Search Results - "Hunt, Hazel"

The glucocorticoid receptor modulator relacorilant reverses the immunosuppressive effects of cortisol by Greenstein, Andrew E., Hunt, Hazel J.

“…Graphical abstract created with BioRender.com [Display omitted] •Both exogenous and endogenous glucocorticoids are immunosuppressive.•We studied the effects of…”
Get full text

Glucocorticoid receptor antagonism promotes apoptosis in solid tumor cells by Greenstein, Andrew E., Hunt, Hazel J.

“…BACKGROUNDResistance to antiproliferative chemotherapies remains a significant challenge in the care of patients with solid tumors. Glucocorticoids, including…”
Get full text

Effect of Miricorilant, a Selective Glucocorticoid Receptor Modulator, on Olanzapine-Associated Weight Gain in Healthy Subjects: A Proof-of-Concept Study by Hunt, Hazel J., Donaldson, Kirsteen, Strem, Mark, Tudor, Iulia Cristina, Sweet-Smith, Suzanne, Sidhu, Sharan

“…Antipsychotic medications, including olanzapine, are associated with substantial weight gain and metabolic disturbances. We sought to determine whether…”
Get full text

Peripheral glucocorticoid receptor antagonism by relacorilant with modest HPA axis disinhibition by Viho, Eva M G, Kroon, Jan, Feelders, Richard A, Houtman, René, van den Dungen, Elisabeth S R, Pereira, Alberto M, Hunt, Hazel J, Hofland, Leo J, Meijer, Onno C

“…Glucocorticoid stress hormones are produced in response to hypothalamic–pituitary–adrenal (HPA) axis activation. Glucocorticoids are essential for physiology…”
Get full text

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 by Hunt, Hazel J, Belanoff, Joseph K, Walters, Iain, Gourdet, Benoit, Thomas, Jennifer, Barton, Naomi, Unitt, John, Phillips, Timothy, Swift, Denise, Eaton, Emily

“…The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing’s…”
Get full text

Glucocorticoid receptor antagonism decreases alcohol seeking in alcohol-dependent individuals by Vendruscolo, Leandro F, Estey, David, Goodell, Vivian, Macshane, Lauren G, Logrip, Marian L, Schlosburg, Joel E, McGinn, M Adrienne, Zamora-Martinez, Eva R, Belanoff, Joseph K, Hunt, Hazel J, Sanna, Pietro P, George, Olivier, Koob, George F, Edwards, Scott, Mason, Barbara J

“…Alcoholism, or alcohol use disorder, is a major public health concern that is a considerable risk factor for morbidity and disability; therefore, effective…”
Get full text

An In Vitro and In Vivo Evaluation of the Effect of Relacorilant on the Activity of Cytochrome P450 Drug Metabolizing Enzymes by Custodio, Joseph M., Donaldson, Kirsteen M., Hunt, Hazel J.

“…Relacorilant is a selective modulator of the glucocorticoid receptor in development for the treatment of several serious diseases. The widely used cocktail…”
Get full text

Glucocorticoid receptor modulators decrease alcohol self-administration in male rats by McGinn, M. Adrienne, Tunstall, Brendan J., Schlosburg, Joel E., Gregory-Flores, Adriana, George, Olivier, de Guglielmo, Giordano, Mason, Barbara J., Hunt, Hazel J., Koob, George F., Vendruscolo, Leandro F.

“…Alcohol use disorder (AUD) is associated with the dysregulation of brain stress and reward systems, including glucocorticoid receptors (GRs). The mixed…”
Get full text

Selection and early clinical evaluation of the brain‐penetrant 11β‐hydroxysteroid dehydrogenase type 1 (11β‐HSD1) inhibitor UE2343 (Xanamem™) by Webster, Scott P, McBride, Andrew, Binnie, Margaret, Sooy, Karen, Seckl, Jonathan R, Andrew, Ruth, Pallin, T David, Hunt, Hazel J, Perrior, Trevor R, Ruffles, Vincent S, Ketelbey, J William, Boyd, Alan, Walker, Brian R

“…Background and Purpose Reducing glucocorticoid exposure in the brain via intracellular inhibition of the cortisol‐regenerating enzyme 11β‐hydroxysteroid…”
Get full text

Insights into the Therapeutic Potential of Glucocorticoid Receptor Modulators for Neurodegenerative Diseases by De Nicola, Alejandro F, Meyer, Maria, Guennoun, Rachida, Schumacher, Michael, Hunt, Hazel, Belanoff, Joseph, de Kloet, E Ronald, Gonzalez Deniselle, Maria Claudia

“…Glucocorticoids are crucial for stress-coping, resilience, and adaptation. However, if the stress hormones become dysregulated, the vulnerability to…”
Get full text

Selective Glucocorticoid Receptor Antagonist CORT125281 Activates Brown Adipose Tissue and Alters Lipid Distribution in Male Mice by Kroon, Jan, Koorneef, Lisa L, van den Heuvel, Jose K, Verzijl, Cristy R C, van de Velde, Nienke M, Mol, Isabel M, Sips, Hetty C M, Hunt, Hazel, Rensen, Patrick C N, Meijer, Onno C

“…Abstract Glucocorticoids influence a wide range of metabolic processes in the human body, and excessive glucocorticoid exposure is known to contribute to the…”
Get full text

Differential targeting of brain stress circuits with a selective glucocorticoid receptor modulator by Zalachoras, Ioannis, Houtman, René, Atucha, Erika, Devos, Rene, Tijssen, Ans M. I., Hu, Pu, Lockey, Peter M., Datson, Nicole A., Belanoff, Joseph K., Lucassen, Paul J., Joëls, Marian, de Kloet, E. Ronald, Roozendaal, Benno, Hunt, Hazel, Meijer, Onno C.

“…Glucocorticoid receptor (GR) antagonism may be of considerable therapeutic value in stress-related psychopathology such as depression. However, blockade of all…”
Get full text

1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile by Hunt, Hazel J., Belanoff, Joseph K., Golding, Emily, Gourdet, Benoit, Phillips, Timothy, Swift, Denise, Thomas, Jennifer, Unitt, John F., Walters, Iain

“…[Display omitted] We report the further optimization of our series 1H-pyrazolo[3,4-g]hexahydro-isoquinoline sulfonamides as GR antagonists. By incorporating a…”
Get full text

Identification of an acute functional cross-talk between amyloid-β and glucocorticoid receptors at hippocampal excitatory synapses by Kootar, Scherazad, Frandemiche, Marie-Lise, Dhib, Gihen, Mouska, Xavier, Lorivel, Thomas, Poupon-Silvestre, Gwenola, Hunt, Hazel, Tronche, François, Bethus, Ingrid, Barik, Jacques, Marie, Hélène

“…Amyloid-β is a peptide released by synapses in physiological conditions and its pathological accumulation in brain structures necessary for memory processing…”
Get full text

Effects of selective and non-selective glucocorticoid receptor II antagonists on rapid-onset diabetes in young rats by Beaudry, Jacqueline L, Dunford, Emily C, Teich, Trevor, Zaharieva, Dessi, Hunt, Hazel, Belanoff, Joseph K, Riddell, Michael C

“…The blockade of glucocorticoid (GC) action through antagonism of the glucocorticoid receptor II (GRII) has been used to minimize the undesirable effects of…”
Get full text

An integrated framework for quantifying immune-tumour interactions in a 3D co-culture model by Al-Hity, Gheed, Yang, FengWei, Campillo-Funollet, Eduard, Greenstein, Andrew E., Hunt, Hazel, Mampay, Myrthe, Intabli, Haya, Falcinelli, Marta, Madzvamuse, Anotida, Venkataraman, Chandrasekhar, Flint, Melanie S.

“…Investigational in vitro models that reflect the complexity of the interaction between the immune system and tumours are limited and difficult to establish…”
Get full text

Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat by Hunt, Hazel J., Ray, Nicholas C., Hynd, George, Sutton, Jon, Sajad, Mohammed, O’Connor, Elizabeth, Ahmed, Shahadat, Lockey, Peter, Daly, Steve, Buckley, Gerry, Clark, Robin D., Roe, Robert, Blasey, Christine, Belanoff, Joe

“…This manuscript reports the identification of a potent, selective GR antagonist with oral bioavailability. CORT118335 exhibited excellent efficacy at a low…”
Get full text

Azepines and Piperidines with Dual Norepinephrine Dopamine Uptake Inhibition and Antidepressant Activity by Brown, Dean G, Bernstein, Peter R, Wu, Ye, Urbanek, Rebecca A, Becker, Christopher W, Throner, Scott R, Dembofsky, Bruce T, Steelman, Gary B, Lazor, Lois A, Scott, Clay W, Wood, Michael W, Wesolowski, Steven S, Nugiel, David A, Koch, Stephanie, Yu, Jian, Pivonka, Donald E, Li, Shuang, Thompson, Carol, Zacco, Anna, Elmore, Charles S, Schroeder, Patricia, Liu, JianWei, Hurley, Christopher A, Ward, Stuart, Hunt, Hazel J, Williams, Karen, McLaughlin, Joseph, Hoesch, Valerie, Sydserff, Simon, Maier, Donna, Aharony, David

“…Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin…”
Get full text

FKBP5 mRNA Expression Is a Biomarker for GR Antagonism by Bali, Utsav, Phillips, Tim, Hunt, Hazel, Unitt, John

“…Context: Endogenous Cushing's syndrome is caused by chronically elevated levels of cortisol. Mifepristone, a glucocorticoid receptor (GR) antagonist, is…”
Get full text

SAT-224 Pharmacokinetics of the selective glucocorticoid receptor modulator miricorilant in healthy volunteers and patients with presumed metabolic dysfunction-associated steatohepatitis (MASH) by Custodio, Joseph M., Donaldson, Kirsteen, Kunta, Jeevan, Juneja, Kavita, Alkhouri, Naim, Hunt, Hazel J.

Get full text