Search Results - "Xia, Anjie"
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Ligand recognition and allosteric regulation of DRD1-Gs signaling complexes
Published in Cell (18-02-2021)“…Dopamine receptors, including D1- and D2-like receptors, are important therapeutic targets in a variety of neurological syndromes, as well as cardiovascular…”
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A new generation Mpro inhibitor with potent activity against SARS-CoV-2 Omicron variants
Published in Signal transduction and targeted therapy (16-03-2023)“…Emerging SARS-CoV-2 variants, particularly the Omicron variant and its sublineages, continually threaten the global public health. Small molecule antivirals…”
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Discovery of 5-((1H-indazol-3-yl) methylene)-2-thioxoimidazolidin-4-one derivatives as a new class of AHR agonists with anti-psoriasis activity in a mouse model
Published in Bioorganic & medicinal chemistry letters (15-08-2023)“…[Display omitted] Aryl hydrocarbon receptor (AHR) is a ligand dependent transcription factor and participates in the regulation of the immune balance of…”
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Structure‐Guided Discovery of a Potent and Selective Cell‐Active Inhibitor of SETDB1 Tudor Domain
Published in Angewandte Chemie International Edition (12-04-2021)“…SET domain bifurcated protein 1 (SETDB1) is a histone lysine methyltransferase that promotes the silencing of some tumour suppressor genes and is overexpressed…”
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C3 ester side chain plays a pivotal role in the antitumor activity of Maytansinoids
Published in Biochemical and biophysical research communications (20-08-2021)“…Maytansinoids, the chemical derivatives of Maytansine, are commonly used as potent cytotoxic payloads in antibody-drug conjugates (ADC)…”
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Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1
Published in Nature chemical biology (01-08-2022)“…Given the promising clinical value of allosteric modulators of G protein-coupled-receptors (GPCRs), mechanistic understanding of how these modulators alter…”
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Discovery of (S)-3-(4-(benzyloxy)phenyl)-2-(2-phenoxyacetamido)propanoic acid derivatives as a new class of GPR34 antagonists
Published in Bioorganic & medicinal chemistry letters (01-01-2024)“…[Display omitted] GPR34 is a rhodopsin-like class G protein-coupled receptor (GPCR) that is involved in the development and progression of several diseases…”
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Discovery of 2-vinyl-10H-phenothiazine derivatives as a class of ferroptosis inhibitors with minimal human Ether-a-go-go related gene (hERG) activity for the treatment of DOX-induced cardiomyopathy
Published in Bioorganic & medicinal chemistry letters (15-10-2022)“…[Display omitted] Ferroptosis was an iron-dependent, nonapoptotic form of regulated cell death. In our previous study, we discovered a potent ferroptosis…”
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Metal-Free Aerobic Oxidative Selective C–C Bond Cleavage in Heteroaryl-Containing Primary and Secondary Alcohols
Published in Organic letters (03-05-2019)“…A transition-metal-free aerobic oxidative selective C–C bond-cleavage reaction in primary and secondary heteroaryl alcohols is reported. This reaction was…”
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Identification of a new class of activators of the Hippo pathway with antitumor activity in vitro and in vivo
Published in Biochemical pharmacology (01-06-2024)“…[Display omitted] The Hippo pathway is a key regulator of tissue growth, organ size, and tumorigenesis. Activating the Hippo pathway by gene editing or…”
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Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis
Published in European journal of medicinal chemistry (15-03-2022)“…The NLRP3 inflammasome, which regulated a proinflammatory programmed cell death form termed pyroptosis, is involved in the pathological process of various…”
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Discovery of Small Molecule Agonist of Gonadotropin-Releasing Hormone Receptor (GnRH1R)
Published in Journal of chemical information and modeling (24-10-2022)“…The gonadotrophin-releasing hormone (GnRH) is a central regulator of the human reproductive system and exerts physiological effects by binding to GnRH1R. The…”
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Discovery of benzodiazepine derivatives as a new class of covalent inhibitors of SARS-CoV–2 main protease
Published in Bioorganic & medicinal chemistry letters (15-08-2023)“…[Display omitted] The COVID-19 pandemic has caused people immense suffering all over the world. Although the World Health Organization (WHO) has announced the…”
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Structure-based identification of a G protein-biased allosteric modulator of cannabinoid receptor CB1
Published in Proceedings of the National Academy of Sciences - PNAS (11-06-2024)“…is known for its therapeutic benefit in various diseases including pain relief by targeting cannabinoid receptors. The primary component of cannabis,…”
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Discovery of 3-phenyl-1,2,4-oxadiazole derivatives as a new class of SARS-CoV-2 main protease inhibitors
Published in Bioorganic & medicinal chemistry letters (15-04-2023)“…[Display omitted] The ongoing COVID-19 pandemic has led to massive infections and deaths and caused tremendous grief among the people. Although vaccines have…”
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Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors
Published in Bioorganic & medicinal chemistry letters (15-09-2019)“…[Display omitted] Inhibitors of the Hippo signaling pathway have been demonstrated to have a potential clinical application in cases such as tissue repair and…”
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Discovery of a novel pyroptosis inhibitor acting though modulating glutathionylation to suppress NLRP3-related signal pathway
Published in International immunopharmacology (25-01-2024)“…Pyroptosis is a proinflammatory type of regulated cell death and has been involved in many pathological processes. Inhibition of pyroptosis is thought to be a…”
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Discovery of 6,7-dihydro-5H-pyrrolo[3,4-d] pyrimidine derivatives as a new class of ATR inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2022)“…[Display omitted] Ataxia telangiectasia and Rad3-related (ATR) kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing…”
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Discovery of 4‑(1,2,4-Oxadiazol-5-yl)azepan-2-one Derivatives as a New Class of Cannabinoid Type 2 Receptor Agonists for the Treatment of Inflammatory Pain
Published in Journal of medicinal chemistry (09-03-2023)“…Selectively targeting the cannabinoid receptor CB2 is an attractive therapeutic strategy for the treatment of inflammatory pain without psychiatric side…”
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