Small Molecule Ligand-Drug Conjugation

As a leading service provider focused on drug conjugation, BOC Sciences's contract drug development program offers a comprehensive solutions for small molecule drug conjugates that can be custom designed and developed to fit your needs. Through the binding of small molecule ligands to drugs, the targeting of small molecule ligands can be utilized to direct the drugs to specific cells or tissues.

What are Small Molecule Drug Conjugates?

Small molecule drug conjugates (SMDCs) have three modules: targeting ligands, linkers, and drug payloads. The conjugation is designed to be stable in the bloodstream and then release active drugs from targeting ligands when SMDCs are absorbed by diseased cells. This modular approach allows for the use of different targeting ligands, connector systems, and drug payloads.

SMDCs have relatively low molecular weight and good cell permeability, as well as non-immunogenicity and ease of synthesis. The design of small molecule drug conjugates requires comprehensive consideration of the properties of the drug, the function of the coupling molecule, the stability of the linkage, as well as compatibility and toxicity to the organism.

Fig. 1 Schematic diagram of a typical small molecule drug conjugate. (Patel et al., 2021)

Custom Small Molecule Drug Conjugates

• Targeting small molecule screening

BOC Sciences provides screening services for targeting small molecules, which can be combined with drugs to achieve efficient identification and treatment of targets. We can screen small molecule ligands with high affinity and activity for you based on the target information provided.

• Small molecule-drug conjugation

BOC Sciences provides synthesis services for small molecule-drug conjugates. We can select the appropriate drugs and ligands for the coupling reaction according to your requirements and prepare the conjugates.

Preparation process of small molecule drug conjugates:

1) Selection of small molecule drugs

Select small molecule drugs with therapeutic effects and pharmacological properties, such as anticancer agents, anti-inflammatory agents, etc.

2) Chemical conjugation

Linking targeting molecules and small molecule drugs usually requires designing and synthesizing a suitable chemical linker. The position and method of conjugation need to consider the chemical properties of the drug and the structural characteristics of the target molecule.

3) Purification of conjugates

• Activity evaluation of small molecule-drug conjugates

Why Small Molecule Drug Conjugates?

a. Strong targeting

Ligands can point to specific targets, reduce the impact of drugs on healthy cells, and improve the therapeutic effect of drugs.

b. Strong controllability

The release of drugs can be regulated by appropriate chemical linkers, so that the drugs can be released at specific locations and timings to achieve more precise treatments.

c. Wide range of adaptation

Small molecule drugs have a small molecular weight and are easy to penetrate into tissues and cells, so they can be widely used in the treatment of various diseases.

Our Advantages

• Drug substance characterization
• Advanced equipment and technique
• Experienced scientific team
• Highly reliable and reproducible result
• Quality one-stop service
• Full Spectrum of Modification and Activation Services
• Data analysis, detailed report with results and discussion.

Project Workflow