9 / 13
Page 43
Notes:
conferenceseries
.com
Volume 7
Molecular Biology: Open Access
Molecular Biology Meet 2018
August 27-28, 2018
August 27-28, 2018 Dubai, UAE
Molecular Biology and Medicine
International Conference on
Drug repositioning as an effective therapy for protease-activated receptor-2 inhibition
Uzma Saqib
Indian Institute of Technology Indore, India
P
roteinase-Activated Receptor-2 (PAR-2) is a GPCR activated by both trypsin and a specific agonist peptide, SLIGKV-NH2.
It has been linked to various pathologies, including pain and inflammation. Several peptide and peptidomimetic agonists for
PAR-2 have been developed exhibiting high potency and efficacy. However, the number of PAR-2 antagonists has been smaller.
We screened the FDA library of approved compounds to retrieve novel antagonists for repositioning in the PAR-2 structure. The
most efficacious compound Bicalutamide bound to the PAR-2 binding groove near the extracellular domain as observed in the
in
silico
studies. Further, it showed reduced Ca
2+
release in trypsin activated cells in a dose-dependent manner. Hence, Bicalutamide
is a novel and potent PAR-2 antagonist which could be therapeutically useful in blocking multiple pathways diverging from PAR-2
signaling. Further, the novel scaffold of Bicalutamide represents a new molecular structure for PAR-2 antagonism and can serve
as a basis for further drug development.
uzma05@gmail.comMol Biol 2018, Volume 7
DOI: 10.4172/2168-9547-C1-003