Protease Screening & Profiling Services

OverviewService ScopeCapabilitiesApplicationsProfessional SupportContact Us

Overview

Proteases represent one of the largest enzyme families encoded by the human genome. By catalyzing the hydrolysis of peptide bonds, they regulate a wide array of physiological and pathological processes, including cell proliferation, tissue remodeling, embryonic development, coagulation, blood pressure regulation, protein activation and degradation, inflammatory responses, infection, and tumorigenesis. The human degradome comprises at least 569 proteases, categorized into five major classes: metalloproteases, serine proteases, cysteine proteases, threonine proteases, and aspartic proteases. Due to their central roles in disease mechanisms, proteases have become highly valued drug targets. Successful inhibitors of key proteases, such as HIV protease, matrix metalloproteases (MMPs), dipeptidyl peptidases (DPPs), and angiotensin-converting enzyme (ACE), have demonstrated significant clinical efficacy in treating hypertension, diabetes, HIV infection, and coagulation disorders.

Protease Screening & Profiling Services Figure 1. Protease basics. (Turk B. 2006)

Service Scope

To support diverse protease-targeted drug discovery needs, Creative Biogene has established a comprehensive protease screening and functional profiling platform. Covering more than 50 protease targets across metalloproteases, serine proteases, cysteine proteases, aspartic proteases, and threonine proteases, our platform integrates multiple assay technologies and resources to facilitate compound evaluation throughout the drug discovery pipeline.

Table 1. Protease screening targets

Metalloprotease	MMP1	MMP2	MMP3	MMP7	MMP8
	MMP9	MMP10	MMP12	MMP13	MMP14
	Neprilisin	TACE	ADAM10	ACE1	ACE2
Serine protease	Kallikrein1	Kallikrein5	Kallikrein7	Kallikrein12	Kallikrein13
	Kallikrein14	DPP3	DPP4	DPP7	DPP8
	DPP9	HCV1a	HCV1b	HCV2a	Matriptase2
	Chymase	Proteinase A	Proteinase K	Thrombin	Trypsin b2
	Trypsin g1	Urokinase	Factor VIIa	Factor Xa	Factor XIa
	Elastase	Cathepsin G	Chymotrypsin
Cysteine protease	Papain	Calpain 1	Cathepsin B	Cathepsin C	Cathepsin H
	Cathepsin L	Cathepsin S	Cathepsin V	MALT1	UCHL1
	USP1	USP2	USP3	Calpain 2	UCHL3
Aspartic Protease	HIV-1	BACE1	Caspase-1	Caspase-3	Caspase-6
Aspartic Protease	Caspase-7	Caspase-8	Caspase-9	Caspase-4
Threonine protease	PSMA1	PSMA2	PSMA3	PSMA4	PSMA5
Threonine protease	PSMA6	PSMA7	GGT1	GGT2

Capabilities

High-Purity Protease Reagents: We supply rigorously validated recombinant proteases, isoforms, and reference inhibitors to support studies across drug discovery workflows.
Substrate Specificity Profiling: Advanced substrate-profiling tools define active-site subsite preferences and guide inhibitor design. High-specificity fluorescent assays reduce false positives and negatives.
High-Throughput & Fragment Screening: Our platform enables large-scale screening without prior substrate knowledge and supports the discovery of allosteric or exosite inhibitors, ideal for proteases with conserved active sites.
Mechanistic Assessment: Both reversible and irreversible inhibitors are evaluated with key kinetic parameters, including IC₅₀, Ki, and binding constants.
Computational & Structural Support: CADD methods—molecular docking, MD simulations, and 3D-QSAR—facilitate virtual screening and lead optimization, complemented by structural characterization of protease–inhibitor complexes.
Customizable Assays: Detection formats and miniaturized high-throughput systems are tailored to project needs for efficient, precise assay development.

Applications and Project Experience

Our platform has supported drug discovery projects across antiviral agents (HCV and HIV protease inhibitors), antithrombotics (thrombin and factor Xa inhibitors), metabolic disease therapies (DPP-4 inhibitors), and anticancer drugs (proteasome and cathepsin inhibitors). We offer tailored solutions grounded in a deep understanding of protease biology and family-specific challenges.

Quality Assurance and Professional Support

Creative Biogene maintains rigorous quality control and a highly experienced research team to ensure reliable, reproducible experimental data. Every step—from protein expression and purification to activity verification, assay optimization, and data analysis—is carefully monitored. Flexible service models accommodate unique project requirements, from basic functional validation to complex mechanistic studies, providing professional technical support throughout.

Contact Us

For more information about our protease service platform or to discuss a specific research project, please contact us. We are committed to supporting your innovative drug discovery initiatives with professional expertise and comprehensive analytical insights.

* For research use only. Not intended for any clinical use.

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