Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTVFO0U)

• DTT Name: Gastrin/cholecystokinin type B receptor (CCKBR)
• Synonyms: Cholecystokinin-2 receptor; CCKRB; CCK2-R; CCK-BR; CCK-B receptor
• Gene Name: CCKBR
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: GASR_HUMAN
• TTD ID: T05849
• Sequence:
  MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
  YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
  IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
  LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
  ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
  RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
  PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
  PDEDPPTPSIASLSRLSYTTISTLGPG
• Function: The CCK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Receptor for gastrin and cholecystokinin.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Gastric acid secretion (hsa04971)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  Gastrin-CREB signalling pathway via PKC and MAPK (R-HSA-881907)
  Peptide ligand-binding receptors (R-HSA-375276)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ceruletide	DM2WE5K	Caerulein stimulated gastric and pancreatic secretion	5A4Y	Approved	[2]
Pentagastrin	DMRCLZB	Diagnostic imaging	N.A.	Approved	[1]

9 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GASTRAZOLE	DMO3ITF	Duodenal ulcer	DA63	Phase 3	[3]
Dexloxiglumide	DM52HUD	Pancreatic malfunction	DC30-DC3Z	Phase 2	[4]
Itriglumide	DM5UFRO	Anxiety disorder	6B00-6B0Z	Phase 2	[5]
S-0509	DM4KWEF	Ulcerative colitis	DD71	Phase 2	[6]
Spiroglumide	DM7NJWY	Stomach disease	DA43-DA4Y	Phase 2	[7]
TT-223	DMCDMFP	Type-1 diabetes	5A10	Phase 2	[8]
YF-476	DM54MAJ	Stomach ulcer	DA60.Z	Phase 2	[9]
Z 360	DM2M80G	Discovery agent	N.A.	Phase 2	[10]
Demogastrin	DMTULGS	Thyroid cancer	2D10	Phase 1	[11]

13 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GV-150013	DMZD023	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 2	[12]
L-365260	DMT13ZR	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 2	[13]
PD-134308	DM80UNM	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 2	[14]
CR-2093	DMWVBGD	Intestine cancer	2C0Z	Discontinued in Phase 1	[15]
AG-041R	DM625LN	Ulcerative colitis	DD71	Terminated	[18]
FR-208419	DMLG426	Dyspepsia	MD92	Terminated	[19]
GR-199114X	DMA7FX1	Stomach ulcer	DA60.Z	Terminated	[20]
IQM-95333	DMYCPFU	N. A.	N. A.	Terminated	[4]
LY288513	DMG8YE9	Anxiety disorder	6B00-6B0Z	Terminated	[21]
PD-135666	DMLEVNC	N. A.	N. A.	Terminated	[22]
PD136450	DMD6L82	N. A.	N. A.	Terminated	[23]
SNF-9007	DM4CNM9	N. A.	N. A.	Terminated	[24]
YM-022	DM97ULM	Gastrointestinal disease	DE2Z	Terminated	[25]

3 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GG-8573	DMFQI38	Obesity	5B81	Preclinical	[16]
JNJ-26070109	DMSXOPE	Gastroesophageal reflux disease	DA22.Z	Preclinical	[17]
PD-170292	DMEOVDQ	Obesity	5B81	Preclinical	[16]

58 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[26]
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe	DMKAHYQ	Discovery agent	N.A.	Investigative	[27]
BC-264	DMQWOZ5	Discovery agent	N.A.	Investigative	[28]
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2	DMPJR98	Discovery agent	N.A.	Investigative	[29]
CCK-33	DM1N0ED	Discovery agent	N.A.	Investigative	[30]
CCK-8	DMN0J4W	N. A.	N. A.	Investigative	[30]
Cholecystokinin-9	DMVJMG8	Discovery agent	N.A.	Investigative	[31]
CI-1015	DMQ5CE1	Discovery agent	N.A.	Investigative	[32]
desulfated cholecystokinin-8	DMW740T	Discovery agent	N.A.	Investigative	[33]
GW-5823	DMCOYF9	Discovery agent	N.A.	Investigative	[34]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo	DMW50ZQ	Discovery agent	N.A.	Investigative	[35]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H	DMF82C1	Discovery agent	N.A.	Investigative	[35]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H	DMSXD63	Discovery agent	N.A.	Investigative	[36]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac	DMRUD37	Discovery agent	N.A.	Investigative	[36]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc	DMIPXCZ	Discovery agent	N.A.	Investigative	[36]
PBC-264	DM39LS5	Discovery agent	N.A.	Investigative	[37]
PD-135118	DMUTEWI	Discovery agent	N.A.	Investigative	[22]
PD-135158	DMA7YJV	Discovery agent	N.A.	Investigative	[38]
PD-136621	DM8N3RB	Discovery agent	N.A.	Investigative	[22]
PD-137337	DMJWK0T	Discovery agent	N.A.	Investigative	[22]
PD-137342	DMH2OV9	Discovery agent	N.A.	Investigative	[22]
PD-138915	DMLVRU7	Discovery agent	N.A.	Investigative	[22]
PD-138916	DMIAFN5	Discovery agent	N.A.	Investigative	[22]
PD-138917	DMUG2L9	Discovery agent	N.A.	Investigative	[22]
PD-140547	DMF86P3	Discovery agent	N.A.	Investigative	[22]
PD-140548	DMNO2EP	Discovery agent	N.A.	Investigative	[22]
PD-140723	DMWTOJN	Discovery agent	N.A.	Investigative	[22]
PD-149164	DMP65EI	Discovery agent	N.A.	Investigative	[39]
RB-400	DMJDE6Y	Discovery agent	N.A.	Investigative	[28]
RP-69758	DMXMRVG	Discovery agent	N.A.	Investigative	[40]
RP-71483	DMUFLNT	Discovery agent	N.A.	Investigative	[40]
RP-72540	DMWIXQS	Discovery agent	N.A.	Investigative	[40]
RP73870	DMLKPZ6	Discovery agent	N.A.	Investigative	[41]
RPR-107836	DM9ODEZ	Anxiety disorder	6B00-6B0Z	Investigative	[42]
Tetragastrin	DMDWUCX	Discovery agent	N.A.	Investigative	[43]
tetronothiodin	DM8T7CG	Discovery agent	N.A.	Investigative	[44]
TP-680	DMM41O9	Discovery agent	N.A.	Investigative	[45]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2	DM0D1Z5	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2	DMPH1G0	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc	DMB2TCF	Discovery agent	N.A.	Investigative	[36]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2	DMUXMVQ	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2	DMREJ69	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2	DMY9NIJ	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2	DMQREP2	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2	DMZ24LN	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2	DMPSJ72	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2	DMIWMN6	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2	DM2CEWT	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2	DMKM81A	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2	DMZOTGM	Discovery agent	N.A.	Investigative	[24]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2	DMM9H07	Discovery agent	N.A.	Investigative	[24]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2	DMN7290	Discovery agent	N.A.	Investigative	[24]
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2	DM8THU2	Discovery agent	N.A.	Investigative	[24]
[125I]-BDZ2	DMYBQOG	Discovery agent	N.A.	Investigative	[46]
[125I]PD142308	DMEHK9M	Discovery agent	N.A.	Investigative	[42]
[3H]JB-93182	DMJCI2A	Discovery agent	N.A.	Investigative	[47]
[3H]PBC-264	DMK46C7	Discovery agent	N.A.	Investigative	[48]
[3H]PD140376	DMWAT5S	Discovery agent	N.A.	Investigative	[49]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Thyroid cancer	2C82	Thyroid	6.53E-01	1.00E-03	4.05E-03

References

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