PCSK9-Targeted Drug Discovery Services

Introduction

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is encoded by the PCSK9 gene in humans. This gene encodes a member of the subtilisin-like proprotein convertase family, which includes proteases that process protein and peptide precursors trafficking through regulated or constitutive branches of the secretory pathway. The encoded protein undergoes an autocatalytic processing event with its prosegment in the ER and is constitutively secreted as an inactive protease into the extracellular matrix and trans-Golgi network. It is expressed in liver, intestine, and kidney tissues and escorts specific receptors for lysosomal degradation. It plays a role in cholesterol and fatty acid metabolism. Mutations in this gene have been associated with autosomal dominant familial hypercholesterolemia. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Feb 2014]

Direction of Drugs Discovery

• PCSK9 Modulator
• PCSK9 Inhibitor
• Developing New Clinical Effects on PCSK9 from Existing Drugs

Drugs

• PCSK9 Modulator- PCSK9 Adnectin, AMG 145
• PCSK9 Inhibitor- SPC5001

What We Offer

Target Testing

CD BioSciences provides PCSK9 testing services by ELISA, Flow, WB, IHC, ICC, or IF assay. The results of PCSK9 testing are used to evaluate the activities of candidates against PCSK9 or targeted diseases. You can choose one or more testing ways to detect the level of PCSK9 according to your experiment.

Hit Identification (show more)

The goal of early drug discovery is to find novel lead compounds that have the desired potency, selectivity, and ADMET properties for pre-clinical evaluation.
CD BioSciences offers hit identification services to make your finding of targeted compounds more successful and faster.
• High-Throughput Screening
• PCSK9-Targeted in Silico Virtual Screening
• Fragment-Based Screening
• High-Content Screening

Antibody Drugs Development Services (show more)

Antibody drugs exhibit many incomparable advantages, such as high specificity, affinity, and efficiency, which is an emerging direction on targeted drug development. CD BioSciences provides comprehensive services on PCSK9-targeted antibody drugs development with professional technology, extensive experience, and advanced equipment.
• Antibody Preparation Services
• Phage Display Services
• Antibody-Drug Conjugates
• Bispecific Antibody Services
• Antibody Humanization Services

Pharmacological Experiments (show more)

We will create a specific experimental plan according to your requirements, including but not limited to
• Pharmacokinetics / Pharmacodynamics
• Pharmacodynamics
• Pharmacokinetics
• Safety Pharmacology

Disease Models Screening (show more)

We will create specific disease models to accelerate your targeted drug discovery project, including but not limited to
• Cancers—Prostate cancer, breast cancer, colorectal carcinomas, etc. (show more)
• Other Diseases—Hypercholesterolemia.
CD BioSciences will establish the specific disease models according to your requirements to evaluate the inhibitory activity of your candidates targeted PCSK9. We have various cell lines and the species of our animal models cover rats, mice, rabbits, dogs, and non-human primates.

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References

1. Stelzer G.; et al. The GeneCards Suite: From Gene Data Mining to Disease Genome Sequence Analysis, Current Protocols in Bioinformatics (2016), 54:1.30.1 - 1.30.33.doi: 10.1002 / cpbi.5.
2. Wishart DS; et al. DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue): D901-6.
3. Y. Zhou; et al. Therapeutic target database update 2022: facilitating drug discovery with enriched comparative data of targeted agents. Nucleic Acids Research. 50(D1): 1398-1407 (2022). PMID: 34718949.