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May 13-14, 2019 | Prague, Czech Republic
Chemistry and Medicinal Chemistry
9th World Congress on
Page 15
Asian Journal of Biomedical and Pharmaceutical Sciences | Volume 9 ISSN: 2249-622X
Notes:
Andrés E Dulcey
National Institute of Health, USA
Discovery, optimization and characterization of CNS-Penetrant
Allosteric Inhibitors of c-Abl Kinase
The loss of different neuronal populations leading
to neuronal dysfunction, cytoskeletal alterations
and abnormal protein phosphorylation are the main
hallmarks of neurodegenerative diseases. In particular, the
neuropathological hallmarks of Alzheimer’s disease (AD) are
neuronal loss in regions related to memory and cognition,
neurotransmitter depletion, synaptic alteration and the
deposition of abnormal protein aggregates. Currently, there
is no effective treatment for AD, creating a need for new
therapeutic treatments that can treat or prevent AD and
other neurodegenerative diseases. c-Abl tyrosine kinase is
a ubiquitous non-receptor tyrosine kinase involved in signal
transduction. In addition to its classic function in leukemia
pathogenesis, c-Abl is also thought to play a role in neuronal
development, neurogenesis, neuronal migration, axonal
extension, and synaptic plasticity, whereby deregulation of
c-Abl could be related to early neuronal dysfunction and
cytoskeletal alterations. Here we describe the chemical and
pharmacological characterization of novel brain-penetrant
allosteric inhibitors of c-Abl tyrosine kinase activity, with
proof of principle towards their applicability as a potential
treatment for neurodegenerative disorders.
Speaker Biography
Andrés E Dulcey was born in Cali, Colombia. After completing a
Bachelor of Science in Chemistry from the Ohio State University, he
joined the laboratory of Professor Virgil Percec at the University of
Pennsylvania. His doctoral research focused on the design, synthesis
and structural characterization of biologically-inspired libraries of
amphiphilic compounds which self-assemble into functional, helical,
porous channels. After completion of his doctoral degree, he joined
the National Institutes of Health (NIH), first as a Postdoctoral Fellow
and then as a Research Scientist, where he has spent over 10 years
working in different modalities of medicinal chemistry. Currently, he is
at the National center for advancing translational sciences at the NIH,
where he works as a Research Scientist at the forefront of translation,
advancing programs in target identification and validation, assay
development and screening, probe development and lead optimization,
and drug repurposing, with the goal of furthering the understanding of
biochemical pathways and aiding the development of new medicines.
e:
Andrés E Dulcey, Asian J Biomed Pharmaceut Sci, Volume:9
DOI: 10.4066/2249-622X-C2-019