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Your Position: Casa > ADC proteases for peptide linker——Screening and validation of linker
ADC proteases for peptide linker——Screening and validation of linker

ADC proteases for peptide linker——Screening and validation of linker

Background
Product List
Assay Data
Resources
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Product Features
Comprehensive products: Cathepsin B, Cathepsin L, Cathepsin S, MMP-2, MMP-7, MMP-9, β-glucuronidase, β-galactosidase
Natural conformation: HEK293 expressed protein to ensure the natural structure
Robust and consistent enzyme activity, ensuring reproducibility across batches
High purity: Verified by SDS-PAGE and SEC-MALS
Research Applications
Analysis and characterization for ADCs: Conducting linker screening and stability evaluation verification
Assessment of drug release to guarantee efficient intracellular payload delivery
ADC catabolism study
ADC Enzymatic degradability tests
Background
In the development of antibody-drug conjugates (ADCs), the linker plays a crucial role by connecting the antibody and cytotoxic payload, influencing key properties such as stability, potency, safety, and pharmacokinetics (PK). Selecting the appropriate linker is paramount for maximizing the therapeutic efficacy and safety of ADCs. An ideal linker should remain stable in the circulatory system and release the cytotoxic payload specifically within the tumor. However, linkers often lead to nonspecific release of payloads, resulting in off-target toxicity and narrowing the therapeutic window.
Linkers are typically classified as cleavable or non-cleavable based on their cleavage mechanism. Cleavable linkers can be efficiently triggered to release the cytotoxic payload in the tumor, with over 80% of clinically approved ADCs incorporating them. Current research in the ADC field primarily focuses on cleavable linkers, especially those cleaved by proteases like Cathepsin B. Ongoing investigations are also exploring the roles of other enzymes, including Cathepsin M, Cathepsin L, β-glucuronidase, and β-galactosidase, to further refine linker cleavage mechanisms and enhance the specificity and effectiveness of ADC therapies.
For the screening and validation of linkers for ADCs, we have developed a series of proteases specialized in linker cleavage, encompassing Cathepsin B, Cathepsin L, Cathepsin S, MMP-2, MMP-7, MMP-9, β-glucuronidase, and β-galactosidase.
Product List
MoleculeCat. No.Product DescriptionPreorder/Order
Assay Data
Enzyme Activity Data
Product( Cat. No.:CTB-H5222 ) Human Cathepsin B / CTSB Protein, His Tag (active enzyme)
SubstrateFluorogenic peptide substrate Z-LR-AMC
Enzyme Activity
（pmol/min/μg）		> 2,500
Product( Cat. No.:CAL-H52H3 ) Human Cathepsin L / CTSL1 Protein, His Tag (active enzyme)
SubstrateFluorogenic peptide substrate Z-LR-AMC
Enzyme Activity
（pmol/min/μg）		> 35,000
Product( Cat. No.:MM2-M52H9 ) Mouse MMP-2 (30-460) Protein, His Tag (active enzyme)
SubstrateFluorogenic peptide substrate Mca-PLGL-Dpa-AR-NH2
Enzyme Activity
（pmol/min/μg）		> 1,500
Product( Cat. No.:MM9-H5221 ) Human MMP-9 Protein, His Tag (active enzyme)
SubstrateFluorogenic peptide substrate Mca-PLGL-Dpa-AR-NH2
Enzyme Activity
（pmol/min/μg）		> 2,500
Product( Cat. No.:BEB-H52H3 ) Human beta-Glucuronidase/GUSB Protein, His Tag (active enzyme)
Substrate4-methylumbelliferyl-beta -D-glucuronide
Enzyme Activity
（pmol/min/μg）		> 3,500
Product( Cat. No.:BG1-H52H3 ) Human beta-Galactosidase-1 Protein, His Tag (active enzyme)
SubstrateFluorogenic substrate, 4-Methylumbelliferyl-β-D-galactopyranoside
Enzyme Activity
（pmol/min/μg）		> 1,800
Purity over 90% verified by SEC-MALS
Cathepsin B, MALS-validated protein

The purity of Human Cathepsin B, His Tag (Cat. No. CTB-H5222) is more than 90% and the molecular weight of this protein is around 60-75 kDa verified by SEC-MALS.

MMP9, MALS-validated protein

The purity of Human MMP-9, His Tag (Cat. No. MM9-H5229) is more than 90% and the molecular weight of this protein is around 50-70 kDa verified by SEC-MALS.

Case Show

Case studies show that ADC DS-8201 can be cleaved by Cathepsin B from ACROBiosystems

Case studies show that ADC DS-8201 can be cleaved by Cathepsin B from ACROBiosystems
Resources

Webinar playback and appointment

Addressing Challenges in Antibody-Drug Conjugate Development
Here is the brief recap of the webinar:ADCs have the potential to enable 'precision medicine' with a wide market reach.Challenges in ADCs include managing Target Affinity, enhancing payload conjugation, and assessing Payload Delivery in vivo Pharmacokinetics. We can provide high-quality solutions to address these challenges.
Addressing Challenges in Antibody-Drug Conjugate Development
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Building the Perfect Antibody-based Therapeutic from Selection to Engineering and Manufacturing
In this webinar, discover how advanced techniques such as Al-driven candidate selection optimization of antibody sequences, and precise conjugation methods come together to address some of the current challenges in antibody-based therapeutics.
Addressing Challenges in Antibody-Drug Conjugate Development
Watch Now

Resource download

More core reagents for Antibody-drug conjugates (ADCs) development
AGLink® ADC site-specific conjugation kit: Powering your magic bullets
Fc Receptor Proteins - Partners for Antibody Drug Development
[Flyer]Fucntional Cell Lines and Development Service
Tools for ADC PK Analysis

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Tools for ADC PK Analysis——Anti-payload antibodiesicon

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AGLink® Site-specific conjugation kiticon

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