Latest Scientific Insight

Multiscreen 231-GPCR Cell-Based Assay Panel

GPCRs have historically been among the most important classes of pharmaceutical targets across a wide range of clinical indications. Recent clinical, scientific and technical advances have also opened new therapeutic avenues to exploit members of this class. In this paper, we discuss how Multispan’s MULTISCREEN GPCR panel can provide important insights during the development of new compounds and in repurposing existing therapies.

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GPCR Mutants

How mutagenesis enables understanding structure/function relationships of GPCRs. Read full article.

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Building Better Drugs

Every year, researchers invest billions of dollars toward clinical approval of innovative new drug compounds. However, the U.S. Federal Drug Administration (FDA) only accepts a select number of new chemical entries every year. In fact, from 2011 to 2018, the FDA only approved 309 new drugs. While this is a marked improvement from the approval rate of decades prior, it still points to the administration’s selectivity. One way to streamline the drug development process? Invest in assay development. This analytical function is key to high-quality drug discovery research. Today, we’re diving into the important role it plays. Ready to learn more? Let’s dive in!

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Targeting Allosteric Modulation and Cell Signaling Bias: Strategies and Tools to Develop a Better GPCR Targeted Therapeutic

An allosteric modulator binds to an allosteric site on a protein, such as a receptor or enzyme, distinct from the active site, which alters the activity of the protein. This modulation of enzyme and receptor function differs from that of traditional agonists and antagonists. A positive allosteric modulator will enhance the affinity and/or efficacy of a receptor for its endogenous ligand or agonist, and increase the catalytic activity for enzymes. A negative allosteric modulator will reduce the affinity and/or efficacy of the receptor, and decrease the catalytic activity for enzymes.

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