GPCRs Targeted Drug Development for Brain Tumors

G protein-coupled receptors (GPCRs) targeted drugs for brain tumors aim to inhibit tumor growth by modulating GPCRs signaling pathways, offering a promising therapeutic approach. Alfa Cytology focuses on GPCR-targeted drugs for brain tumors, aiming to develop innovative therapeutic to combat these malignancies.

Introduction to GPCRs in Brain Tumors

G protein-coupled receptors (GPCRs) are widely found in animals and are the largest family of membrane receptor proteins in the human body. They are widely involved in the regulation of cell proliferation, differentiation, migration, and other physiological activities. The structural features and important role in signaling determine that they can be good drug targets for brain tumor drug screening.

Fig 1. Schematic of diverse signalling pathways of G-protein-coupled receptors triggered upon activation of G-protein subunits (α, β and γ). (BYRNE K F, et al., 2021)

Signal Transduction Mechanisms of GPCRs

• Classical G Protein Pathway: The ligand binds to the receptor, activating the heterotrimeric G protein (α, β, γ subunits). The α subunit binds to GTP and dissociates from the β and γ subunits, then regulates downstream effector molecules (such as adenylyl cyclase and phospholipase C), leading to the production of second messengers like cAMP, IP₃, and DAG.
• Non-Canonical Pathway: Some GPCRs transmit signals independently of G proteins through β-arrestin or other proteins (such as the MAPK pathway).

Our Services

Alfa Cytology provides GPCRs targeting screening and discovery services to our clients. We proactively understand our client's specific requirements for brain tumor drug development and facilitate their research and product development, combining years of experience in design, development, and data to deliver satisfactory results for our clients.

Evaluation for GPCRs Targeted Drugs

Alfa Cytology has evaluated GPCR-targeted drugs through a series of in vitro and in vivo experiments. Their research aims to verify the efficacy and safety of these drugs in the treatment of brain tumors, thereby advancing the development of novel therapeutic approaches.

In Vitro Evaluation

• Cell Viability Assay
• Cytotoxicity Assay
• Cytokine Release Assay
• Western Blot for Checkpoint Protein Expression
• RNA Sequencing for Tumor and Immune Cell Analysis
• Co-Culture Assay of Tumor Cells and Immune Cells

In Vivo Evaluation

• In Vivo Tumor Growth Inhibition Study
• Pharmacokinetics (PK) Studies
• Pharmacodynamics (PD) Studies
• Toxicology and Safety Assessment
• Checkpoint Inhibitor Combination Therapy Evaluation

Our Strengths

• Multiple compounds can be screened simultaneously at one time.
• Test flexibility, can provide target-compound binding assays and functional analysis services separately, and provide single concentration or concentration gradient IC₅₀ assay services.
• We provide agonist, antagonist, inverse agonist, and transmodulation screening and evaluation for different types of targets.
• High throughput screening platform based on calcium flow, cAMP quantification, and reporter gene style.

Alfa Cytology leverages rigorously optimized and validated methodologies across all dimensions of GPCR screening to provide exemplary services and outstanding results through our cutting-edge experimental platforms. Our dedicated mission is to accelerate our clients' novel drug discovery and development initiatives for brain tumors. Please contact us to discuss your specific requirements.

Reference

1. BYRNE K F, PAL A, CURTIN J F, et al. G-protein-coupled receptors as therapeutic targets for glioblastoma [J]. Drug Discovery Today, 2021, 26(12): 2858-70.