A mixed glucocorticoid/mineralocorticoid selective modulator with dominant antagonism in the male rat brain.
Atucha et al. • 2015 • Endocrinology. 2015;156(11):4105-4114.
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Entries by jeremiah@devisedesigns.com
Identification of the clinical candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): a selective Glucocorticoid Receptor (GR) antagonist.
Hunt et al. • 2017 • J Med Chem. 2017;60(8):3405-3421.
1H-pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoidreceptor antagonists with high functional activity.
Clark et al. • 2008 • Bioorg Med Chem Lett. 2008;18(4):1312-7.
Assessment of safety, tolerability, pharmacokinetics, and pharmacological effect of orally administered CORT125134: an adaptive, double-blind, randomized, placebo-controlled phase 1 clinical study.
Hunt et al. • 2017 • Clin Pharmacol Drug Dev. 2017 Oct 2. doi: 10.1002/cpdd.389.
FKBP5 mRNA expression is a biomarker for GR antagonism.
Bali et al. • 2016 • J Clin Endocrinol Metab. 2016;101(11):4305-4312.
Selective Glucocorticoid Receptor Modulators (SGRMs) delay castrate-resistant prostate cancer growth.
Kach et al. • 2017 • Mol Cancer Ther. 2017;16(8):1680-1692.
Minireview: nuclear receptors and breast cancer.
Conzen SD • 2008 • Mol Endocrinol.2008;22(10):2215-28.
The biology of hormone refractory prostate cancer. Why does it develop?
Isaacs JT • 1999 • Urol Clin North Am. 1999;26(2):263-73.
Glucocorticoid receptor activation inhibits chemotherapy-induced cell death in high-grade serous ovarian carcinoma.
Stringer-Reasor et al. • 2015 • Gynecol Oncol. 2015;138(3):656-62.
Glucocorticoid receptor activity contributes to resistance to androgen-targeted therapy in prostate cancer.
Isikbay et al. • 2014 • Horm Cancer. 2014;5(2):72-89.