ALL libraries (COBIB.SI union bibliographic/catalogue database)
PDF
  • Small and simple, yet sturdy [Elektronski vir] : conformationally constrained peptides with remarkable properties
    Bozovičar, Krištof ; Bratkovič, Tomaž, farmacevt, 1978-
    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.
    Source: International journal of molecular sciences [Elektronski vir]. - ISSN 1422-0067 (Vol. 22, iss. 4, 2021, str. 1-25)
    Type of material - e-article ; adult, serious
    Publish date - 2021
    Language - english
    COBISS.SI-ID - 50385155

    Link(s):

    https://www.mdpi.com/1422-0067/22/4/1611
    Repository of the University of Ljubljana – RUL
    DOI

Shelf entry