chemistry-2019-keynote

5 / 28

allied
academies
May 13-14, 2019 | Prague, Czech Republic
Chemistry and Medicinal Chemistry
9th World Congress on
Page 18
Asian Journal of Biomedical and Pharmaceutical Sciences | Volume 9 ISSN: 2249-622X
Gemini surfactants are amphiphilic molecules
containing two head groups and two aliphatic tails
which are linked by a spacer between the head groups,
or between the linker region connecting the heads and
the tails. Because their critical aggregate concentration
is 103-fold lower they are more effective surfactants than
the corresponding monovalent compounds (i.e. classical
surfactants with a single chain and a single head group),
which makes them interesting for various biomedical
applications.
Cationic geminis have shown to be viable agents for
transfection, the introduction of nucleotides into a
eukaryotic cell, thereby providing an alternative to viruses
and cationic polymers. Amphiphilic peptides consisting of
a peptide spacer with the N- and C-termini appended with
hydrophobic groups are asymmetric geminis and are called
gemini-like or geminoids. Interestingly, the SPKR geminoid
with unsaturated alkyl tails can achieve transfection
without the lysogenic helper lipid that is required in other
cases.
The proteases involved in the maturation of the
polyprotein of dengue virus to new virus particles have
cationic peptide sequences as their preferred substrates.
Saturated geminoids of the KGnK and KAnK series (n = 1
or 2) are inhibitors of dengue virus 2 protease and the
host protease furin, with slight selectivity of one over the
other.The inhibitors are also active against dengue virus
2 infection in a cellular context, at concentrations below
which they are toxic.
Speaker Biography
Martin C Feiters graduated in biochemistry, bio-organic chemistry
and food chemistry and did PhD research on structure-function
relationship of the enzyme lipoxygenase, followed by postdoctoral
work in X-ray absorption spectroscopy, before his appointment as
Associate Professor at Radboud University (1989). He has > 150
publications and a number of patents. He has applied various kinds of
radiation, viz. synchrotron X-rays and neutrons, to the elucidation of
supramolecular structures such as viruses, lipid-DNA complexes, and
porphyrin assemblies, as well as the coordination chemistry of metals
in homogeneous catalysts, metalloproteins, and biological non-metal
trace elements such as bromine and iodine. He has contributed to the
development of hyperpolarization in NMR, viz. by the optimization
of the catalyst and the co-substrate approach for detection and
quantitative analysis by Signal Amplification by Reversible Exchange
(SABRE) and high-field non-hydrogenative para-hydrogen-induced
hyperpolarization (PHIP) at micromolar concentrations. He is involved
in the developments of various drugs, viz. antimalarials, cyclodextrin-
based steroid transporters, and amphiphilic peptides for transfection
as well as, together with his spin-off company Protinhi Therapeutics, as
inhibitors of viral proteases.
e:
Martin C Feiters
Radboud University, The Netherlands
Cationic gemini and geminoid peptide amphiphiles:
From transfection to Protease inhibition
Martin C Feiters, Asian J Biomed Pharmaceut Sci, Volume:9
DOI: 10.4066/2249-622X-C2-019
Notes: