Inter G-Protein Heterotrimer Interaction Assay Services

Heterotrimeric G proteins control a wide range of physiological and pathological processes and act as molecular switches in GPCR signaling pathways. More than 30% of currently prescribed medications target GPCRs because they are effective pharmacological targets. Targeting a single GPCR specifically, however, might not be the best course of action in a number of complex disorders when several receptors are implicated. Furthermore, illnesses are often linked to aberrant G protein expression or activation. Moreover, mutations in G proteins frequently cause cancerous illnesses. Therefore, targeting G proteins rather than GPCRs may offer different strategies for treating these illnesses. Creative Biolabs offers inter G-protein heterotrimer interaction assay services to meet the requirement of GPCR drug discovery.

G Protein and Diseases

Heterotrimeric G proteins are significant signal transduction proteins that play a major role in the development and progression of numerous diseases in addition to controlling a number of basic physiological functions. G proteins are either overexpressed or incorrectly activated in some disorders, thus their properties differ from those of normal states. Furthermore, constitutive activation of G proteins is frequently triggered by mutations at particular residues, and this is a crucial factor in the advancement of disease. The growing body of research on G proteins has led to a progressive elucidation of the causal relationships between many disease types and G protein signaling pathways in recent times. With all the advancements made, targeting G proteins may offer novel therapeutic options for the management of these diseases.

Targeting G proteins may offer novel therapeutic options for many diseases. (Li, Jian, et al, 2019) Fig.1 G protein-related diseases.¹

G Protein Inhibitors

G protein inhibitor development is a promising yet difficult area of medicine discovery for associated disorders. Only Gαq/11, out of the four G protein subfamilies, contains natural depsipeptides that are available as selective inhibitors and have demonstrated remarkable potential in multiple preclinical investigations. Conversely, there hasn't been any information released about specific small molecules for Gαi, Gαs, or Gα12/13, among other G protein subfamilies. It is imperative that selective, effective, and synthetically feasible G protein inhibitors be developed. This will not only give G protein inhibitors usefulness as tool chemicals but also make it easier to investigate the therapeutic potential of G proteins in drug discovery.

G proteins have not been thoroughly investigated yet are viable pharmacological targets. The absence of effective and selective inhibitors that can precisely alter their activity is one of the main obstacles to their research. To support research on the therapeutic potential of heterotrimeric G proteins in drug discovery, ongoing efforts are required to create selective and effective G protein inhibitors. Creative Biolabs offers inter G-protein heterotrimer interaction assay services to help the development of G protein inhibitors. Please contact us for more information about our services.

Reference

Li, Jian, et al. "Heterotrimeric G proteins as therapeutic targets in drug discovery." Journal of Medicinal Chemistry 63.10 (2019): 5013-5030.

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