Heparanase is an endo-β-D-glucuronidase that specifically cleaves heparan sulfate (HS) chains within proteoglycans, playing a pivotal role in extracellular matrix (ECM) remodeling. This Glycosyl Functional Enzyme undergoes proteolytic activation into a heterodimer under acidic conditions prevalent in tumor microenvironments and inflammatory sites. Beyond its enzymatic activity, heparanase facilitates cell migration, angiogenesis, and metastasis by releasing HS-bound growth factors like vascular endothelial growth factor (VEGF). This Glycocalyx-Degrading Enzyme also exhibits non-enzymatic functions, such as enhancing Akt signaling and promoting endothelial cell motility. Overexpression correlates with poor cancer prognosis, making it a promising therapeutic target for anti-tumor and anti-inflammatory strategies.

Fig.1. Heparanase trafficking pathway. (OA Literature) Fig.1 Schematic model of heparanase trafficking.¹

Service Overview

Are you currently facing high background noise in your enzymatic assays or challenges in identifying selective non-anticoagulant inhibitors? Our heparanase development service helps you obtain high-quality kinetic profiles and obtain highly specific structural data through advanced screening and innovative engineering techniques. Creative Biolabs enables you to accelerate drug discovery by identifying potent lead compounds with minimized off-target effects and optimized pharmacological profiles. This comprehensive approach ensures your leads are optimized for enzymatic potency and systemic disease modification in oncology and chronic inflammatory research.

Explore How We Can Assist You

Heparanase Development Workflow

Step 1

Substrate Customization

We design bespoke substrates tailored to your lead compound, progressing from native HS to meticulously synthesized homogeneous pentasaccharides or advanced synthetic mimetics. This approach ensures consistent linear enzymatic kinetics while maximizing specificity for heparanase activity.

Step 2

Enzymatic Kinetic Profiling

Utilizing cutting-edge barrel-inspired computational models, we perform high-throughput screening to differentiate between competitive and non-competitive inhibition mechanisms. This provides actionable insights into inhibitor potency and mode of action.

Step 3

Active Heterodimer Detection

Our ssDNA aptamer-based sandwich ELISA platform delivers precise, quantitative measurement of the catalytically active heparanase heterodimer, with zero cross-reactivity against HPSE-2, ensuring unparalleled analytical fidelity.

Step 4

Functional Validation

Lead candidates undergo rigorous phenotypic testing in 3D invasion assays and secretome profiling, directly linking molecular inhibition to measurable biological outcomes.

Step 5

Structural Docking & Optimization

The final report features high-resolution molecular docking simulations, visualizing inhibitor interactions with critical arginine clusters in the catalytic site. This guides iterative structure-based optimization for superior binding affinity and potency.

Fig. 2. Heparanase development workflow. (Creative Biolabs AI) Fig.2 Development schematic for heparanase.

Why Choose Us?

Creative Biolabs is a global leader in glycobiology, offering specialized features designed to mitigate the inherent challenges of HS heterogeneity. Our screening platforms utilize homogeneous substrates to provide precise kinetic constants, ensuring your data is both reproducible and robust. Unlike traditional methods, we incorporate published data standards to validate every lead, offering a unique dual-detection system that pairs enzymatic activity with structural occupancy. This technical rigor minimizes false positives and accelerates your transition to clinical-stage development, providing high-resolution insights for regulatory success.

Uncover the Ways We Can Support You

Applications

Cancer Metastasis Research
Heparanase development service is pivotal in cancer metastasis studies. High-purity heparanase enables researchers to dissect its role in degrading the extracellular matrix, facilitating tumor cell invasion and spread, and guiding anti-metastasis drug design.

Angiogenesis Investigation
In angiogenesis research, this service provides essential tools. Heparanase's impact on blood vessel formation can be precisely studied using purified enzyme and relevant assays, helping to identify new targets for inhibiting abnormal angiogenesis in diseases.

Inflammatory Disease Studies
For inflammatory diseases, the heparanase development service aids in understanding the enzyme's involvement in inflammation. By analyzing its activity and expression changes, researchers can explore novel therapeutic approaches to modulate the inflammatory response.

Drug Screening and Optimization
This service is crucial for drug discovery against heparanase-related disorders. It offers platforms to screen and optimize small molecules or biologics that target heparanase, accelerating the development of effective therapeutic agents with improved efficacy and safety.

Tissue Engineering Applications
In tissue engineering, the heparanase development service helps regulate extracellular matrix remodeling. By controlling heparanase activity, researchers can optimize the microenvironment for cell growth and tissue regeneration, promoting the development of functional tissue constructs.

Customer Reviews

Enhanced Optimization
"Leveraging the structural docking service has brought about a substantial enhancement in our lead optimization process for TIM-barrel inhibitors, enabling us to achieve more precise and effective results."- Two months ago, Prof. M*o R.

Streamlined Screening
"Incorporating the screening method into our research has greatly streamlined our high-throughput screening campaign. By transitioning to homogeneous pentasaccharides, we've successfully eliminated the kinetic variability issues that were prevalent with native HS, thereby enhancing the reliability and efficiency of our screening process."- Two months ago, Dr. S*a K.

FAQs

Q: What is heparanase, and why is its development service key in biotech and pharma?

A: Heparanase is an enzyme degrading HS proteoglycans in the ECM and basement membranes, involved in angiogenesis, tumor metastasis, etc. Its development service is crucial as it helps explore and control its functions, enabling the development of novel therapies for diseases with heparanase dysregulation, like cancer.

Q: Can you list common services in a heparanase development service package?

A: It usually includes high-quality heparanase production/purification, enzyme activity assays, custom antibody development for heparanase detection, and in vitro/in vivo model development for evaluating heparanase modulation effects, as well as drug discovery and optimization services.

Q: In what ways does heparanase development service help cancer research?

A: Heparanase is upregulated in cancers, promoting invasiveness and metastasis. The service provides purified enzymes for molecular studies, custom antibodies for expression visualization, and models to test heparanase modulators, offering preclinical data for anti-cancer therapy development.

Q: What are the advantages of outsourcing heparanase development service?

A: Outsourcing offers expertise, state-of-the-art facilities, and cost-effectiveness. Specialized providers ensure high-quality results, let clients focus on core tasks, and offer flexible, customized service packages, speeding up projects and reducing costs.

Extended Services

Glycan Tool Enzyme Development Services

Our glycan tool enzyme development service is your gateway to unlocking the full potential of glycans. We engineer high-performance enzymes that enable precise glycan modification, facilitating breakthroughs in drug discovery and disease understanding.

New Amylase Development Services

Our expert team designs novel amylases that offer superior performance, driving efficiency and sustainability in various industrial processes.

How to Contact Us

Creative Biolabs provides a vertically integrated heparanase development service, from structural modeling and HTS to clinical biomarker detection. For detailed project discussions or to request a tailored quote, please reach out to our scientific consulting team.

Reference

Masola, Valentina, et al. "Heparanase: a multitasking protein involved in extracellular matrix (ECM) remodeling and intracellular events." Cells 7.12 (2018): 236. Distributed under Open Access license CC BY 4.0, without modification. https://doi.org/10.3390/cells7120236.

For Research Use Only.

Related Services

Online Inquiry