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CRF Research Publications
 2008
2007
2006
2005
2004
2003
2008
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Regan CF, Guo Z, Chen Y, Huang CQ, Chen M, Jiang W, Rueter JK, Coon T, Chen C, Saunders J, Brown MS, Betz SF, Struthers RS, Yang C, Wen J, Madan A, Zhu YF. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4503-7. Epub 2008 Jul 17.
See also Bioorganic & Medicinal Chemistry Letters
Non-peptide gonadotropin-releasing hormone receptor antagonists.
Betz SF, Zhu YF, Chen C, Struthers RS. J Med Chem. 2008 Jun 26;51(12):3331-48. Review. No abstract available.
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Chen C, Chen Y, Pontillo J, Guo Z, Huang CQ, Wu D, Madan A, Chen T, Wen J, Xie Q, Tucci FC, Rowbottom M, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3301-5. Epub 2008 Apr 26.
See also Bioorganic & Medicinal Chemistry Letters
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
Zhao L, Guo Z, Chen Y, Hu T, Wu D, Zhu YF, Rowbottom M, Gross TD, Tucci FC, Struthers RS, Xie Q, Chen C. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3344-9. Epub 2008 Apr 15.
See also Bioorganic & Medicinal Chemistry Letters
Small molecule antagonists of the corticotropin releasing factor (CRF) receptor: recent medicinal chemistry developments.
Tellew JE, Luo Z. Curr Top Med Chem. 2008;8(6):506-20. Review.
Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation
Hoare SR, Fleck BA, Gross RS, Crowe PD, Williams JP, Grigoriadis DE. Mol Pharmacol. 2008 Jan 31; [Epub ahead of print]
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2007
Emerging Anxiolytics: Corticoptropin-Releasing Factor Receptor Antagonists
Grigoriadis D., Hoare RJ. Handbook of Contemporary Neuropharmacology, (2007) 2: 177-213
Cortricotropin-Releasing Factor Receptors
Grigoriadis DE. Encyclopedia of Stress, 2nd Edition (2007), 1: 641-48
High-Affinity CRF(1) Receptor Antagonist NBI-34041: Preclinical and Clinical Data Suggest Safety and Efficacy in Attenuating Elevated Stress Response
Ising M, Zimmermann US, et al. Neuropsychopharmacology 32(9):1941-9
NMR structural characterization of a minimal peptide antagonist bound to the extracellular domain of the corticotrophin-releasing factor 1 receptor
Mesleh MF, Shirely WA, Heise CE, Ling N, et al. J Biol Chem 282(9): 6338-46
Corticotropin-releasing factor receptor-1-deficient mice show decreased anxiety and colonic sensitivity
Trimble N, Johnson AC, Foster AC, et al. Neurogastroenterology and Motility 19:754-760
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2006
Recent advances in small molecule antagonists of the corticotrophin-releasing factor type-1 receptor-focus on pharmacology and pharmacokinetics
Chen C. Curr Med Chem 13(11):126-82
Single amino acid residue determinants of non-peptide antagonist binding to the corticotrophin-releasing factor(1) (CRF(1)) receptor
Hoare SR, Brown BT, et al. Biochem Pharmacol 72:244-255
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2005
Corticotropin-releasing factor: effect on cerebral blood flow in physiologic and ischaemic conditions.
De Michele M, Touzani O, Foster AC, Fieschi C, Sette G, McCulloch J. Exp Brain Res 2005, 165:375-382
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.
Dyck B, Grigoriadis DE, Gross RS, Guo Z, Haddach M, Marinkovic D, McCarthy JR, Moorjani M, Regan CF, Saunders J, et al. J Med Chem 2005, 48:4100-4110
The corticotropin-releasing factor receptor: a novel target for the treatment of depression and anxiety-related disorders.
Grigoriadis DE. Expert Opin Ther Targets 2005, 9:651-684
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, et al. J Med Chem 2005, 48:5780-5793
Design and Synthesis of Tricyclic Imidazo[4,5-b]pyridin-2-ones as Corticotropin-Releasing Factor-1 Antagonists.
Guo Z, Tellew JE, Gross RS, Dyck B, Grey J, Haddach M, Kiankarimi M, Lanier M, Li BF, Luo Z, et al. J Med Chem 2005, 48:5104-5107
Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupling sensitivity and determinants of CRF(2) receptor selectivity.
Hoare SR, Sullivan SK, Fan J, Khongsaly K, Grigoriadis DE. Peptides 2005, 26:457-470
The CRF(1) receptor antagonist, NBI-35965, abolished the activation of locus coeruleus neurons induced by colorectal distension and intracisternal CRF in rats.
Kosoyan HP, Grigoriadis DE, Tache Y. Brain Res 2005, 1056:85-96
Chronic cocaine administration switches corticotropin-releasing factor2 receptor-mediated depression to facilitation of glutamatergic transmission in the lateral septum.
Liu J, Yu B, Orozco-Cabal L, Grigoriadis DE, Rivier J, Vale WW, Shinnick-Gallagher P, Gallagher JP. J Neurosci 2005, 25:577-583
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.
Lowe RF, Nelson J, Dang TN, Crowe PD, Pahuja A, McCarthy JR, Grigoriadis DE, Conlon P, Saunders J, Chen C, et al. J Med Chem 2005, 48:1540-1549
Distinct Conformations of the Corticotropin Releasing Factor Type 1 Receptor Adopted following Agonist and Antagonist Binding Are Differentially Regulated.
Perry SJ, Junger S, Kohout TA, Hoare SR, Struthers RS, Grigoriadis DE, Maki RA. J Biol Chem 2005, 280:11560-11568
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2004
CRF receptor type 1 and 2 expression and anatomical distribution in the rat colon.
Chatzaki E, Crowe PD, Wang L, Million M, Tache Y, Grigoriadis DE: J Neurochem 2004, 90:309-316
Differential profile of CRF receptor distribution in the rat stomach and duodenum assessed by newly developed CRF receptor antibodies.
Chatzaki E, Murphy BJ, Wang L, Million M, Ohning GV, Crowe PD, Petroski R, Tache Y, Grigoriadis DE. J Neurochem 2004, 88:1-11
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.
Chen C, Wilcoxen KM, Huang CQ, McCarthy JR, Chen T, Grigoriadis DE. Bioorg Med Chem Lett 2004, 14:3669-3673
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1 ,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.
Chen C, Wilcoxen KM, Huang CQ, Xie YF, McCarthy JR, Webb TR, Zhu YF, Saunders J, Liu XJ, Chen TK, et al. J Med Chem 2004, 47:4787-4798
Modulation of dendritic differentiation by corticotropin-releasing factor in the developing hippocampus.
Chen Y, Bender RA, Brunson KL, Pomper JK, Grigoriadis DE, Wurst W, Baram TZ. Proc Natl Acad Sci U S A 2004, 101:15782-15787
Synthesis of pyrrolopyrimidine CRF-R1 antagonists containing a tricyclic core via an intramolecular heck reaction.
Dyck B, McCarthy JR. Heterocycles 2004, 62:191-195
Ligand affinity for amino-terminal and juxtamembrane domains of the corticotropin releasing factor type I receptor: Regulation by G-protein and nonpeptide antagonists.
Hoare SR, Sullivan SK, Schwarz DA, Ling N, Vale WW, Crowe PD, Grigoriadis DE. Biochemistry 2004, 43:3996-4011
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.
Huang CQ, Grigoriadis DE, Liu Z, McCarthy JR, Ramphal J, Webb T, Whitten JP, Xie MY, Chen C. Bioorg Med Chem Lett 2004, 14:2083-2086
Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.
Huang CQ, Wilcoxen KM, Grigoriadis DE, McCarthy JR, Chen C. Bioorg Med Chem Lett 2004, 14:3943-3947
Corticotropin-releasing factor and Urocortin I modulate excitatory glutamatergic synaptic transmission.
Liu J, Yu B, Neugebauer V, Grigoriadis DE, Rivier J, Vale WW, Shinnick-Gallagher P, Gallagher JP. J Neurosci 2004, 24:4020-4029
Central CRF, urocortins and stress increase colonic transit via CRF1 receptors while activation of CRF2 receptors delays gastric transit in mice.
Martinez V, Wang L, Rivier J, Grigoriadis D, Tache Y. J Physiol 2004, 556:221-234
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.
Webb TR, Moran T, Huang CQ, McCarthy JR, Grigoriadis DE, Chen C. Bioorg Med Chem Lett 2004, 14:3869-3873
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2003
Corticotropin releasing hormone type 2 receptors in the dorsal raphe nucleus mediate the behavioral consequences of uncontrollable stress.
Hammack SE, Schmid MJ, LoPresti ML, Der-Avakian A, Pellymounter MA, Foster AC, Watkins LR, Maier SF. J Neurosci 2003, 23:1019-1025
Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists.
Hoare SR, Sullivan SK, Ling N, Crowe PD, Grigoriadis DE. Mol Pharmacol 2003, 63:751-765
Conformational states of the corticotropin releasing factor 1 (CRF1) receptor: detection, and pharmacological evaluation by peptide ligands.
Hoare SR, Sullivan SK, Pahuja A, Ling N, Crowe P, Grigoriadis D. Peptides 2003 24(12):1881-1897
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.
Huang CQ, Waisman A, Wilcoxen K, McCarthy JR, Haddach M, Webb TR, Gu J, Xie YF, Grigoriadis DE, Chen C. Bioorg Med Chem Lett 2003, 13:3375-3379
Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists.
Huang CQ, Wilcoxen K, McCarthy JR, Haddach M, Grigoriadis D, Chen C. In Bioorg Med Chem Lett. Edited by; 2003:3371-3374. vol 13.]
Effects of a selective agonist and antagonist of CRF(2) receptors on cardiovascular function in the rat.
Mackay KB, Stiefel TH, Ling N, Foster AC. In Eur J Pharmacol. Edited by; 2003:111-115. vol 469.]
Antagonists of the corticotropin releasing factor receptor.
Saunders J, Williams J. Prog Med Chem 2003, 41:195-247
Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists.
Wilcoxen K, Huang CQ, McCarthy JR, Grigoriadis DE, Chen C. Bioorg Med Chem Lett 2003, 13:3367-3370
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