Publications 2017-09-25T09:37:00+00:00

Publications by Our Team Members

Passive Membrane Permeability in Cyclic Peptomer Scaffolds Is Robust to Extensive Variation in Side Chain Functionality and Backbone Geometry

Synthetic and natural cyclic peptides provide a testing ground for studying membrane permeability in nontraditional drug scaffolds. Cyclic peptomers combine the stereochemical and geometric complexity of peptides with the functional group diversity accessible to peptoids.
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October 3rd, 2016|by our Team Members, Publications|

Simple Predictive Models of Passive Membrane Permeability Incorporating Size-Dependent Membrane-Water Partition

We investigate the relationship between passive permeability and molecular size, in the context of solubility-diffusion theory, using a diverse compound set with molecular weights ranging from 151 to 828, which have all been characterized in a consistent manner using the RRCK cell monolayer assay.
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May 23rd, 2016|by our Team Members, Publications|

Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products

Cyclic peptide natural products contain a variety of conserved, nonproteinogenic structural elements such as d-amino acids and amide N-methylation. In addition, many cyclic peptides incorporate γ-amino acids and other elements derived from polyketide synthases.
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May 7th, 2015|by our Team Members, Publications|

Testing the conformational hypothesis of passive membrane permeability using synthetic cyclic peptide diastereomers

Little is known about the effect of conformation on passive membrane diffusion rates in small molecules. Evidence suggests that intramolecular hydrogen bonding may play a role by reducing the energetic cost of desolvating hydrogen bond donors, especially amide N-H groups.
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November 1st, 2006|by our Team Members, Publications|

Industry Publications on Macrocycles

Macrocycles and Constrained Peptides

Macrocycles and constrained peptides have undergone a rebirth over the last five years in drug discovery, due mainly to the introduction of new approaches for their synthesis and screening. This scientific progress has fueled a burst of business activity, with at least 12 biotech companies in the space, of which almost half were founded in the last 5 years.
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April 11th, 2013|on Macrocycles, Publications|