20.500.12556/RUL-134890 Small and simple, yet sturdy conformationally constrained peptides with remarkable properties The sheer size and vast chemical space (i.e., diverse repertoire and spatial distribution of functional groups) underlie peptides' ability to engage in specific interactions with targets of various structures. However, the inherent flexibility of the peptide chain negatively affects binding affinity and metabolic stability, thereby severely limiting the use of peptides as medicines. Imposing conformational constraints to the peptide chain offers to solve these problems but typically requires laborious structure optimization. Alternatively, libraries of constrained peptides with randomized modules can be screened for specific functions. Here, we present the properties of conformationally constrained peptides and review rigidification chemistries/strategies, as well as synthetic and enzymatic methods of producing macrocyclic peptides. Furthermore, we discuss the in vitro molecular evolution methods for the development of constrained peptides with pre-defined functions. Finally, we briefly present applications of selected constrained peptides to illustrate their exceptional properties as drug candidates, molecular recognition probes, and minimalist catalysts. constrained peptides macrocycles crosslinking enzymatic cyclization stapling hairpin loop peptidi true false true Angleški jezik Slovenski jezik Članek v reviji 2022-02-10 11:31:46 2022-02-10 11:31:48 2022-09-14 04:10:31 0000-00-00 00:00:00 2021 0 0 25 str. iss. 4, art. 1611 Vol. 22 2021 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 543.645.6:615 1422-0067 10.3390/ijms22041611 50385155 RAZ_Bozovicar_Kristof_2021.pdf RAZ_Bozovicar_Kristof_2021.pdf 1 4114A0931F3C116C90AC9E689A5A6752 8200ba5ba95df0e784540d9670cdb562dbd78a74c0e5e20d18e4590cefabd6b5 a078764b-8a5c-11ec-abdb-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=153618 https://www.mdpi.com/1422-0067/22/4/1611 1 6bbf138d-8a5c-11ec-abdb-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=153617 Fakulteta za farmacijo 0 0 0