GRPR-Targeted Drug Discovery Services

Introduction

The gastrin-releasing peptide receptor (GRPR) is a receptor of gastrin-releasing peptide (GRP), which regulates numerous functions of the gastrointestinal and central nervous systems, including release of gastrointestinal hormones, smooth muscle cell contraction, and epithelial cell proliferation and is a potent mitogen for neoplastic tissues. The effects of GRP are mediated through the gastrin-releasing peptide receptor. GRPR is a glycosylated, 7-transmembrane G-protein coupled receptor that activates the phospholipase C signaling pathway. GRPR is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate. An individual with autism and multiple exostoses was found to have a balanced translocation between chromosome 8 and a chromosome X breakpoint located within the gastrin-releasing peptide receptor gene.[provided by RefSeq, Apr 2020]

Direction of Drugs Discovery

• GRPR Antagonist
• GRPR Inhibitor
• GRPR Agonist
• GRPR Modulator
• Developing New Clinical Effects on GRPR from Existing Drugs

Drugs

• GRPR Antagonist- ASP-7147, 177-Lu-NeoB, 177Lu-labelled RM2, bantag-1, bantag-1, PD 168368
• GRPR Inhibitor- RC-3095, JMV 1535, JMV 1693, JMV 1719, JMV 1719
• GRPR Agonist- 177Lu-AMBA, bombesin, MK-5046, neuromedin B
• GRPR Modulator- BIM-26226

What We Offer

Target Testing

CD BioSciences provides GRPR testing services by WB,IF, ICC or IHC assay. The results of GRPR testing are used to evaluate the activities of candidates against GRPR or targeted diseases. You can choose one or more testing ways to detect the level of GRPR 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
• GRPR-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 GRPR-targeted antibody drugs development with professional technology, extensive experience, and advanced equipment.
• Antibody Preparation Services
• Phage Display Services
• Antibody-Drug Conjugates
• Bispecific Antibody 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, solid tumor/cancer, breast cancer. (show more)
• Other Diseases—Agoraphobia, irritable bowel syndrome.
CD BioSciences will establish the specific disease models according to your requirements to evaluate the inhibitory activity of your candidates targeted GRPR. We have various cell lines and the species of our animal models cover rats, mice, rabbits, dogs, and non-human primates.

Inquire Us

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: 34718759.