• Identify Native Lead Sequence & Binding Affinity
• Resolve Bioactive Conformation (NMR / X-ray)
• Map Critical Residues via Alanine Scanning
• Next Step: Proceed to Rational Design.
| Property | Natural Peptides | Our Custom Peptidomimetics |
|---|---|---|
| Metabolic Stability | Low (Rapidly degraded by proteases within minutes) | High (Resists enzymatic cleavage via engineered backbones) |
| Membrane Permeability | Poor (Difficult cellular uptake) | Enhanced (Modified side chains improve lipophilicity) |
| Target Affinity | High but flexible (Loss of entropy) | Locked & Rigid (Macrocyclized for precise binding) |
| In Vivo Half-Life | Short (Requires frequent dosing) | Extended (Optimized pharmacokinetic profiles) |
PHASE 1: TARGET CHARACTERIZATION
• Identify Native Lead Sequence & Binding Affinity
• Resolve Bioactive Conformation (NMR / X-ray)
• Map Critical Residues via Alanine Scanning
• Next Step: Proceed to Rational Design.
PHASE 2: RATIONAL DESIGN
• Backbone Mimicry (Amide Bond Bioisosteres, Peptoids)
• Non-Natural Side Chains (D-Amino Acids, Bulky Groups)
• Macrocyclization (Disulfide Staples, Hydrocarbon Stapling)
• Next Step: Proceed to Synthesis & ScreeningLength of the peptide from 20aa to 200aa.
PHASE 3: SYNTHESIS & SCREENING
• Solid-Phase Peptide Synthesis (SPPS) & RP-HPLC Purification
• Proteolytic Stability Assays (Serum/Plasma Half-Life)
• Binding Kinematics Evaluation (SPR, BLI, or ITC for Kd)
• Next Step: Proceed to Optimization & In Vivo.
PHASE 4: OPTIMIZATION & IN VIVO
• Permeability Testing (PAMPA or Caco-2 Monolayers)
• In Silico Refinement & Docking to Minimize Toxicity
• Preclinical In Vivo Pharmacokinetics (PK/PD Modeling)
Priveel Custom Peptides
Plot 16, SIPCOT- IT Park- Siruseri,
4th Main Road, 2nd Cross Street
Chennai.
Tamilnadu: 603103
+91 9123531574 / +91 8754672403
getinfo@priveelpeptides.com