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Peptide–Small Molecule / Ligand Conjugates (Non-Drug)

Peptide–ligand conjugates and non-drug peptide conjugation for research, imaging, capture, and functional studies.

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Site-defined attachment (project-dependent) Fluorophores & tags Carbohydrates & GalNAc Imaging conjugates Fit-for-purpose QC
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Overview

Peptide–small molecule / ligand conjugates are non-drug research constructs in which peptides are covalently linked to functional small molecules or ligands that do not possess intrinsic therapeutic activity. These conjugates are widely used as analytical and mechanistic tools to enable visualization, capture, uptake evaluation, and structure–function studies in biological systems [1], [2].

Unlike peptide–drug conjugates (PDCs), which incorporate pharmacologically active payloads, non-drug peptide–ligand conjugates are designed to support imaging, detection, receptor interaction, and transport pathway investigations without introducing therapeutic effects [3], [4]. Common ligand classes include fluorophores, affinity tags, vitamins and cofactors, carbohydrates, GalNAc ligands, and imaging-compatible probes.

Bio-Synthesis provides custom peptide–small molecule / ligand conjugation services focused exclusively on non-therapeutic applications. Projects are designed using site-defined chemistries and ligand-aware conjugation strategies to preserve peptide function, minimize heterogeneity, and deliver fit-for-purpose conjugates for discovery-stage and preclinical research [5].

Branched peptide synthesis schematic showing a lysine branching core with two to eight peptide arms (MAP-2, MAP-4, MAP-8) and dendrimer for multivalent epitope presentation.

Representative non-drug peptide–ligand conjugates (fluorophore-, biotin/affinity tag-, GalNAc-, and glyco-/carbohydrate-peptide formats) used for imaging, capture, and uptake studies.

Fluorophores Affinity tags Vitamins / cofactors Targeting ligands Glycopeptides GalNAc Imaging probes

Non-Drug Peptide Conjugate Categories

Expand each category to view representative ligands, typical applications, and design considerations. All examples are research-stage, non-drug conjugates; feasibility is project-dependent.

Peptides labeled with fluorescent dyes for visualization, localization, and quantitative analysis in biological systems.

Representative fluorophores Typical applications Notes
FITC, Fluorescein Cell imaging, binding assays Simple labeling; sensitive to pH and photobleaching
TAMRA, Rhodamine dyes Internalization studies Higher photostability vs fluorescein
Cy3 / Cy5, Alexa Fluor® Flow cytometry, multicolor imaging Selected by excitation/emission compatibility
View details →

Peptides conjugated with small-molecule affinity tags to enable selective capture or detection.

Representative tags Typical applications Notes
Biotin Pull-down assays, immobilization High affinity streptavidin binding
Desthiobiotin Reversible capture workflows Elutable from streptavidin
Biotin-PEG, DIG Detection, assay development Reduced steric hindrance / antibody-based systems
View details →

Peptides conjugated to vitamins or cofactors to study transport mechanisms and receptor-mediated uptake.

Representative vitamins Typical applications Notes
Vitamin E (α-tocopherol) Membrane interaction, uptake studies Hydrophobic; linker selection important
Vitamin A, D derivatives Receptor binding studies Functionalized handles required
Vitamin B1, B12, C Transport and mechanistic studies Preserve recognition motifs
View details →

Peptides conjugated with receptor- or transporter-binding ligands to support target validation and cellular uptake studies. Conjugation is typically site-defined to preserve both peptide and ligand activity.

Representative ligands Typical applications Notes
RGD motifs / RGD-derived ligands Integrin binding assays, uptake/internalization studies Attachment site selected to maintain binding activity
Folate derivatives (research use) Receptor engagement studies, uptake mechanism work Ligand handle/linker chosen to retain recognition
Project-defined small-molecule binders Target validation and comparative screening Feasibility depends on ligand functional groups and stability
View details →

Examples shown for research purposes; selection is based on project requirements and feasibility.

Glycopeptides are peptides covalently linked to carbohydrates to support studies of glycan-mediated recognition, immune interactions, and structure–function relationships. Designs may use pre-functionalized sugars or protected glycan building blocks depending on project needs.

Representative glycans Typical applications Notes
Glucose, mannose, galactose Glycan recognition assays; binding/interaction studies Defined glycosylation site supports reproducibility
Project-defined oligosaccharides Mechanistic studies; immunology and receptor work Complexity and protecting-group strategy impact route
Glycan analogs (functionalized handles) Probe development and comparative screening Handle selection used to maintain biological relevance
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All glycopeptide builds are custom and evaluated for synthetic feasibility and fit-for-purpose QC.

Glycolipid–peptide conjugates combine peptide sequences with lipid-linked carbohydrate structures. These constructs are explored in membrane interaction studies, immune modulation research, and receptor engagement investigations.

Representative formats Typical applications Notes
Glycosylated lipid anchors + peptide Membrane association studies; immune interaction assays Hydrophobicity and dispersion planned early
Amphiphilic peptide–glycolipid constructs Assembly/interaction experiments; probe development Route optimized to balance solubility and integrity
Project-defined glycolipid motifs Mechanistic research; receptor engagement screening Feasibility depends on lipid and glycan chemistry
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Examples shown for research purposes; final selection is defined by project scope and compatibility.

Imaging conjugates are designed for visualization and tracking in biological systems using imaging-compatible labels. Selection focuses on signal quality, stability, and compatibility with the intended imaging workflow.

Representative labels Typical applications Notes
Fluorescent probes (platform-selected) In vitro imaging; localization studies Chosen by excitation/emission and assay matrix
Imaging-compatible ligands (project-defined) Tracking/biodistribution proof-of-concept Fit-for-purpose QC based on intended use
Dual-label formats (case-by-case) Multiplexed experiments Feasibility depends on stability and steric effects
View details →

Designs are planned for research-stage use; labels are selected to support your platform requirements.

Peptides conjugated to GalNAc ligands to support ASGPR-mediated uptake studies.

GalNAc format Typical applications Notes
Mono-GalNAc Proof-of-concept uptake studies Simpler synthesis
Triantennary GalNAc Enhanced liver uptake research Higher avidity; defined geometry
View details →

FAQ

What fluorophores can be conjugated to peptides?

Common fluorophore requests include FITC, TAMRA, Cy3/Cy5, and Alexa Fluor®-type dyes. Selection depends on excitation/emission needs and assay conditions. Site-defined attachment (e.g., N-terminus or single-Cys) is often used to preserve peptide activity.

Which affinity tags do you support for peptide conjugation?

Representative affinity tags include biotin, desthiobiotin, biotin-PEG, and digoxigenin (DIG). These are widely used for capture/pull-down assays, surface immobilization, and detection workflows.

Can you conjugate vitamins (e.g., Vitamin E, B12) to peptides?

Yes. Representative vitamin/cofactor requests include Vitamin E (α-tocopherol), Vitamin A, Vitamin B1, Vitamin B12, Vitamin C, and Vitamin D. Conjugation typically uses functionalized vitamin handles and linkers selected to maintain ligand recognition and peptide integrity.

Do you offer GalNAc and glycopeptide formats?

Yes. We support peptide–GalNAc conjugates (including mono- and multivalent formats) and glycopeptides with project-defined carbohydrate structures. These are commonly used for uptake mechanism studies, receptor-mediated interactions, and structure–function investigations.

More FAQ'sAll FAQ's

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What to provide
  • Peptide sequence and desired attachment site
  • Ligand type (fluorophore, tag, carbohydrate, imaging probe)
  • Preferred linker or handle (if any)
  • Target quantity and intended application

Share your design details and timeline. Our scientists will recommend a feasible conjugation strategy and appropriate analytical characterization.

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Recommended Reading

  • Review on peptide–drug conjugates and conjugation concepts useful for peptide–ligand design: Chemical Society Reviews (2021). RSC article page
  • Site-selective peptide/protein modification strategies (useful for handle-enabled conjugation): Nature Reviews Chemistry (2019). Nature article page
  • Glycopeptide chemistry and applications overview: Chemical Reviews (review articles on glycopeptides). ACS Chemical Reviews (journal)
  • GalNAc conjugation and receptor-mediated uptake concepts (general background): Advanced Drug Delivery Reviews (journal resource). ScienceDirect journal page

Links are provided for reference; access may depend on institutional subscriptions.

Why Choose Bio-Synthesis

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Greetings Researchers,

Please be advised that any information, guidelines, writeups, and oral/video/graphic content on our website are intended solely as general guidelines.
It is the researcher's sole responsibility to conduct thorough research on the designs of the products intended for their experiments before submitting
their designs to Biosynthesis for review of production feasibility.
Thank you for your understanding.

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