Advancing Next-Generation Peptide Therapeutics
Peptide Drug Discovery Platform
Overview
Accelerate Peptide Discovery Pipeline with Smarter, and More Efficient Solutions
Peptide drug discovery is evolving rapidly, ushered by innovations in biotechnology and AI-enabled tools. Medicilon stands at the forefront with a comprehensive peptide discovery platform, offering end-to-end solutions from ultrahigh-diversity library construction to lead optimization and functional validation.
Why Medicilon is Your Ideal Peptide Discovery Partner?
Our capabilities include:
- mRNA display for high diversity libraries
- Solid-phase / liquid- phase peptide synthesis
- AI-powered peptide modeling and structure-based virtual screening
With Medicilon, your peptide discovery pipeline becomes faster, smarter, and more efficient.
75+ peptide scientists
with expertise across synthesis, screening, and analysis
From DNA to candidate
complete discovery workflow
Proven track record
in macrocycles, conjugates, and radioligands
Innovative cyclization techniques
including DBX, Thioether, Click chemistry, and RCM etc. methods
AI-enabled peptide design + mRNA display
for unmatched discovery power
A Comparison of Cyclic Peptide Screening Technologies
Approaches
Library Size
Amino Acid Diversity
In Vivo/ In Vitro
Main Advantages
Main Limitations
- Phage Display
10^8-10^9
- Natural
- In vivo
- High diversity, well-established
- Limited chemistry, biological bias
- SICLOPPS
10^6 – 10^8
- Natural
- In vivo
- Intracellular cyclization
- Lower diversity, sequence bias
- OBOC
10^4 – 10^6
- Natural & unnatural
- In vitro
- Chemical diversity, fast screening
- Lower diversity, higher cost
- mRNA Display
10^12 -10^13
- Natural & unnatural
- In vitro
- Ultra-high diversity, chemically flexible
- Technical complexity
Core services
mRNA Display Technology: Heart of Medicilon Peptide Platform
mRNA display technology links peptides directly to their mRNA templates, enabling rapid screening of trillions of variants against “undruggable” targets. Medicilon’s mRNA display workflow includes:
Library Construction
DNA libraries are transcribed into mRNA and ligated to puromycin-DNA linkers.
Translation & Conjugates
Ribosomes generate peptide chains, and puromycin creates a peptide-mRNA conjugates.
Affinity Selection
Peptide conjugates are screened against immobilized targets; binders are enriched and amplified.
Amplification & Sequencing
Selected sequences are reverse transcribed and analyzed by NGS.
Advantages Over Other Platforms
mRNA display supports unnatural amino acid incorporation and avoids aggregation issues, making it ideal for macrocyclic peptide discovery.
Feature
mRNA Display
Phage Display
Ribosome Display
- Library Size
Up to 10^13
- ~10^8
- ~10^12
- Linker
Small puromycin-DNA
- Large viral particle
- Ribosome complex
- Environment
Fully in vitro
- Cell-dependent
- In vitro, ribosome-bound
- Control
High
- Limited
- Limited by ribosome stability
Strategies for Improved Stability and Activity
Medicilon's Peptide Synthesis and Engineering Capabilities
Cyclization enhances peptide stability and function. Our platform supports:
Thioether-Based Cyclization
Spontaneous or reagent-driven macrocyclization between cysteines and functional groups (e.g., mCNP), useful for monocycles and modular bicyclic constructs.
Reference:
Hayden Peacock, et al. Discovery of De Novo Macrocyclic Peptides by Messenger RNA Display. Trends Pharmacol Sci.2021 May;42 (5):385-397. doi: 10.1016/j.tips.2021.02.004.
m/p-Dibromoxylene (DBX) Cyclization
Forms rigid bicyclic peptides via thioether linkages between two cysteines. Ideal for structured scaffolds with superior plasma stability and high-affinity target engagement.
Reference:
Hayden Peacock, et al. Discovery of De Novo Macrocyclic Peptides by Messenger RNA Display. Trends Pharmacol Sci.2021 May;42 (5):385-397. doi: 10.1016/j.tips.2021.02.004.
In Silico Peptide Virtual Screening
We integrate computational approaches to accelerate hit identification and refinement:
- Structure-Based Docking: Tools like Rosetta, AutoDock CrankPep (ADCP), HADDOCK, simulate peptide-target binding.
- AlphaFold Integration: AF-Multimer predicts peptide-protein complexes from sequence; refined using protein-peptide MD simulation.
Scenario
Approach
- Known 3D Structure
Refinement Docking + MD simulation
- Unknown Target Structure
Unknown Target Structure
Core services
Medicilon's Peptide Synthesis and Engineering Capabilities
We support, but not limited to:
- Linear Peptide
- Cyclic Peptide
- Modified Peptides
- PEGylation
- Isotopic Labeling
- Fluorescence Modification
- Peptide Protein Coupling
Cyclic Peptide
MK0616, PCSK9 inhibitor
Phospho Peptide
PEGylated Peptide
R = SH or aliphatic amine, or other groups used for modification
Dye modified Peptide
Modified long chain-peptide (Semaglutide Analogs)
H-{Aib}-EGTFTSDVSSYLEGQAA-{C18 diacid-γ-Glu-(AEEA)2-Lys}-EFIAWLVRGRG
Cyclization Expertise
- S-S bridges
- Lactam
- DBX
- Enzymatic macrocyclization
Scale
- From mg to 100g Quantities
- Automated HPLC Purification
- Lyophilization
Proven Success
Case Studies That Prove Our Success
Explore how Medicilon’s IND-focused toxicology studies have helped clients overcome regulatory hurdles, accelerate timelines, and advance drug candidates with confidence. Each case highlights our scientific expertise and strategic approach to IND success.
BT8009 (PDC)
Bicyclic conjugate synthesized and validated with >95% purity.
RDC Ligand
Radioligand construct for tumor targeting delivered successfully
Linear Unnatural Peptides
500 mg batches of modified sequences with >95% purity.
In Vitro Assays to Validate Functionality
Medicilon offers a wide suite of binding and functional assays:
Methods
Assay Type
Applications
- SPR binding assay
Binding assays - protein level
Test binding Kd, Kon, and Koff of a peptide with a target protein
- ELISA binding assay
Binding assays - protein level
Test binding activity of peptide with target protein - IC50
- HTRF-cellular binding assay
Binding assays - cellular level
Test binding activity of peptide with target protein at cellular level - EC50
- Radio-ligand binding assay
Binding assays - cellular level
Test binding activity of peptide with target protein at cellular level - EC50
- cAMP release assay
Functional assays
Test binding Kd, Kon, and Koff of a peptide with a target protein
- Ca²⁺ release assay
Functional assays
Test downstream signal activation of target protein at cellular level - EC50
- Receptor internalization assay
Functional assays
Test peptide-induced receptor internalization activity
Take the Next Step in Your Peptide Discovery Journey
Let Medicilon’s experienced team guide your project from idea to candidate – faster, smarter, and with proven success.
