Identifying the receptor subtype selectivity of retinoid X and retinoic acid receptors via quantum mechanics
Sign Up to like & getrecommendations! Published in 2017 at "FEBS Open Bio"
DOI: 10.1002/2211-5463.12188
Abstract: Understanding and identifying the receptor subtype selectivity of a ligand is an important issue in the field of drug discovery. Using a combination of classical molecular mechanics and quantum mechanical calculations, this report assesses the… read more here.
Keywords: receptor; subtype selectivity; receptor subtype; mechanics ... See more keywords
Upregulation of Striatal Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Rats with Excessive Glutamate Release Induced by N-Acetylcysteine
Sign Up to like & getrecommendations! Published in 2022 at "Neurotoxicity Research"
DOI: 10.1007/s12640-021-00449-4
Abstract: The aim of this study is to investigate the changes in expression of metabotropic glutamate (Glu) receptor subtype 1 (mGluR1), a key molecule involved in neuroexcitetoxicity, during excessive Glu release in the brain by PET… read more here.
Keywords: glu; release; metabotropic glutamate; receptor subtype ... See more keywords
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A3 adenosine receptor subtype.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.08.042
Abstract: [1,2,4]Triazolo[1,5-c]pyrimidine is a promising platform to develop adenosine receptor antagonists. Here, we tried to investigate the effect of the substituent at the 8 position of [1,2,4]triazolo[1,5-c]pyrimidine derivatives on affinity and selectivity at the human A3… read more here.
Keywords: position; adenosine receptor; receptor subtype; receptor antagonists ... See more keywords
Structure-dependent receptor subtype selectivity and G protein subtype preference of heterocyclic agonists in heterologously expressed silkworm octopamine receptors.
Sign Up to like & getrecommendations! Published in 2021 at "Pesticide biochemistry and physiology"
DOI: 10.1016/j.pestbp.2021.104895
Abstract: (R)-Octopamine (OA), a major invertebrate biogenic amine, plays an important role in a wide variety of physiological processes as a neurohormone, neuromodulator, and neurotransmitter in insects. OA receptors (OARs) are class A G protein-coupled receptors… read more here.
Keywords: subtype selectivity; dependent receptor; receptor subtype; subtype ... See more keywords
Cannabinoid Receptor Subtype 2 (CB2R) in a Multitarget Approach: Perspective of an Innovative Strategy in Cancer and Neurodegeneration.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01357
Abstract: The cannabinoid receptor subtype 2 (CB2R) represents an interesting and new therapeutic target for its involvement in the first steps of neurodegeneration as well as in cancer onset and progression. Several studies, focused on different… read more here.
Keywords: subtype cb2r; cannabinoid receptor; cb2r; receptor subtype ... See more keywords
Somatostatin Receptor Subtype-2 Targeting System for Specific Delivery of Temozolomide
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.3c00223
Abstract: Temozolomide (TMZ) is a DNA alkylating agent that produces objective responses in patients with neuroendocrine tumors (NETs) when the DNA repair enzyme O6-methylguanine-DNA methyltransferase (MGMT) is inactivated. At high doses, TMZ therapy exhausts MGMT activity… read more here.
Keywords: receptor; receptor subtype; delivery; somatostatin receptor ... See more keywords
Discovery of 4-(5-Membered)Heteroarylether-6-methylpicolinamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5
Sign Up to like & getrecommendations! Published in 2024 at "ACS Medicinal Chemistry Letters"
DOI: 10.1021/acsmedchemlett.4c00481
Abstract: This Letter details our efforts to develop novel, non-acetylene-containing metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulators (NAMs) with improved pharmacological properties. This endeavor involved replacing the ether-linked pyrimidine moiety, a metabolic liability, with… read more here.
Keywords: allosteric modulators; receptor subtype; negative allosteric; glutamate receptor ... See more keywords
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00306
Abstract: A series of structurally diverse azaspirodecanone and spirooxazolidinone analogues were designed and synthesized as potent and selective somatostatin receptor subtype 5 (SSTR5) antagonists. Four optimized compounds each representing a subseries showed improvement in their metabolic… read more here.
Keywords: somatostatin receptor; optimization preclinical; preclinical metabolism; receptor subtype ... See more keywords
Altered Prostaglandin E Receptor Subtype 3 Expression in Lacrimal Glands of Patients with Chronic Stevens-Johnson Syndrome
Sign Up to like & getrecommendations! Published in 2022 at "Ocular Immunology and Inflammation"
DOI: 10.1080/09273948.2022.2028286
Abstract: ABSTRACT Purpose To compare the prostaglandin E2 receptor subtype 3 (EP3) distribution in the lacrimal glands of normals, non-specific dacryoadenitis, and chronic Stevens-Johnson syndrome (SJS) patients. Methods Biopsies from lacrimal glands of four chronic SJS… read more here.
Keywords: chronic stevens; expression; receptor subtype; ep3 expression ... See more keywords
Cannabinoid Receptor Subtype-1 Regulates Allergic Airway Eosinophilia During Lung Helminth Infection.
Sign Up to like & getrecommendations! Published in 2021 at "Cannabis and cannabinoid research"
DOI: 10.1089/can.2020.0167
Abstract: Introduction: Over 1 billion humans carry infectious helminth parasites that can lead to chronic comorbidities such as anemia and growth retardation in children. Helminths induce a T-helper type 2 (Th2) immune response in the host… read more here.
Keywords: cannabinoid receptor; receptor subtype; mice; infection ... See more keywords
Single neuron serotonin receptor subtype gene expression correlates with behaviour within and across three molluscan species
Sign Up to like & getrecommendations! Published in 2018 at "Proceedings of the Royal Society B: Biological Sciences"
DOI: 10.1098/rspb.2018.0791
Abstract: The marine mollusc, Pleurobranchaea californica varies daily in whether it swims and this correlates with whether serotonin (5-HT) enhances the strength of synapses made by the swim central pattern generator neuron, A1/C2. Another species, Tritonia… read more here.
Keywords: neuron; serotonin; gene expression; expression ... See more keywords