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Cyclic peptides in plants are synthesized via a two-step process; the translation of a linear peptide chain, and its subsequent formation into a cyclic structure through activities of a protease-like enzyme or other ways. [6] [7] [8] Some peptides, such as cyclotides, are gene-coded products obtained by the processing of larger precursor proteins.
The stunting effect of kalata B1 cyclic peptide on growth and development of Helicoverpa punctigera, a caterpillar from the Lepidopteran order. [6]Cyclotides have been reported to have a wide range of biological activities, including anti-HIV, insecticidal, anti-tumour, antifouling, anti-microbial, hemolytic, neurotensin antagonism, trypsin inhibition, and uterotonic activities.
These drugs block activation of the integrin responsible for aggregation of platelets (αIIbβ3, also known as glycoprotein IIb/IIIa) in response to the blood glycoproteins fibrinogen and von Willebrand factor. Eptifibatide (marketed as Integrilin) is a cyclic (circular) seven amino acid peptide, whereas tirofiban is a small molecule designed ...
[3] Circular peptides tend to be resistant to protease activity, and may be suitable for use as orally administered drugs. Once a cyclic peptide is identified with a biological activity of interest, it may also be possible to identify the target of the peptide (a gene that encodes a protein with which it interacts) by functional complementation ...
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DKP's are the smallest known class of cyclic peptide. [1] Despite their name, they are not ketones, but amides. Three regioisomers are possible, differing in the locations of the carbonyl groups. Retosiban [2] is a diketopiperazine being investigated as an oral drug. One isomer is an oxamide obtained from ethylenediamine.
Novo Nordisk scientist Lotte Bjerre Knudsen paved the way for popular GLP-1 drugs like Ozempic. Her work in the 1990s was instrumental in turning short-acting hormones into long-acting drugs.
The use of peptides as drugs has some disadvantages because of their bioavailability and biostability. Rapid degradation, poor oral availability, difficult transportation through cell membranes, nonselective receptor binding, and challenging multistep preparation are the major limitations of peptides as active pharmaceutical ingredients. [ 3 ]