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Journal of Chromatography & Separation Techniques | Volume: 09
8
th
World Congress on Chromatography
September 13-14, 2018 | Prague, Czech Republic
Polymer Science and Technology
4
th
International Conference on
Joint Event on
&
Gilles Goetz
Pfizer, USA
A
pplications of a new chromatographic method using SFC technology
developed recently at Pfizer are described here. The EPSAmethod, as readout
of polarity, correlates retention on a specific stationary phase with the exposed
polarity of a molecule. Changes in retention can be interpreted by changes in
polarity induced by the presence of intra-molecular hydrogen bonding (IMHB):
indeed, IMHBs tend to impact molecular conformation, inducing hidden polarity
that results in a decrease in analyte retention on the EPSA
support.Wedemonstrate
here the impact of this method on multiple beyond rule of five projects (NS5A,
Oxytocin Receptor, CXCR7 Modulator, others). Given that conformational
changes (induced and/or stabilized by the formation of IMHB) increases potential
for membrane permeability, we show here that EPSA, and the EPSA prediction
model, have significant impact in peptide drug design.
Gilles Goetz, J Chromatogr Sep Tech 2018, Volume: 09
DOI: 10.4172/2157-7064-C2-042
EPSA: a novel supercritical fluid chromatography technique enabling the design of permeable
cyclic peptides
Biography
Gilles Goetz is a Principal Scientist at Pfizer in Groton, Connecticut, USA. He received his BSc (1991) and PhD (1995) at the University of Strasbourg in France. After
his Post-doctoral studies at the University of Hawaii (1996-97) and of Neuchatel (CH) (1998-99) studying marine and fungal natural products, he joined Monsanto in
2000. There, he worked through mergers and acquisitions for Pharmacia and Pfizer successively in the natural product group, the HTS group (analytical support),
and the purification group. In 2010, he transferred to the expert purification group at Pfizer Groton and in 2011 to the molecular properties group. He is a part of
the team influencing medicinal chemistry design through insights into molecular properties such as polarity, lipophilicity, shape, and conformation that will impact
molecular behaviors like solubility, permeability, and efflux. They develop and use mainly chromatographic techniques (EPSA) to assess those properties, and work
towards predicting molecular behaviors.
gilles.h.goetz@pfizer.com