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Custom GPCR Production Service

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Creative Biolabs has been known worldwide for its breakthrough GPCR production technology. We have established a strategic and unparalleled MemProArt™ platform applying membrane protein structure-function technology to provide an integrated service for producing G-protein coupled receptor (GPCR) and applying to wide fields. In addition, our excellent scientists in Creative Biolabs will evaluate and analyze the utility of customized GPCR for certain pharmaceutical research and drug discovery. We envision that our GPCR production technology with structure-based drug design know-how will provide future pharmaceutical clients with an innovative, integrated platform for solving more crucial GPCR structures and discovering novel small molecule therapeutic.

Custom GPCR Production Service
Rhodopsin-Like GPCR

G protein–coupled receptors (GPCRs), also known as seven-transmembrane domain receptors and G protein–linked receptors (GPLR), constitute a large protein family of receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses.

As a macromolecule, GPCRs are structurally flexible and dynamic. They adopt different structure, namely conformation, in response to different factors from environment. Change of structure is also termed conformational change. It is believed that a conformational equilibrium exists in GPCR molecule between active and inactive biophysical states. The binding of ligands to GPCR may shift the equilibrium toward the active receptor states. Three types of ligands exist: Agonists, Inverse agonists or Antagonists and Neutral antagonists. It is not yet known how exactly the active and inactive states differ from each other. If we really understand how these receptors work, then we should be able to rationally design ligands to control their function. Using structural knowledge for successful drug discovery remains an ultimate goal in the field.

Custom GPCR Production Service
GPCR: Conformational Change and Signal Transduction

Biochemical and biophysical techniques, such as NMR, X-ray crystallography and mass spectrometry, are providing complementary insights into ligand dependent dynamic equilibrium between different functional states. Additional details revealed by high-resolution structures illustrate the receptors as allosteric machines. The data helps redefining our knowledge of how GPCRs recognize such a diverse array of ligands and how they transmit signals 30 angstroms across the cell membrane; it also sheds light on a structural basis of GPCR allosteric modulation and biased signaling.

Computer modeling plays an important role in creating a comprehensive GPCR structure-function picture by filling remaining gaps in the superfamily, by illustrating molecular interactions and by providing a platform for rational drug discovery.

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