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May 13-14, 2019 | Prague, Czech Republic
Chemistry and Medicinal Chemistry
9
th
World Congress on
Page 23
Asian Journal of Biomedical and Pharmaceutical Sciences | Volume 9
ISSN: 2249-622X
Simona Collina
Marta Rui, Giacomo Rossino
and
Daniela Rossi
University of Pavia, Italy
Across the “Universe” of Sigma receptor modulators.
The experience of the MedChemLab
S
igma Receptors (SRs) represent an interesting orphan
class of molecular targets to hit for counteracting
neurodegenerative diseases and cancer. They can
be divided into two receptor subtypes (S1R and S2R,
respectively), endowed with different physio-pathological
and structural properties. From a therapeutic standpoint,
the pharmacological activity of S1Rs is strictly related to the
modulators that they interact with. In detail, S1R agonists
promote neuroprotection and neuroplasticity, whereas
antagonists can be beneficial in thwarting neuropathic
pain and tumorous manifestations. Conversely, S2R
modulators may have a pivotal role as anticancer agents.
So far, four compounds reached the Clinical Stage of the
Drug Discovery Process, as drug candidate in therapy and
diagnosis for Alzheimer’s disease (ANAVEX 2-73, AVP-923),
for neuropathic pain (MR309) and cancer ([18F]-ISO-1).
TheMedicinal Chemistry Laboratory (MedChemLab) is part of
this scenario and has a long lasting experience in this field.
Indeed,thegroupspentitseffortsindesigningandsynthetizing
molecules with affinity and selectivity towards SRs and
discoved
(R)
-RC-33 and RC-106 as promising compounds.
(R)
-
RC-33 is a S1R agonist compound, characterized by good S1R
affinity, good in vivo pharmacokinetic profile and endowed
with neuroprotective properties. RC-106 is a pan-SR ligand
(S1R antagonist and S2R agonist) showing anticancer activity
towards a panel of cancer cell lines. These encouraging results
lead members of the MedChemLab group to keep believing
that SR modulators could become a relevant opportunity
in the pharmaceutical field. Accordingly, throughout this
speech the state-of-art and new insights of SRs, as well as the
MedChemLab projects will be depicted.
Speaker Biography
Simona Collina is interested in the design and synthesis of small
molecules, peptides, and peptidomimetics, focusing on their
therapeutic application, in particular in neurodegenerative diseases,
cancer and pain. Her interests also focus on drug discovery from natural
sources. Among the different research topics, the discovery of small
molecules able to affect the protein kinase C (PKC)/ELAV proteins/
mRNA system as well as new modulators of sigma receptors as well as
of are the most challenging.
e:
simona.collina@unipv.itSimona Collina et al., Asian J Biomed Pharmaceut Sci, Volume:9
DOI: 10.4066/2249-622X-C2-019
Notes: