Ace Therapeutics offers GPCR screening and analysis services for antipsychotic drugs. As pioneers in the field, we can leverage our expertise and innovative technology platform to save you time and cost on your discovery programs.

Introduction of GPCR Screening of Antipsychotics

Ligands known to bind to G protein-coupled receptors (GPCRs) include odor molecules, pheromones, hormones, neurotransmitters, chemokines, etc. The structural characteristics of GPCRs and their important role in signal transduction dictate that GPCRs can serve as excellent drug targets for screening therapeutic agents for diseases such as neurological disorders and psychiatric disorders. Accumulating clinical, pharmacological, and genetic evidence suggests that GPCRs play an important role in the induction, development, and treatment of psychiatric disorders and that GPCRs are the most common targets of antipsychotic drugs. It is with this in mind that we offer you our GPCR screening service for antipsychotic drugs.

Fig. 1 Model of GPCR-mediated NMDA receptor pathways in striatopallidal medium-sized spiny neurons. (Komatsu H, et al., 2019)

GPCR Screening Services

Based on the GPCR objectives and requirements provided by the client, Ace Therapeutics can analyze and develop specific protocols for GPCR screening for antipsychotic services and screen for target antipsychotics that meet the requirements. For each type of GPCR, we have developed a unique solution, including the techniques, instruments, and reagents we use. We are also actively exploring new GPCR screening protocols for antipsychotic drugs, which could lead to a range of innovations in the field. Over 100 cell-based human and orphan GPCR assays are available for a variety of direct functional readouts, including second messenger signaling, inhibition of protein recruitment, and receptor internalization. Our services provide you with maximum flexibility to select the ideal screening platform to meet your project needs. Whether you are concerned with hit identification, selective analysis, or lead compound optimization, these services can reduce the time and cost of antipsychotic drug discovery.

GPCRs for Antipsychotic Screening

• Monoamine neurotransmitter transporters (NTTs)
• γ-aminobutyric acid (GABA) transporters
• Taurine transporters (TAUTs)
• Glycine transporters
• Glutamate transporters
• Other amino acid transporters
• Other G protein-coupled receptors (GPCR)

GPCR Screening Process for Antipsychotics

• Identify GPCR targets for screening antipsychotic drugs and develop proprietary experimental protocols accordingly.
• Construct large-scale compound libraries and GPCR screening models for antipsychotic drugs at biochemical, cellular, and animal levels.
• Score and evaluate compounds for efficacy, and obtain candidate compounds by statistical analysis.
• Repeat the previous step to obtain antipsychotic drugs by GPCR screening.

Fig. 2 GPCR screening process of antipsychotics.

Advantages of Our Services

• Multiple assay formats to choose from
• G protein-independent functional assays, including internalization assays, beta-arrestin recruitment assays, and label-free whole-cell assays, are available
• Single concentration or dose-response screens for EC50 and IC50 assays
• Covers over 100 GPCR targets
• Fast turnaround time

Ace Therapeutics offers specialized high-throughput GPCR screening services for the identification of potential GPCR-targeted antipsychotic drugs. If you are interested in this service, please make an inquiry to learn how we can support you in your project.

Reference

1. Komatsu H, Fukuchi M, Habata Y. Potential Utility of Biased GPCR Signaling for Treatment of Psychiatric Disorders. Int J Mol Sci. 2019, 20(13):3207.