Inverse agonist of ERRγ reduces cannabinoid receptor type 1-mediated induction of fibrinogen synthesis in mice with a high-fat diet-intoxicated liver
Sign Up to like & getrecommendations! Published in 2018 at "Archives of Toxicology"
DOI: 10.1007/s00204-018-2270-4
Abstract: Upon liver intoxication with malnutrition or high-fat diet feeding, fibrinogen is synthesized by hepatocytes and secreted into the blood in human and mouse. Its primary function is to occlude blood vessels upon damage and thereby… read more here.
Keywords: fat diet; inverse agonist; fibrinogen; high fat ... See more keywords
Cannabidiol, a novel inverse agonist for GPR12.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2017.09.001
Abstract: GPR12 is a constitutively active, Gs protein-coupled receptor that currently has no confirmed endogenous ligands. GPR12 may be involved in physiological processes such as maintenance of oocyte meiotic arrest and brain development, as well as… read more here.
Keywords: inverse agonist; cbd; agonist gpr12; cancer ... See more keywords
Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2017.03.013
Abstract: Abstract Histaminergic H3 inverse agonists, by stimulating central histamine release, represent attractive drug candidates to treat cognitive disorders. The present studies aimed to describe the mechanistic profile of S 38093 a novel H3 receptors inverse… read more here.
Keywords: inverse agonist; human receptors; novel inverse; agonist ... See more keywords
PPARγ in Complex with an Antagonist and Inverse Agonist: a Tumble and Trap Mechanism of the Activation Helix
Sign Up to like & getrecommendations! Published in 2018 at "iScience"
DOI: 10.1016/j.isci.2018.06.012
Abstract: Summary Peroxisome proliferator activated receptor γ (PPARγ) is a nuclear receptor and target for antidiabetics that increase insulin sensitivity. Owing to the side effects of PPARγ full agonists, research has recently focused on non-activating ligands… read more here.
Keywords: ppar; inverse agonist; activation helix; helix ... See more keywords
The tamoxifen derivative ridaifen‐B is a high affinity selective CB2 receptor inverse agonist exhibiting anti‐inflammatory and anti‐osteoclastogenic effects
Sign Up to like & getrecommendations! Published in 2018 at "Toxicology and Applied Pharmacology"
DOI: 10.1016/j.taap.2018.06.009
Abstract: &NA; Selective estrogen receptor modulators (SERMs) target estrogen receptors (ERs) to treat breast cancer and osteoporosis. Several SERMs exhibit anti‐cancer activity not related to ERs. To discover novel anti‐cancer drugs acting via ER‐independent mechanisms, derivatives… read more here.
Keywords: anti inflammatory; inverse agonist; high affinity; affinity ... See more keywords
Engineered Coiled-Coil Protein for Delivery of Inverse Agonist for Osteoarthritis.
Sign Up to like & getrecommendations! Published in 2018 at "Biomacromolecules"
DOI: 10.1021/acs.biomac.8b00158
Abstract: Osteoarthritis (OA) results from degenerative and abnormal function of joints, with localized biochemistry playing a critical role in its onset and progression. As high levels of all- trans retinoic acid (ATRA) in synovial fluid have… read more here.
Keywords: protein; inverse agonist; delivery; osteoarthritis ... See more keywords
Discovery of Novel N-Sulfonamide-tetrahydroquinolines as Potent Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists for the Treatment of Psoriasis.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c02318
Abstract: Guided by the mode of action of 13, our previously discovered RORγt inverse agonist, we conducted five rounds of design syntheses and structure-activity relationship (SAR) studies, ultimately identifying RORγt inverse agonist 5a, which exhibited superior… read more here.
Keywords: receptor; ror inverse; discovery novel; inverse agonist ... See more keywords
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00392
Abstract: The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to… read more here.
Keywords: acid receptor; inverse agonist; receptor related; retinoic acid ... See more keywords
Synthesis of A-9758, an Inverse Agonist of Retinoic Acid-Related Orphan Receptor γt
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c06060
Abstract: A-9758 is an inverse agonist of retinoic acid-related orphan receptor γt with well-characterized in vitro and in vivo anti-inflammatory activity. A chromatography-free decagram-scale synthesis of this compound was developed to support pre-clinical research activities. This… read more here.
Keywords: acid related; agonist retinoic; acid; 9758 inverse ... See more keywords
Backbone Modification Provides a Long-Acting Inverse Agonist of Pathogenic, Constitutively Active PTH1R Variants.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.3c09694
Abstract: Parathyroid hormone 1 receptor (PTH1R) plays a key role in mediating calcium homeostasis and bone development, and aberrant PTH1R activity underlies several human diseases. Peptidic PTH1R antagonists and inverse agonists have therapeutic potential in treating… read more here.
Keywords: active pth1r; constitutively active; pth1r; backbone modification ... See more keywords
Opposite alterations of 5HT2A receptor brain density in subjects with schizophrenia: relevance of radiotracers pharmacological profile
Sign Up to like & getrecommendations! Published in 2021 at "Translational Psychiatry"
DOI: 10.1038/s41398-021-01430-7
Abstract: The status of serotonin 5HT 2A receptors (5HT 2A Rs) in schizophrenia has been controversial. In vivo positron emission tomography neuroimaging and in vitro post-mortem binding studies have reported conflicting results about 5HT 2A R… read more here.
Keywords: inverse agonist; pharmacological profile; subjects schizophrenia; density ... See more keywords