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SUMMARY:Design of nature-inspired stabilized peptides for GPCR drug discov
 ery
DTSTART:20241122T090000
DTEND:20241122T100000
DTSTAMP:20260504T184133Z
UID:564c8c69b647e6e921dd997bac7faa2c7b5933d828e9c0fdf2cff937
CATEGORIES:Conferences - Seminars
DESCRIPTION:Prof. Christian W. Gruber\nNeuropeptides are the most diverse 
 class of signaling molecules with crucial roles for human health and disea
 se. Most of these peptides act as hormones or as neurotransmitters via G p
 rotein-coupled receptors (GPCRs). GPCRs represent the largest family of ce
 ll surface receptors encoded by the human genome and they have been exploi
 ted as drug targets for many years. In fact\, drugs that target these rece
 ptors account for ~30% of the global market share of therapeutics.\nThe de
 velopment of peptide therapeutics targeting GPCRs has been limited by poor
  pharmacokinetics (metabolic instability\, short half-life\, and rapid cle
 arance) and lack of oral bioavailability (low gastrointestinal stability a
 nd membrane permeability). Furthermore\, the pharmacological concepts of b
 iased signaling\, receptor selectivity and allosterism need to be implemen
 ted into successful GPCR drug discovery projects to avoid harmful off-targ
 et effects.\nTo tackle these challenges\, we explore genomes/transcriptome
 s to identify evolutionary-related human neuropeptides and utilize pharmac
 ology-guided screening of nature-derived peptide extracts to discover nove
 l GPCR ligands. Using state-of-the-art chemical and computational tools su
 ch as molecular grafting\, backbone cyclization\, cysteine stapling and de
  novo design\, we have been developing innovative ligands for the k-opioid
  and cannabinoid-type 2 receptors that exhibit enhanced stability\, and im
 proved pharmacodynamic properties. As proof-of-concept\, two lead candidat
 es were analyzed in vivo for their analgesic and anti-inflammatory propert
 ies\, which may be drug candidates for the treatment of chronic abdominal 
 pain or inflammatory conditions.
LOCATION:BCH 3118 https://plan.epfl.ch/?room==BCH%203118
STATUS:CONFIRMED
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