Cisbio eBook - 20

Trends in Protein-Protein Interactions Research | Advantages May Place Peptides Ahead of Small-Molecule Drugs

David Earp Circle Pharma

The chemistry-extensive automated platform allows investigators at Circle
Pharma to produce macrocycles rapidly and at a low cost, allowing several
design hypotheses to be tested in parallel. These investigators are focusing
on so-called "undruggable" oncology targets for which high-quality structural data is available to facilitate drug design.
"We are working on compelling targets that are well understood from the
biology perspective but have not been clinically validated," says Dr. Earp. "As
our programs advance, we are starting to look at metabolic liability in our
macrocyles. It appears to be similar to small molecule drug metabolism,
and we can modulate it with appropriate side-chain substitutions."
Scientists at Circle Pharma are working to develop a deeper understanding
of metabolic liability, one that they can use to refine their computational
algorithms and improve their design methods. "At the same time, we are
actively reviewing our target selection while taking into account newly
available structural information and scientific advances," declares Dr. Earp.
"As we expand our platform throughput with further synthesis automation,
we will have the ability to work on multiple targets in parallel while we add
or switch targets as appropriate."
CXCR7, a chemokine receptor implicated in several diseases, is being targeted by peptidic

CXCR7, a chemokine receptor implicated in several diseases, is being
targeted by peptidic macrocycles produced by Circle Pharma. These molecules incorporate a residue that permits extensive exploration of peptide
side chains. Models and assays lead to peptidic macrocycles, such as the
20 | GENengnews.com

macrocycles produced by Circle Pharma. These molecules incorporate a residue that
permits extensive exploration of peptide side chains. Models and assays lead to peptidic
macrocycles, such as the one shown here (yellow), that may perform better than small
molecules in terms of potency and selectivity.



http://www.GENengnews.com

Cisbio eBook

Table of Contents for the Digital Edition of Cisbio eBook

Contents
Cisbio eBook - 1
Cisbio eBook - 2
Cisbio eBook - 3
Cisbio eBook - Contents
Cisbio eBook - 5
Cisbio eBook - 6
Cisbio eBook - 7
Cisbio eBook - 8
Cisbio eBook - 9
Cisbio eBook - 10
Cisbio eBook - 11
Cisbio eBook - 12
Cisbio eBook - 13
Cisbio eBook - 14
Cisbio eBook - 15
Cisbio eBook - 16
Cisbio eBook - 17
Cisbio eBook - 18
Cisbio eBook - 19
Cisbio eBook - 20
Cisbio eBook - 21
Cisbio eBook - 22
Cisbio eBook - 23
Cisbio eBook - 24
Cisbio eBook - 25
Cisbio eBook - 26
Cisbio eBook - 27
Cisbio eBook - 28
Cisbio eBook - 29
Cisbio eBook - 30
Cisbio eBook - 31
https://www.nxtbookmedia.com