Target Information
| Target General Information | Top | |||||
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| Target ID |
T60182
(Former ID: TTDS00439)
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| Target Name |
Glucagon receptor (GCGR)
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| Synonyms |
GLR; GL-R
Click to Show/Hide
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| Gene Name |
GCGR
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Hypo-glycaemia [ICD-11: 5A41] | |||||
| Function |
Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system. G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis.
Click to Show/Hide
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| BioChemical Class |
GPCR secretin
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| UniProt ID | ||||||
| Sequence |
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNR
TFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQ CQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANL FASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYC WLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDN MGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGV HEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Dasiglucagon | Drug Info | Approved | Hypoglycemia | [2] | |
| 2 | Glucagon recombinant | Drug Info | Approved | Hypoglycemia | [3] | |
| Clinical Trial Drug(s) | [+] 16 Clinical Trial Drugs | + | ||||
| 1 | Retatrutide | Drug Info | Phase 3 | Obesity | [4] | |
| 2 | Efinopegdutide | Drug Info | Phase 2 | Non-alcoholic steatohepatitis | [5] | |
| 3 | LGD-6972 | Drug Info | Phase 2 | Type-2 diabetes | [6] | |
| 4 | LY-2409021 | Drug Info | Phase 2 | Type-2 diabetes | [7] | |
| 5 | LY2944876 | Drug Info | Phase 2 | Diabetic complication | [8] | |
| 6 | LY3437943 | Drug Info | Phase 2 | Obesity | [9] | |
| 7 | MK-8521 | Drug Info | Phase 2 | Type-2 diabetes | [6], [10] | |
| 8 | PF-06291874 | Drug Info | Phase 2 | Type-2 diabetes | [6], [11] | |
| 9 | REMD 477 | Drug Info | Phase 2 | Type-1 diabetes | [12] | |
| 10 | TT-401 | Drug Info | Phase 2 | Type-2 diabetes | [6], [13] | |
| 11 | DD01 | Drug Info | Phase 1 | Obesity | [14] | |
| 12 | LY3305677 | Drug Info | Phase 1 | Type 2 diabetes | [15] | |
| 13 | Pemvidutide | Drug Info | Phase 1 | Obesity | [16] | |
| 14 | REGN1193 | Drug Info | Phase 1 | Type-2 diabetes | [17] | |
| 15 | SAR425899 | Drug Info | Phase 1 | Diabetic complication | [18] | |
| 16 | ZP2929 | Drug Info | Phase 1 | Type-1 diabetes | [6] | |
| Discontinued Drug(s) | [+] 5 Discontinued Drugs | + | ||||
| 1 | BAY-27-9955 | Drug Info | Discontinued in Phase 1 | Type-2 diabetes | [19], [20] | |
| 2 | BAY-73-7977 | Drug Info | Discontinued in Phase 1 | Diabetic complication | [21] | |
| 3 | NN-2501 | Drug Info | Discontinued in Phase 1 | Type-2 diabetes | [22] | |
| 4 | DIO-901 | Drug Info | Terminated | Type-1 diabetes | [23] | |
| 5 | NNC-252504 | Drug Info | Terminated | Type-2 diabetes | [24] | |
| Mode of Action | [+] 7 Modes of Action | + | ||||
| Agonist | [+] 10 Agonist drugs | + | ||||
| 1 | Dasiglucagon | Drug Info | [2] | |||
| 2 | Retatrutide | Drug Info | [26] | |||
| 3 | Efinopegdutide | Drug Info | [27] | |||
| 4 | LY3437943 | Drug Info | [31] | |||
| 5 | TT-401 | Drug Info | [6] | |||
| 6 | DD01 | Drug Info | [34] | |||
| 7 | LY3305677 | Drug Info | [35] | |||
| 8 | Pemvidutide | Drug Info | [36] | |||
| 9 | DIO-901 | Drug Info | [44] | |||
| 10 | glucagon-(1-6) | Drug Info | [50] | |||
| Binder | [+] 2 Binder drugs | + | ||||
| 1 | Glucagon recombinant | Drug Info | [1], [25] | |||
| 2 | DwLIP-GCGRrx | Drug Info | [49] | |||
| Antagonist | [+] 45 Antagonist drugs | + | ||||
| 1 | LGD-6972 | Drug Info | [28] | |||
| 2 | LY-2409021 | Drug Info | [29] | |||
| 3 | PF-06291874 | Drug Info | [32] | |||
| 4 | REMD 477 | Drug Info | [33] | |||
| 5 | 3-substituted-2-furancarboxylic acid hydrazide derivative 1 | Drug Info | [40] | |||
| 6 | 3-substituted-2-furancarboxylic acid hydrazide derivative 5 | Drug Info | [40] | |||
| 7 | Aromatic ring compound 1 | Drug Info | [40] | |||
| 8 | Aromatic ring compound 2 | Drug Info | [40] | |||
| 9 | Aromatic ring compound 3 | Drug Info | [40] | |||
| 10 | Aromatic ring compound 4 | Drug Info | [40] | |||
| 11 | Biphenyl carboxamidopropanoic acid derivative 1 | Drug Info | [40] | |||
| 12 | Biphenyl carboxamidopropanoic acid derivative 2 | Drug Info | [40] | |||
| 13 | Biphenyl carboxamidopropanoic acid derivative 3 | Drug Info | [40] | |||
| 14 | Biphenyl carboxamidopropanoic acid derivative 4 | Drug Info | [40] | |||
| 15 | Heterocycle-containing compound 1 | Drug Info | [40] | |||
| 16 | Heterocycle-containing compound 2 | Drug Info | [40] | |||
| 17 | Heterocycle-containing compound 3 | Drug Info | [40] | |||
| 18 | Heterocycle-containing compound 4 | Drug Info | [40] | |||
| 19 | Heterocycle-containing compound 5 | Drug Info | [40] | |||
| 20 | Picolinamido propanoic acid derivative 1 | Drug Info | [40] | |||
| 21 | Picolinamido propanoic acid derivative 2 | Drug Info | [40] | |||
| 22 | Picolinamido propanoic acid derivative 3 | Drug Info | [40] | |||
| 23 | PMID25828189-Compound-19 | Drug Info | [40] | |||
| 24 | PMID25828189-Compound-21 | Drug Info | [40] | |||
| 25 | PMID25828189-Compound-22 | Drug Info | [40] | |||
| 26 | Pyrrolidine derivative 6 | Drug Info | [40] | |||
| 27 | Pyrrolidine derivative 7 | Drug Info | [40] | |||
| 28 | Pyrrolidine derivative 8 | Drug Info | [40] | |||
| 29 | Quinolinyl compound 1 | Drug Info | [40] | |||
| 30 | Quinolinyl compound 2 | Drug Info | [40] | |||
| 31 | Spiroimidazolone derivative 1 | Drug Info | [40] | |||
| 32 | Spiroimidazolone derivative 2 | Drug Info | [40] | |||
| 33 | Spiroimidazolone derivative 3 | Drug Info | [40] | |||
| 34 | Spiroimidazolone derivative 4 | Drug Info | [40] | |||
| 35 | Spiroimidazolone derivative 5 | Drug Info | [40] | |||
| 36 | Spiroimidazolone derivative 6 | Drug Info | [40] | |||
| 37 | Spiroimidazolone derivative 7 | Drug Info | [40] | |||
| 38 | BAY-27-9955 | Drug Info | [41] | |||
| 39 | BAY-73-7977 | Drug Info | [42] | |||
| 40 | NN-2501 | Drug Info | [43] | |||
| 41 | NNC-252504 | Drug Info | [45] | |||
| 42 | DSR-17759 | Drug Info | [48] | |||
| 43 | hGCGR antagonist | Drug Info | [51] | |||
| 44 | L-168049 | Drug Info | [48] | |||
| 45 | NNC 92-1687 | Drug Info | [52] | |||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | LY2944876 | Drug Info | [30] | |||
| 2 | SAR425899 | Drug Info | [38] | |||
| 3 | ZP2929 | Drug Info | [39] | |||
| 4 | MAR-531 | Drug Info | [48] | |||
| Co-agonist | [+] 1 Co-agonist drugs | + | ||||
| 1 | MK-8521 | Drug Info | [6] | |||
| Blocker | [+] 1 Blocker drugs | + | ||||
| 1 | REGN1193 | Drug Info | [37] | |||
| Inhibitor | [+] 6 Inhibitor drugs | + | ||||
| 1 | BI-32169 | Drug Info | [46] | |||
| 2 | Des-His1[Glu9]glucagon-NH2 | Drug Info | [47] | |||
| 3 | [des-His1,Tyr5,Glu9,D-Ala10]glucagon-NH2 | Drug Info | [53] | |||
| 4 | [des-His1,Tyr5,Glu9,D-Phe10]glucagon-NH2 | Drug Info | [53] | |||
| 5 | [des-His1,Tyr5,Glu9,D-Tyr10]glucagon-NH2 | Drug Info | [53] | |||
| 6 | [des-His1,Tyr5,Glu9]glucagon-NH2 | Drug Info | [53] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Oleic acid | Ligand Info | |||||
| Structure Description | Crystal structure of the human glucagon receptor (GCGR) in complex with the antagonist MK-0893 | PDB:5EE7 | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | Yes | [54] |
| PDB Sequence |
YSSFQVMYTV
147 GYSLSLAALL157 LALAILGGLS167 KLHCTANAIH177 ANLFLSFVLK187 ASAVLFIDGL 197 LRTVSTWLSD218 GAVAACRVAA228 VFMQYGIVAN238 YCWLLVEGLY248 LHNLLGLNIF 1002 EMLRIDEGLR1012 LKIYKDYYTI1025 GIGHLLTKSP1035 SLNAAKSELD1045 KAIGRNTNGV 1055 ITKDEAEKLF1065 NQDVDAAVRG1075 ILRNAKLKPV1085 YDSLDAVRRA1095 ALINMVFQMG 1105 ETGVAGFTNS1115 LRMLQQKRWD1125 EAAVNLAKSR1135 WYNQTPNRAK1145 RVITTFRTGT 1155 WDAYPERSFF264 SLYLGIGWGA274 PALFVVPWAV284 VKCLFENVQC294 WTNMGFWWIL 307 RFPVFLAILI317 NFFIFVRIVQ327 LLVAKLRARQ337 MHHTDYAFRL347 AKSTLTLIPL 357 LGVHFVVFAF367 VTDEHRSAKL382 FFDLALSSFQ392 GLLVAVLYCF402 LNKEVQSELR 412 RRWHRA
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SER139
4.683
GLN142
3.941
VAL143
3.856
THR146
3.642
VAL147
3.849
SER150
3.289
LEU151
4.376
LEU153
3.841
LEU157
3.951
LEU160
3.804
ALA161
4.475
HIS170
4.607
CYS171
3.604
THR172
3.092
ALA175
3.799
ASN179
3.315
LEU182
3.805
VAL185
3.857
LEU186
4.804
SER189
3.224
LEU192
3.849
PHE193
3.845
LEU197
3.903
ARG199
4.469
THR200
4.794
SER217
4.093
ASP218
3.661
GLY219
4.312
ALA220
3.867
VAL221
3.750
ALA222
3.783
ALA223
4.092
ARG225
3.590
VAL226
3.838
VAL229
3.907
TYR233
4.020
HIS250
2.723
PHE264
3.596
SER265
4.093
LEU268
3.254
GLY269
4.203
TRP272
3.730
GLY273
4.105
ALA276
4.696
VAL280
3.763
ALA283
4.082
TRP295
3.946
LEU313
3.845
LEU316
4.225
ILE317
3.614
PHE320
3.803
ILE321
4.668
PHE322
3.993
ARG324
2.870
VAL326
3.928
LEU328
4.337
LEU329
4.322
VAL330
4.677
LEU333
4.562
PHE345
3.570
LEU352
3.501
THR353
4.575
PRO356
4.190
LEU357
4.123
HIS361
2.570
ALA380
3.576
LYS381
3.714
PHE384
4.050
ASP385
3.138
LEU388
3.139
SER389
4.197
PHE391
3.457
GLN392
3.973
LEU394
3.744
LEU395
4.170
VAL398
4.364
ASP1157
4.441
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| Ligand Name: Alpha-Aminoisobutyric Acid | Ligand Info | |||||
| Structure Description | Cryo-EM structure of the GIPR/GLP-1R/GCGR triagonist peptide 20-bound human GCGR-Gs complex | PDB:7V35 | ||||
| Method | Electron microscopy | Resolution | 3.50 Å | Mutation | Yes | [55] |
| PDB Sequence |
QVMDFLFEKW
36 KLYGDQCHHN46 LSLLPPPTEL56 VCNRTFDKYS66 CWPDTPANTT76 ANISCPWYLP 86 WHHKVQHRFV96 FKRCGQWVRG109 PRGQPWRDAS119 QCQMDGEEIE129 VQKEVAKMYS 139 SFQVMYTVGY149 SLSLGALLLA159 LAILGGLSKL169 HCTRNAIHAN179 LFASFVLKAS 189 SVLVIDGLLR199 TRYSQKIGDD209 LSVSTWLSDG219 AVAGCRVAAV229 FMQYGIVANY 239 CWLLVEGLYL249 HNLLGLATLP259 ERSFFSLYLG269 IGWGAPMLFV279 VPWAVVKCLF 289 ENVQCWTSND299 NMGFWWILRF309 PVFLAILINF319 FIFVRIVQLL329 VAKLRARQMH 339 HTDYKFRLAK349 STLTLIPLLG359 VHEVVFAFVT369 DEHAQGTLRS379 AKLFFDLFLS 389 SFQGLLVAVL399 YCFLNKEVQS409 ELRRRWHRWR419 LG
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Glucagon signaling pathway | hsa04922 | Affiliated Target |
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| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Degree | 3 | Degree centrality | 3.22E-04 | Betweenness centrality | 2.23E-05 |
|---|---|---|---|---|---|
| Closeness centrality | 1.83E-01 | Radiality | 1.31E+01 | Clustering coefficient | 3.33E-01 |
| Neighborhood connectivity | 1.80E+01 | Topological coefficient | 3.61E-01 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| 2 | Glucagon signaling pathway | |||||
| Reactome | [+] 4 Reactome Pathways | + | ||||
| 1 | Glucagon signaling in metabolic regulation | |||||
| 2 | G alpha (q) signalling events | |||||
| 3 | G alpha (s) signalling events | |||||
| 4 | Glucagon-type ligand receptors | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | GPCRs, Class B Secretin-like | |||||
| 2 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 3 | Integration of energy metabolism | |||||
| 4 | GPCR ligand binding | |||||
| 5 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Glucagon receptor expression and glucagon stimulation of ghrelin secretion in rat stomach. Biochem Biophys Res Commun. 2007 Jun 15;357(4):865-70. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021 | |||||
| REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 4 | ClinicalTrials.gov (NCT05882045) A Randomized, Double-Blind, Phase 3 Study to Investigate the Efficacy and Safety of LY3437943 Once Weekly Compared to Placebo in Participants With Severe Obesity and Established Cardiovascular Disease. U.S.National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT04944992) A Phase 2a, Randomized, Active-Comparator-Controlled, Open-Label Study to Evaluate the Efficacy and Safety of Efinopegdutide (MK-6024) in Individuals With Nonalcoholic Fatty Liver Disease. U.S.National Institutes of Health. | |||||
| REF 6 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 7 | ClinicalTrials.gov (NCT02091362) A Study of LY2409021 on Blood Pressure and Pulse Rate in Participants With Type 2 Diabetes Mellitus. U.S. National Institutes of Health. | |||||
| REF 8 | ClinicalTrials.gov (NCT02119819) A Study to Compare a New Drug for Type 2 Diabetes to Placebo and to a Treatment Already Available for Type 2 Diabetes. U.S. National Institutes of Health. | |||||
| REF 9 | ClinicalTrials.gov (NCT04881760) A Phase 2 Study of Once-Weekly LY3437943 Compared With Placebo in Participants Who Have Obesity or Are Overweight With Weight-Related Comorbidities. U.S.National Institutes of Health. | |||||
| REF 10 | ClinicalTrials.gov (NCT02492763) A Preliminary Study of the Efficacy and Safety of MK-8521 for Type 2 Diabetes (MK-8521-004). | |||||
| REF 11 | ClinicalTrials.gov (NCT02175121) Safety, Tolerability, Pharmacokinetics And Pharmacodynamics Study Of PF-06291874 As Oral Monotherapy To Treat Adults With Type 2 Diabetes Mellitus. U.S. National Institutes of Health. | |||||
| REF 12 | ClinicalTrials.gov (NCT03117998) Multiple Dose Study to Evaluate the Efficacy, Safety and Pharmacodynamics of REMD-477 in Subjects With Type 1 Diabetes Mellitus. U.S. National Institutes of Health. | |||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035378) | |||||
| REF 14 | ClinicalTrials.gov (NCT04812262) A Phase 1, Randomized, Double-blind, Placebo-controlled, Single and Multiple Dose Study to Assess Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of DD01 in Overweight/Obese Subjects With T2DM and NAFLD. U.S.National Institutes of Health. | |||||
| REF 15 | ClinicalTrials.gov (NCT03928379) A Multiple-Ascending Dose Study in Patients With Type 2 Diabetes Mellitus to Investigate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of LY3305677. U.S.National Institutes of Health. | |||||
| REF 16 | ClinicalTrials.gov (NCT05292911) A 12-Week Extension Study of ALT-801 in Diabetic and Non-Diabetic Overweight and Obese Subjects With Non-alcoholic Fatty Liver Disease (NAFLD). U.S.National Institutes of Health. | |||||
| REF 17 | ClinicalTrials.gov (NCT02284425) Study of REGN1193 in Patients With Type 2 Diabetes Mellitus. U.S. National Institutes of Health. | |||||
| REF 18 | ClinicalTrials.gov (NCT02411825) Multiple Ascending Dose Study in Healthy Male Subjects. U.S. National Institutes of Health. | |||||
| REF 19 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3491). | |||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013061) | |||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024072) | |||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018428) | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022421) | |||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014586) | |||||
| REF 25 | Fully human monoclonal antibodies antagonizing the glucagon receptor improve glucose homeostasis in mice and monkeys. J Pharmacol Exp Ther. 2009 Apr;329(1):102-11. | |||||
| REF 26 | Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in the treatment of diabetes and obesity? Expert Opin Investig Drugs. 2023 May;32(5):355-359. | |||||
| REF 27 | Emerging glucagon-like peptide 1 receptor agonists for the treatment of obesity. Expert Opin Emerg Drugs. 2021 Sep;26(3):231-243. | |||||
| REF 28 | Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31. | |||||
| REF 29 | Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes. Diabetes Obes Metab. 2015 Apr;17(4):414-22. | |||||
| REF 30 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 31 | LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9. | |||||
| REF 32 | Clinical pipeline report, company report or official report of pfizer. | |||||
| REF 33 | Effect of a glucagon receptor antibody (REMD-477) in type 1 diabetes: A randomized controlled trial. Diabetes Obes Metab. 2018 May;20(5):1302-1305. | |||||
| REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight | |||||
| REF 35 | IBI362?(LY3305677), a weekly-dose GLP-1 and glucagon receptor dual agonist, in Chinese adults with overweight or obesity: A randomised, placebo-controlled, multiple ascending dose phase 1b study. EClinicalMedicine. 2021 Aug 13;39:101088. | |||||
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