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. 2019 Jun 14;10(7):1026-1032.
doi: 10.1021/acsmedchemlett.9b00149. eCollection 2019 Jul 11.

Permeability of Cyclic Peptide Macrocycles and Cyclotides and Their Potential as Therapeutics

Spiros Liras  1 , Kim F Mcclure  2
Affiliations

Permeability of Cyclic Peptide Macrocycles and Cyclotides and Their Potential as Therapeutics

Spiros Liras et al. ACS Med Chem Lett. .

Abstract

Macrocycles have emerged as a viable approach for the modulation of tough targets in drug discovery. In this Innovations article we discuss recent progress toward the design of cell permeable and orally bioavailable peptide macrocycles and cyclotides and provide a perspective for their potential as therapeutics. We highlight design concepts that may be broadly relevant to drug discovery efforts beyond the rule of five.

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Conflict of interest statement

The authors declare no competing financial interest.

Figures

Figure 1
Figure 1
Structure of 1, 1NMe3; 2, hexaleucine peptide; 3a, R1 = Me, R2 = H = sanguinamide A; 3b, R1 = t-Bu, R2 = Me; 3c, R1 = t-Bu, R2 = H; 4, kalata b1.
See this image and copyright information in PMC

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