GHSR-Targeted Drug Discovery Services

Introduction

Growth hormone secretagogue receptor (GHSR) is also known as ghrelin receptor. It is encoded by the GHSR gene. GHSR is a member of the G-protein coupled receptor family. The encoded protein may play a role in energy homeostasis and regulation of body weight. Two identified transcript variants are expressed in several tissues and are evolutionary conserved in fish and swine. One transcript, 1a, excises an intron and encodes the functional protein; this protein is the receptor for the Ghrelin ligand and defines a neuroendocrine pathway for growth hormone release. The second transcript (1b) retains the intron and does not function as a receptor for Ghrelin; however, it may function to attenuate activity of isoform 1a. Mutations in this gene are associated with autosomal idiopathic short stature.[provided by RefSeq, Apr 2010]

Direction of Drugs Discovery

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

Drugs

• GHSR Agonist- Macimorelin, TZP-101, GTP-200, RQ-00000005
• GHSR Modulator- Ibutamoren, tabimorelin, ipamorelin, PF-05190457
• GHSR Stimulator- PF-05190457
• GHSR Antagonist- CYT-009-GhrQb, AEZS-123, EP-01492, EP-01492
• GHSR Inhibitor- AwFwLL-NH2, DprwFwLL-NH2, RPKPfQwFwLL-NH2, RwFwLL-NH2

What We Offer

Target Testing

CD BioSciences provides GHSR testing services by ELISA, WB, IF, ICC or IHC assay. The results of GHSR testing are used to evaluate the activities of candidates against GHSR or targeted diseases. You can choose one or more testing ways to detect the level of GHSR 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
•GHSR-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 GHSR-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—Solid tumour/cancer. (show more)
• Other Diseases—Chronic pain, pituitary gland disorder, growth hormone deficiency, fibromyalgia, postoperative ileus, etc.
CD BioSciences will establish the specific disease models according to your requirements to evaluate the inhibitory activity of your candidates targeted GHSR. 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: 34718814.