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.
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.
Receptor Family (Human) | Nomenclature | G Protein Coupling | Host Cell Line |
Adrenoceptors | Alpha 1A receptor | Gq family | HEK293T |
Alpha 2A receptor | Gi family | HEK293T | |
Alpha 2B receptor | Gi family | HEK293T | |
Beta 1 receptor | Gs family | HEK293T | |
Beta 2 receptor | Gs family | HEK293T | |
Cannabinoid receptors | CB1 receptor | Gi/Go family | HEK293T |
CB2 receptor | Gi/Go family | HEK293T | |
Chemokine receptors | CCR1 receptor | Gi/Go family | HEK293T |
CCR2 receptor | Gi/Go family | HEK293T | |
CCR3 receptor | Gi/Go family | HEK293T | |
Somatostatin receptors | SSTR1 receptor | Gi/Go family | HEK293T |
SSTR2 receptor | Gi/Go family | HEK293T | |
SSTR3 receptor | Gi/Go family | HEK293T | |
SSTR4 receptor | Gi/Go family | HEK293T |
Receptor Family (Human) | Nomenclature | G Protein Coupling | Host Cell Line |
Glucagon receptor family | GHRH receptor | Gs family | HEK293T |
glucagon receptor | Gs family | HEK293T | |
GLP-1 receptor | Gs family | HEK293T | |
GIP receptor | Gs family | HEK293T | |
Tachykinin receptors | NK1 receptor | Gs family | HEK293T |
NK2 receptor | Gs family | HEK293T | |
NK3 receptor | Gq/G11 family | HEK293T | |
Vasopressin and oxytocin receptors | OT receptor | Gq/G11 family | HEK293T |
Calcium-sensing receptor | CaS receptor | Gq/G11 family | HEK293T |
Endothelin receptors | ETA receptor | Gq/G11 family | HEK293T |
Opioid receptors | δ receptor | Gi/Go family | HEK293T |
κ receptor | Gi/Go family | HEK293T | |
μ receptor | Gi/Go family | HEK293T |
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
1. 3 functional cell lines
2. Validation of 2 blank cell lines
● GPCR cell bank
Further validation using molecular pharmacology and other methods
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.
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.
Voltage gated ion channels | |
Voltage-gated potassium channels | Kv1.1,Kv1.2,Kv1.3,Kv1.4,Kv1.5,KV11.1(HERG),Kv1.6,KCNE1,KCNQ1 |
Sodium channels | NaV1.4,NaV1.5,NaV1.6,NaV1.7 |
hyperpolarization inward rectifying potassium channel | KAT1 |
Ca2+-Activated potassium Channel | KCa3.1 |
Acid sensitive ion channels | ASIC1a,ASIC1b,ASIC2a,ASIC2b,ASIC3 |
Calcium channels | CaV2.1(P/Q-type),CaV2.2 (N-type),CaV3.2 (T-type),CaV1.2 (L-type) |
Chloride channel | CLCN1, CTFR |
Ligand gated ion channels | |
Ach | nAchR α9,nAchR α10 |
GABA | GABAA1-GABAA6 |
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.
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.
Receptor Family (Human) | Nomenclature | G Protein Coupling | Host Cell Line |
Adrenoceptors | Alpha 1A receptor | Gq family | HEK293T |
Alpha 2A receptor | Gi family | HEK293T | |
Alpha 2B receptor | Gi family | HEK293T | |
Beta 1 receptor | Gs family | HEK293T | |
Beta 2 receptor | Gs family | HEK293T | |
Cannabinoid receptors | CB1 receptor | Gi/Go family | HEK293T |
CB2 receptor | Gi/Go family | HEK293T | |
Chemokine receptors | CCR1 receptor | Gi/Go family | HEK293T |
CCR2 receptor | Gi/Go family | HEK293T | |
CCR3 receptor | Gi/Go family | HEK293T | |
Somatostatin receptors | SSTR1 receptor | Gi/Go family | HEK293T |
SSTR2 receptor | Gi/Go family | HEK293T | |
SSTR3 receptor | Gi/Go family | HEK293T | |
SSTR4 receptor | Gi/Go family | HEK293T |
Receptor Family (Human) | Nomenclature | G Protein Coupling | Host Cell Line |
Glucagon receptor family | GHRH receptor | Gs family | HEK293T |
glucagon receptor | Gs family | HEK293T | |
GLP-1 receptor | Gs family | HEK293T | |
GIP receptor | Gs family | HEK293T | |
Tachykinin receptors | NK1 receptor | Gs family | HEK293T |
NK2 receptor | Gs family | HEK293T | |
NK3 receptor | Gq/G11 family | HEK293T | |
Vasopressin and oxytocin receptors | OT receptor | Gq/G11 family | HEK293T |
Calcium-sensing receptor | CaS receptor | Gq/G11 family | HEK293T |
Endothelin receptors | ETA receptor | Gq/G11 family | HEK293T |
Opioid receptors | δ receptor | Gi/Go family | HEK293T |
κ receptor | Gi/Go family | HEK293T | |
μ receptor | Gi/Go family | HEK293T |
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
1. 3 functional cell lines
2. Validation of 2 blank cell lines
● GPCR cell bank
Further validation using molecular pharmacology and other methods
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.
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.
Voltage gated ion channels | |
Voltage-gated potassium channels | Kv1.1,Kv1.2,Kv1.3,Kv1.4,Kv1.5,KV11.1(HERG),Kv1.6,KCNE1,KCNQ1 |
Sodium channels | NaV1.4,NaV1.5,NaV1.6,NaV1.7 |
hyperpolarization inward rectifying potassium channel | KAT1 |
Ca2+-Activated potassium Channel | KCa3.1 |
Acid sensitive ion channels | ASIC1a,ASIC1b,ASIC2a,ASIC2b,ASIC3 |
Calcium channels | CaV2.1(P/Q-type),CaV2.2 (N-type),CaV3.2 (T-type),CaV1.2 (L-type) |
Chloride channel | CLCN1, CTFR |
Ligand gated ion channels | |
Ach | nAchR α9,nAchR α10 |
GABA | GABAA1-GABAA6 |