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Kirtikumar Jadhav
@ProPeptideLab
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Peptide Architects. We design and construct Peptides & Proteins to tinker with Biology: Pro-Peptide Chemical Biology | Medicinal Chemistry
New paper out: Meet Psysol 3—a novel #cyclotide #NaturalProduct from Psychotria solitudinum. A #cystine_knot #peptide that potently inhibits prolyl oligopeptidase, expanding chemical space for POP #pharmacology and #DrugDiscovery. #ChemicalBiology @univienna #PeptAIDes #ZK81B @fwf
Tropical psychotria plants are a rich source for peptide inhibitors of human prolyl oligopeptidase - Natural Products and Bioprospecting
Peptides from natural sources have often served as valuable leads in drug discovery. Plant-derived protease inhibitors are a notable class, yet their distribution, diversity, and targets remain underexplored. Here, eleven tropical Psychotria species were screened for cyclic cysteine-rich peptides, with extracts showing concentration-dependent inhibition of human prolyl oligopeptidase (POP). Peptidomics combining mass spectrometry and transcriptome mining revealed multiple inhibitory peptides. From Psychotria solitudinum, which contained 37 peptides, a novel peptide (psysol 3) was purified and sequenced. Its synthetic analogue inhibited POP with an IC50 of ~ 1.3 µM. Sequence analysis and synthetic probes identified loop 3 as the inhibitory motif. Psysol 3 is a new probe for POP pharmacology and future structure–activity studies.
📢 Call for papers | @FrontiersIn
"Rational Design of Peptide-Based Therapeutics for GPCRs"
We invite original research, reviews & perspectives — from #peptidechemistry and #GPCR biology to #drugdiscovery .
#Peptides #peptide-conjugates #Peptidomimetics