan, Birgitte Andersen, Qianshen Ren, Haimo Liu, Xin-Ping Qu, Yang Yang, Pan Jia, Qiujia Chen, Martin Münzel
Abstract
's and stability were identified among bicyclic peptide hits, further strengthening the body of evidence pointing at the superiority of this class of molecules and providing functional and selective inhibitors of FGFR3c.
Topics & Concepts
Bicyclic moleculePeptideCombinatorial chemistryProtocol (science)Messenger RNAChemistryMetabolic stabilityComputational biologyStereochemistryBiochemistryBiologyMedicineGeneIn vitroAlternative medicinePathologyFibroblast Growth Factor ResearchCancer-related gene regulationMast cells and histamine