Membrane Protein

Category: Protein -

The KS-V Peptide team has more than 20 years of high-expression vector design, expression condition screening, membrane protein purification and rapid detection platforms for membrane protein targets based on eukaryotic expression systems.

Protein

Detailed Introduction of Membrane Protein

GPCR proteins

G protein-coupled receptors (GPCRs) are membrane proteins that regulate various cellular responses to external stimuli. It is involved in a variety of diseases and is an important drug target; more than 50% of modern protein drugs are related to GPCRs. As membrane proteins, GPCRs are very large, structurally flexible, and difficult to crystallize.

G protein-coupled receptors are one of the largest members of the receptor protein family. They play important biological functions in the process of cell signal transduction and are important drug targets. Extracellular drugs or ligands bind to different types of receptors, the receptors are activated, and the signals are transmitted to downstream effectors by activating G protein heterotrimers, through second messengers (cAMP or IP-one, etc.) Regulates the activity of membrane ion channels and nuclear transcription.

GPCR target - completed target

GPCR Cell Line Construction Services

● Cell line validation

1. mRNA integration

2. Cell membrane surface expression (specific tags)

3. Has functional activity

● Method development

1. Liposome cis-transfer

2. Lentiviral Infection-Stable Transfection

● Monoclonal cell screening

3 functional cell lines

Validation of 2 blank cell lines

● GPCR cell bank

Further validation using molecular pharmacology and other methods

Fully autonomously constructed GPCR stably transfected cell line

Glucagon receptor family stable cell lines (GLP1R, GIPR, GCGR) have been established, and more GPCR target cell banks are being constructed in batches.

Advantages: The cell line construction cycle is 6-8 weeks, and the functional verification is two weeks.

Fully_autonomously_constructed_GPCR_stably_transfected_cell_line.jpeg

GPCR functional detection case 1 (GPCR coupled with Gαs)

Technology Platform: FlexStation 3, BMG LABTECH CLARIOstar, FLPR

GPCR: β2-adrenergic receptor (β2-adrenergic receptor, β2AR)

Observation indicators: dose-response curve, EC50 of drug

Experiment report: standard report, in line with GLP specification

β2-adrenergic receptor:

GPCR_functional_detection_case_1_(GPCR_coupled_with_Gαs).jpg

Ion channel

As an important target, ion channel is the second largest drug target after GPCR. It occupies an important position in the research and development of new drugs for the central nervous system and cardiovascular system, and is a rapidly growing hot spot in drug research and development. More than 400 genes are known to encode ion channels, and 300 ion channels have been identified. Among them, there are more than 100 druggable targets with known functions, many of which are proven therapeutic targets.

Among them, ligand-gated and voltage-gated ion channels are ranked third and fourth respectively among the top five gene targets of existing drugs. After G protein-coupled receptors (GPCRs) and the nuclear receptor family. At present, the hot areas of ion channel targets include pain (Nav1.7, ASIC, etc.), epilepsy (potassium channel) and cardiac safety evaluation (hERG), etc.