Target Validation Information
Target ID T99816
Target Name Gastrin-releasing peptide receptor
Target Type
Clinical Trial
Drug Potency against Target [Tyr4]Bombesin Drug Info IC50 = 0.85 nM [527364]
JMV 1801 Drug Info Ki = 2 nM [525815]
(D)Phe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH2 Drug Info Ki = 6.3 nM [525815]
JMV 1693 Drug Info Ki = 53 nM [525815]
JMV 1799 Drug Info Ki = 1.2 nM [525815]
JMV 1802 Drug Info Ki = 0.8 nM [525815]
JMV 1719 Drug Info Ki = 11 nM [525815]
[(N4-Bzdig)0,Nle14]BB(7-14) Drug Info IC50 = 0.6 nM [527364]
(CH3)CCO-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2 Drug Info IC50 = 4.1 nM [531063]
JMV 1813 Drug Info Ki = 2 nM [525815]
JMV 1535 Drug Info Ki = 1 nM [525815]
Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2 Drug Info IC50 = 1.8 nM [531063]
Ac-His-Trp-Ala-Val-D-Ala-His-Leu-Met-NH2 Drug Info IC50 = 3.2 nM [531063]
JMV 1803 Drug Info Ki = 2 nM [525815]
[N40,Pro1,Tyr4,Nle 14]BB Drug Info IC50 = 0.15 nM [527364]
Ac-His-Trp-Ala-Val-Ala-His-Leu-Met-NH2 Drug Info IC50 = 180 nM [531063]
Action against Disease Model RC-3095 RC-3095 at 1 nM concentration effectively inhibited the bombesin-stimulated growth of CFPAC-1 cells in cultures. In the presence of 1 microM RC-3095 in the culture medi uM, the bombesin-induced growth of CFPAC-1 cells was totally suppressed. [527581] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Pharmacologic/receptor-knockout studies show involvement of these receptors in a n uMber of new processes/diseases. Neuromedin B/BB1-receptor is an important physiological regulator of pituitary-thyroid function; in mediating behavior, especially feas/anxiety; in mediating satiety through different cascades than gastrin-releasing peptide/BB2 receptors and for its autocrine tuMor-growth effects. Gastrin-releasing peptide/BB2-receptor plays important roles in mediating signals for pruritus, lung development/injury, small intestinal mucosal defense, and central nervous system processes such as learning/memory. The signaling mechanisms of its potent growth effects are being elucidated and their possible therapeutic targets identified. BB3-receptor knockout mice providedinsights for their obesity/glucose intolerance and demonstrated that this receptor may be important in the lung response to injury, t uMor growth and gastrointestinal motility. Each receptor is frequently overexpressed in h uMan t uMors and has potent growth effects. This effect is being explored to develop new antit uMor treatments, such as bombesin-receptor ligands conjugated to cytotoxic agents. [527364]
References
Ref 527364J Med Chem. 2005 Jan 13;48(1):100-10.Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 527364J Med Chem. 2005 Jan 13;48(1):100-10.Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.
Ref 531063J Med Chem. 1991 Jul;34(7):2102-7.Gastrin releasing peptide antagonists with improved potency and stability.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 531063J Med Chem. 1991 Jul;34(7):2102-7.Gastrin releasing peptide antagonists with improved potency and stability.
Ref 527581Oncogene. 2005 Aug 4;24(33):5262-8.Lipid modification of GRN163, an N3'-->P5' thio-phosphoramidate oligonucleotide, enhances the potency of telomerase inhibition.
Ref 531063J Med Chem. 1991 Jul;34(7):2102-7.Gastrin releasing peptide antagonists with improved potency and stability.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
Ref 527364J Med Chem. 2005 Jan 13;48(1):100-10.Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.
Ref 531063J Med Chem. 1991 Jul;34(7):2102-7.Gastrin releasing peptide antagonists with improved potency and stability.

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