Eurofins Discovery
과발현 세포주
Eurofins DiscoverX는 안정적으로 발현된 표적 단백질을 연구하기 위해 설계된 Stable Cell Line을 제공합니다. 이 세포주는 약물 스크리닝, 표적 검증 및 생물학적 경로 분석에 적합하며, 신뢰할 수 있는 데이터와 간편한 프로토콜을 보장합니다.
제품 소개
Eurofins DiscoverX의
Stable Cell Line은 특정 표적 단백질을 안정적으로 발현하도록 제작되어, 약물
개발 과정에서 효율적인 Workflow와 일관성 있는 데이터를 제공합니다. 다양한 생리학적 경로와 분자 기전을 연구하며 반복 실험이 필요할 때 유용하게 이용될 수 있습니다.
대표 제품군 및 Assay Application
|
Target
Class |
Example |
Assay
Measures |
|
GPCR |
GLP1R |
cAMP Accumulation β-Arrestin Recruitment Internalization Calcium Flux Pharmacotrafficking Translocation |
|
Kinase |
KDR |
Target Engagement Dimerization Functional Activity Targeted Protein Degradation (TPD) |
|
Epigenetic |
SMARCA4 |
Target Engagement Pharmacotrafficking |
|
Ion
Channel |
hERG |
Electrophysiology |
|
Checkpoint
Receptor |
PD-1 |
Cytotoxicity (ADCC, ADCP, CDC) Dimerization |
주요 특징
- 안정적인 단백질 발현: 표적 단백질의 지속적인 발현으로 실험 결과의 일관성 보장
- 다양한 응용 분야: 약물 스크리닝, SAR 연구, 표적 검증 및 경로 분석
- 고품질 세포주: 엄격한 품질 관리로 높은 신뢰성과 재현성 제공
- 사용 편리성: 표준화된 프로토콜과 함께 제공되어 실험 준비 시간 단축
응용 분야
- GPCR, 키나아제, 이온 채널 등 다양한 표적 연구
- 약물 활성 평가 및 효능 분석
- 생리학적 경로 및 분자 기전 연구
Simple Workflow
예시: GPCR β-Arrestin 세포주 Workflow
Target List
A
ACKR1
ADCYAP1R1 (PAC1)
ADGRA1 (GPR123)
ADGRB1 (BAI1)
ADGRB2 (BAI2)
ADGRB3 (BAI3)
ADGRG3 (GPR97)
ADORA1 (A1)
ADORA2A (A2A)
ADORA2B (A2B)
ADORA3 (A3)
ADRA1A
ADRA1B
ADRA1D
ADRA2A
ADRA2B
ADRA2C
ADRB1
ADRB2
ADRB3
AGTR1 (AT1)
AGTR2 (AT2)
Amylin (CALCR-RAMP3)
APJ (AGTRL1)
AVPR1A
AVPR1B
AVPR2
B
BDKRB1
BDKRB2
BRS3 (BB3)
C
C3AR1 (C3a)
C5AR1 (C5a)
C5L2 (C5a2)
Calcium
CALCR (No RAMP)
CALCR-RAMP1 (AMY1)
CALCR-RAMP2 (AMY2)
CALCRL-RAMP1 (CGRP)
cAMP
CASR (CaS)
CCKAR (CCK1)
CCKBR (CCK2)
CCR1 (MIP-1a/RANTES-R)
CCR10 (CCL27R)
CCR2 (MIP-1R)
CCR3
CCR4
CCR5 (MIP-1/RANTES-R)
CCR6 (MIP-3α)
CCR7 (CCL19)
CCR8
CCR9
CCRL1 (ACKR4)
CCRL2
CDC25A (MPIP1)
CHRM1
CHRM2
CHRM3
CHRM4
CHRM5
CMKLR1
CNR1 (CB1)
CNR2 (CB2)
CRHR1
CRHR2
CRTH2 (PTGDR2, DP2)
CX3CR1 (Fractalkine)
CXCR1 (IL8RA)
CXCR2 (IL8RB)
CXCR3 (IP-10R)
CXCR4 (SDF-1R)
CXCR5 (BLR-1)
CXCR5 (BLR1)
CXCR6
CXCR6 (CCL16R)
CXCR7 (ACKR3)
CXCR7 (CMKOR1)
CysLT1
CYSLTR2
D
DRD1
DRD2
DRD3
DRD4
DRD5
E
EDG1 (S1P1)
EDG2 (LPA1)
EDG3 (S1P3)
EDG4 (LPA2)
EDG5 (S1P2)
EDG6 (S1P4)
EDG7 (LPA3)
EDG8 (S1P5)
EDNRA
EDNRB
F
F2R (PAR1)
F2RL1 (PAR2)
F2RL3 (PAR4)
FFAR1 (GPR40)
FFAR2 (GPR43)
FFAR3 (GPR41)
FPR1
FPR2 (FPRL1)
FPR3
FSHR
G
GABBR1-GABBR2
GALR1
GALR2
GCGR
GCGR (GCR)
Gcgr (GL-R)
GHRHR (GHRFR)
GHSR (Ghrelin)
GIP
GIP (GIPR)
GLP-1 (GLP1R)
GLP-2 (GLP2R)
GLP1R
GNRHR
GPBAR1 (GPCR19)
GPR1
GPR101
GPR103 (QRFPR)
GPR107
GPR109A
GPR109B
GPR119
GPR12
GPR120
GPR120 (L)
GPR120 (S)
GPR132
GPR135
GPR137 (TM7SF1)
GPR139
GPR141
GPR142
GPR143
GPR146
GPR148
GPR149
GPR15
GPR150
GPR151
GPR152
GPR157
GPR161
GPR162
GPR17
GPR171
GPR173
GPR176
GPR18
GPR182
GPR183 (EBI2)
GPR20
GPR22
GPR23
GPR25
GPR26
GPR27
GPR3
GPR30
GPR31
GPR32
GPR34
GPR35
GPR37 (EDNRBL)
GPR37L1
GPR39
GPR4
GPR45
GPR50
GPR52
GPR55
GPR6
GPR61
GPR65
GPR68 (OGR1)
GPR75
GPR78
GPR79
GPR81
GPR83
GPR84
GPR85
GPR88
GPR91 (SUCNR1)
GPR92 (LPA5)
GRM1 (mGlu1)
GRM2 (mGlu2)
GRM3 (mGlu3)
GRM4 (mGlu4)
GRM5 (mGlu5)
GRM6 (mGlu6)
GRPR (BB2)
H
HCRTR1 (OX1)
HCRTR2 (OX2)
HRH1 (H1)
HRH2 (H2)
HRH3 (H3)
HRH4 (H4)
HTR1A (5-HT1A)
HTR1B (5-HT1B)
HTR1E (5-HT1E)
HTR1F (5-HT1F)
HTR2A (5-HT2A)
HTR2B (5-HT2B)
HTR2C (5-HT2C)
HTR4 (5-HT4)
HTR5A (5-HT5A)
HTR6 (5-HT6)
HTR7 (5-HT7)
K
KISS1R
L
LGR4
LGR5
LGR6
LHCGR
LTB4R
M
MC1R
MC2R (ACTH)
MC3R
MC4R
MC5R
MCHR1
MCHR2
MLNR (Motilin)
MRGPRD
MRGPRE
MRGPRF
MRGPRX1
MRGPRX2
MRGPRX4
MTNR1A
MTNR1B
N
NMBR
NMU1R
NMU2R
NPBWR1 (GPR7)
NPBWR2 (GPR8)
NPFFR1
NPSR1b (NPSR1)
NPY1R
NPY2R (PYY)
NPY4R (PPYR1)
NTSR1
O
OPN5 (Opsin)
OPRD1 (Opioid δ)
OPRK1 (Opioid κ)
OPRL1 (Opioid)
OPRM1 (Opioid µ)
OXER1
OXGR1 (GPR80, GPR99)
OXTR
P
P2RY1
P2RY11
P2RY12
P2RY2
P2RY4
P2RY6
P2RY8
PRLHR
PROKR1
PROKR2
PTAFR
PTGDR
PTGER1
PTGER2
PTGER3 (PGE2-R)
PTGER4
PTGFR
PTGIR
PTHR1
PTHR2
R
RHO(P23H)
RXFP1 (LGR7)
RXFP2 (LGR8)
RXFP3 (SALPR)
RXFP4
S
SCTR
SMO
SSTR1
SSTR2
SSTR3
SSTR4
SSTR5
T
TAAR1
TAAR5
TACR1
TACR2
TACR3
TBXA2R
TRHR
TSHR(L)
U
UTR2
V
VIPR1
VIPR2
X
XCR1
B
BCMA
BTLA
C
CD137 (4-1BB)
CD200
CD200R
CD28
CD33 (SIGLEC3)
CD47
CD80
CD86
CTLA4
F
FcyRIIb
FcγR1a
FcγRIIa
H
HVEM
I
ICOS
L
LAG3
LAIR1
O
OX40
P
PD-1
PD-L1
PD-L2
S
Siglec9
SIRPa
T
TIM3
TREm1-DAP12
V
VISTA
VISTA/VISTA
A
A-Raf
AAK1
Abl
ACK1
ACTR2
ActRIIB
ACVR1/ACVR2
ACVR1B/BMPR2
ACVR1C/ACVR2
ACVR1C/ACVR2B
ACVRL1/ACVR2
ACVRL1/ACVR2B
ACVRL1/BMPR2
ADP
Akt1 (PKBα)
Akt2 (PKBβ)
Akt3 (PKBγ)
ALK
ALK1
ALK2
ALK4
ALK6
AMHR2/BMPR1A
AMPK
AMPK (α1, β1, γ1)
AMPK (α2, β1, γ1)
Arg
Ask1
ATM
ATR (ATRIP)
Aurora A
Aurora B
Aurora C
Axl
B
B-Raf
BIKe
Blk
BMP-4
BMP-6
BMP-7
BMPR1A/ACVR2
BMPR1A/ACVR2A
BMPR1A/ACVR2B
BMPR1A/BMPR2
BMPR1B/ACVR2A
BMPR1B/ACVR2B
BMPR1B/BMPR2
BMPR2
BMS-564929
Bmx
BRAF1(V600E)
BRK
BrSK1
BrSK2
BTK
C
c-Kit
c-RAF
c-Ret-GFRα1
c-Ret-GFRα2
c-Ret-GFRα3
CaMKI
CaMKIIα
CaMKIIβ
CaMKIIγ
CaMKIIδ
CaMKIV
CaMKIβ
CaMKIγ
CaMKIδ
CaMKK1
CaMKK2
Cdc7 (cyclin B1)
CDK1 (cyclin B)
CDK14 (cyclin Y)
CDK15/cyclin Y
CDK16 (cyclin Y)
CDK17 (cyclin Y)
CDK18 (cyclin Y)
CDK2 (cyclin A)
CDK2 (cyclin E)
CDK3 (cyclin E)
CDK4 (cyclin D3)
CDK5 (p25)
CDK5 (p35)
CDK6 (cyclin D3)
CDK7 (cyclin H, MAT1)
CDK9 (cyclin T1)
CDKL1
CDKL2
CDKL3
CDKL4
CDKL5
CDKN1A (p21)
ChaK1
CHK1
CHK2
CK1α
CK1γ1
CK1γ2
CK1γ3
CK1γδ
CK1ε
CK2α
CK2α2
CLIK1
CLK1
CLK2
CLK3
CLK4
COT1
CRIK
CSF1R
CSF1R/CSF1R
CSK
CSNK1A1L
D
DAPK1
DAPK2
DCAMKL1
DCAMKL2
DCAMKL3
DDR1
DDR2
DMPK
DNA-PK
DRAK1
DRAK2
DYRK1A
DYRK1B
DYRK2
DYRK3
E
eEF-2K
EGFR
EGFR/ErbB2
EGFR/ErbB3
EphA1
EphA2
EphA3
EphA4
EphA5
EphA7
EphA8
EphB1
EphB2
EphB3
EphB4
EphrinA3
EphrinB2-Fc
ErbB2
ErbB2-ErbB3
ErbB2/ErbB3
ErbB2/ErbB4
ErbB4
ErbB4/ErbB4
Erk1 (MAPK3)
Erk2 (MAPK1)
F
FAK
Fer
Fes (Fps)
FGFR1
FGFR1-α-Klotho
FGFR1-β-Klotho
FGFR2
FGFR3
FGFR3(G380R)/FGFR3(G380R)
FGFR3/FGFR3
FGFR4
FGFR4-α-Klotho
FGFR4-β-Klotho
FGR
Flt1
FLT3
FLT4
Fyn
G
GAK
GCK
GCN2
GDF-2
GRK1
GRK2
GRK3
GRK4
GRK5
GRK6
GRK7
GSK3α
GSK3β
H
haspin
Hck
HIPK1
HIPK2
HIPK3
HIPK4
HPK1
HRI
I
ICK
IGF1R
IKKα
IKKβ
IKKε
INSR
IRAK1
IRAK4
IRE1
IRR
Itk
J
JAK1
JAK2
JAK3
JNK1α1 (SAPK1c)
JNK2α2 (SAPK1a)
JNK3 (SAPK1b)
K
KDR
L
LATS1
LATS2
Lck
LIMK1
LIMK2
LKB1
LOK
LRRK2
LTK
Lyn
M
MAK
MAP3K19
MAP3K8 (COT)
MAP4K3
MAP4K4
MAP4K5
MAPKAPK2
MAPKAPK3
MARK1
MARK3
MARK4
MAST1
MATK
MEK1
MEK2
MEKK2
MEKK3
MELK
Mer
MET (c-MET)
MET (c-MET)/EGFR
MINK
MKK3
MKK4
MKK6
MLCK
MLK1
MLK2
MLK3
MLK4
Mnk2
MOK
MRCKg
MRCKα
MRCKβ
MSK1
MSK2
MSSK1
MST1
MST2
MST3
MST4
mTOR (FRAP1)
MuSK
MYLK2
MYO3A
MYO3B
N
NDR1
NDR2
NEK1
NEK10
NEK11
NEK2
NEK3
NEK4
NEK5
NEK6
NEK7
NEK9
NIK
NIM1
NLK
NuaK1 (ARK5)
NUAK2
O
OSR1
P
p38α (SAPK2a)
p38β2 (SAPK2b2)
p38γ (SAPK3)
p38δ (SAPK4)
p70S6K
PAK1
PAK2
PAK3
PAK4
PAK5
PAK6
PAR-1Ba
PASK
PDGFRa
PDGFRb
PDHK2
PDHK4
PDK1
PEK
PhKg1
PhKg2
PI3K-C2α
PI3K-C2β
PI3K-C2γ
PI3Kα
PI3Kα (E542K)
PI3Kα (E545K)
PI3Kα (H1047R)
PI3Kα (p65α)
PI3Kα (p85α)
PI3Kβ (p85α)
PI3Kγ
PI3Kδ
PI3Kδ (p85α)
PI4KA
PIK3C3
PIKFYVE
PIM1
PIM2
PIM3
PIP4K2α
PIP5K1α
PIP5K1γ
PKA
PKAcb
PKCα
PKCβI
PKCβII
PKCγ
PKCδ
PKCε
PKCζ
PKCη
PKCθ
PKCι
PKCµ
PKD2
PKD3 (PKC nu)
PKG1α
PKG1β
PKR
PLCG1
Plk1
PLK3
PRAK
PRK1 (PKN1)
PRK2
PRKG2 (cGK2)
PrKX
PTK5
PYK2
R
Ret
RIPK1
RIPK2
RIPK3
ROKα (ROCK-II)
ROKβ (ROCK-I)
Ron
Ros
Rsk1
Rsk2
Rsk3
Rsk4
S
SGK1
SGK2
SGK3
SIK1
SIK2
SIK3
SLK
SMG1
SNRK
Src
SRPK1
SRPK2
STK25
STK32A
STK33
STK39
Syk
T
Tak1
TAO1
TAO2
TAO3
TBK1
Tec
TGFBR1
TGFBR1/ACVR2
TGFBR1/ACVR2B
TGFBR1/TGFBR2
TGFBR1/TGFBR2/ENG
TGFBR1A/ACVR2A
Tie2
TLK1
TLK2
TrkA
TrkA-P75
TrkB
TrkB-P75
TrkC
TrkC-P75
TSSK1
TSSK2
TSSK3
TSSK4
TTBK2
TTK
Txk
TYK2
TYRO3 (Rse)
U
ULK1
ULK2
ULK3
V
VEGF (VEGFR2, KDR)
VRK2
W
WEE1
WNK2
WNK3
Y
YES1
Z
ZAK
ZAP-70
ZIPK
A
Abl
ACK1
ALK
Arg
Axl
B
Blk
Bmx
BRK
BTK
C
c-Kit
c-Ret-GFRα1
c-Ret-GFRα2
c-Ret-GFRα3
CD45
CDC25A (MPIP1)
CSF1R
CSF1R/CSF1R
CSK
D
DDR1
DDR2
DUSP22
E
EGFR
EGFR/ErbB2
EGFR/ErbB3
EphA1
EphA2
EphA3
EphA4
EphA5
EphA7
EphA8
EphB1
EphB2
EphB3
EphB4
EphrinA3
EphrinB2-Fc
ErbB2
ErbB2-ErbB3
ErbB2/ErbB3
ErbB2/ErbB4
ErbB4
ErbB4/ErbB4
F
FAK
Fer
Fes (Fps)
FGFR1
FGFR1-α-Klotho
FGFR1-β-Klotho
FGFR2
FGFR3
FGFR3(G380R)/FGFR3(G380R)
FGFR3/FGFR3
FGFR4
FGFR4-α-Klotho
FGFR4-β-Klotho
FGR
Flt1
FLT3
FLT4
Fyn
H
Hck
HePTP
I
IGF1R
INSR
IRR
Itk
J
JAK1
JAK2
JAK3
K
KDR
L
Lck
LMPTP
LTK
Lyn
M
MATK
Mer
MET (c-MET)
MET (c-MET)/EGFR
MKP5
MuSK
P
PDGFRa
PDGFRb
PTK5
PTP-1B
PTPMEG-1
PTPMEG-2
PTPN22
PTPβ
PYK2
R
Ret
Ron
Ros
RPTPµ
S
SHP-1
SHP-2
Src
Syk
T
TCPTP
Tec
Tie2
TMDP
TrkA
TrkA-P75
TrkB
TrkB-P75
TrkC
TrkC-P75
Txk
TYK2
TYRO3 (Rse)
V
VEGF (VEGFR2, KDR)
VHR
Y
YES1
YopH
Z
ZAP-70
B
BAZ2A
BRD2
BRD3
BRD4
BRDT
D
DOT1L
E
EHMT1
EP300
G
G9a (EHMT2)
H
HAT1
J
JMJD2A (KDM4A)
JMJD2B
JMJD2C
JMJD2D
JMJD2E
JMJD3
K
KAT2A (GCN5L2)
N
NSD1
P
PHF8
PRMT1
PRMT3
S
SETD2
SETD7
SETD8
Sirtuin 1
Sirtuin 2 (SIRT2)
SMARCA4
SUV39H2
SUV4-20H2 (KMT5C)
T
TAF1L(2)
W
WHSC1 (NSD2, MMSET)
A
ASIC3
C
Cav1.2
Cav2.2
Cav3.2
CFTR
G
GABAA α1/β3/γ2
GABAA α3/β3/γ2
GABAA α4/β3/γ2
GABAA α5/β3/γ2
GABAA α6/β3/γ2
GluR6
GlyRA1
H
HCN1
HCN2
HCN3
HCN4
hERG
K
KCNQ1/hminK
Kir2.1
Kir6.2/SUR2A
Kv1.1
Kv1.2
Kv1.3
Kv1.4
Kv1.5
Kv1.6
Kv1.7
Kv1.8
Kv12.2
Kv2.1
Kv2.1/Kv9.2
Kv3.1
Kv3.2
Kv3.3
Kv4.2/KChIP2
Kv4.3/KChIP1
Kv4.3/KChIP2
Kv7.2/Kv7.3
Kv7.3/Kv7.5
Kv7.4
Kv7.4/Kv7.5
N
nAChR α1/β1/δ/ε
nAChR α3/β4
nAChR α4/β2
nAChR α7/ric3
Nav1.1
Nav1.2
Nav1.3
Nav1.4
Nav1.5
Nav1.6
Nav1.7
Nav1.8
Nav1.8/β1
T
TRPA1
TRPV1
TRPV3
TRPV4
데이터 자료
Figure 1. Assay Formats for Your Modality and Stage of Development.
Figure 2. E3 ligase inhibitors stabilize target proteins.
HCT116 CDKN1A-ED (p21) cell line testing with idasanutlin and nutlin3. CDKN1A (p21) Biosensor is a surrogate readout for TP53 protein stability.
Figure 3. Lipid ligands and lysophospholipid GPCRs tend to be problematic to work with.
Figure 4. Lipid ligands and lysophospholipid GPCRs tend to be problematic to work with.
The difficult to study GPCR lysophospholipid, EDG2 (also called LPA1 or LPAR1), was evaluated for β-arrestin recruitment using the ligand 1-Oleoyl-LPA. A CHO-K1 human EDG2-PK cell line was retrovirally infected with PathHunter β-arrestin2 Retroparticles and assayed for β-arrestin recruitment. Results revealed successful measurement of β-arrestin recruitment upon ligand stimulation and acceptable signal:background of 2.6.
Figure 5. HitHunter cAMP assays provide powerful tools for drug discovery screening and revealing of the correct ligand rank order and pharmacological profile.
Profiling experiment using a cAMP Hunter CHO-K1 adrenergic receptor β2 cell line to test five agonists. The data highlights the receptor’s sensitivity to the various agonists, ultimately revealing the correct rank order of the agonists and showing the agonist salbutamol (EC50 of 160 nM) is less potent than the control ligand isoproterenol (EC50 of 1.7 nM).
추천대상
안정적으로 타깃 발현을 확인했어요
박OO | 제약회사 연구원
타깃 발현이 안정적이어서 약물 스크리닝 실험에서 신뢰할 수 있는 데이터를 얻을 수 있었습니다.
원하는 GPCR 타깃 세포주 구비되어 편리해요
김OO | 제약회사 연구원
원하는 타깃 세포주가 있어서 유용하게 활용했습니다.
데이터가 잘 나와서 프로젝트 진행이 원활해요
송OO | 바이오텍 연구원
Window 값이 좋아서 계속해서 잘 이용 중입니다.
자료 (6)
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Existing candidates for treating non-alcoholic steatohepatitis (NASH), including glucagon-like peptide-1 (GLP-1) analogs and previous GLP-1/glucagon receptor (GLP-1R/GCGR) dual agonists, do not address the need for substantial weight loss adequately. We sought a more effective, evenly balanced GLP-1/GCGR dual agonist suitable for weekly administration. We studied a new class of covalent modifiers, glycolipid surfactants, to prolong the duration of action of candidate peptides. Variation of the hydrophobic tail of such surfactant modifications resulted in a wide and tunable range of physical properties and t1/2 values. We selected compound 17, which demonstrated high, evenly balanced potency for activation of human GLP-1R and GCGRs, return of diet induced obese (DIO) rodents to lean body/liver weight and prolonged duration correlated with high serum albumin binding. We observed a prolonged pharmacodynamic (PD) profile in rodents and pharmacokinetics (PK) in mini-pigs (t1/2 = 52 hours, mean residence time, MRT = 86 hours), suggesting suitability for weekly dosing. Accordingly, 17 (ALT-801) was selected for clinical development.
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Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) regulate glucose and energy homeostasis. Targeting both pathways with GIP receptor (GIPR) antagonist antibody (GIPR-Ab) and GLP-1 receptor (GLP-1R) agonist, by generating GIPR-Ab/GLP-1 bispecific molecules, is an approach for treating obesity and its comorbidities. In mice and monkeys, these molecules reduce body weight (BW) and improve many metabolic parameters. BW loss is greater with GIPR-Ab/GLP-1 than with GIPR-Ab or a control antibody conjugate, suggesting synergistic effects. GIPR-Ab/GLP-1 also reduces the respiratory exchange ratio in DIO mice. Simultaneous receptor binding and rapid receptor internalization by GIPR-Ab/GLP-1 amplify endosomal cAMP production in recombinant cells expressing both receptors. This may explain the efficacy of the bispecific molecules. Overall, our GIPR-Ab/GLP-1 molecules promote BW loss, and they may be used for treating obesity.
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