Zobrazeno 1 - 10 of 59 pro vyhledávání: '"Junliang, Hao"'
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Akademický článek
EXPRESSION OF BLOOD EXOSOMAL miR-223 AND NUCLEOTIDE-BINDING OLIGOMERIZATION DOMAIN-LIKE RECEPTOR PROTEIN 3 IN PATIENTS WITH ALZHEIMER’S DISEASE AND THEIR CLINICAL SIGNIFICANCE
Autor: SHI Junliang, HAO Yuping, XIA Yuan, DAI Enyun
Publikováno v: 精准医学杂志, Vol 38, Iss 5, Pp 460-464 (2023)
Objective To investigate the expression levels of serum exosomal miR-223 and nucleotide-binding oligome-rization domain-like receptor protein 3 (NLRP3) in patients with Alzheimer’s disease (AD) and their association with the development and progres
Externí odkaz: https://doaj.org/article/ba833b3618e744f482a0e775f7ee4504
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2
Effects of DPTQ, a novel positive allosteric modulator of the dopamine D1 receptor, on spontaneous eye blink rate and spatial working memory in the nonhuman primate
Autor: Stacy A. Castner, Linli Zhang, Charles R. Yang, Junliang Hao, Jeffrey W. Cramer, Xushan Wang, Robert F. Bruns, Hugh Marston, Kjell A. Svensson, Graham V. Williams
Publikováno v: Psychopharmacology. 240:1033-1048
Rationale Dopamine (DA) signaling through the D1 receptor has been shown to be integral to multiple aspects of cognition, including the core process of working memory. The discovery of positive allosteric modulators (PAMs) of the D1 receptor has enab
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a6213ca6a6549d7eb6e405c83245911c
https://doi.org/10.1007/s00213-022-06282-7
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Ensemble Docking Approach to Mitigate Pregnane X Receptor-Mediated CYP3A4 Induction Risk
Autor: Qi Chen, Xin Zhou, Jessica Rehmel, James P. Steele, Kjell A. Svensson, James P. Beck, Erik J. Hembre, Junliang Hao
Publikováno v: Journal of Chemical Information and Modeling. 63:173-186
Three structurally closely related dopamine D1 receptor positive allosteric modulators (D1 PAMs) based on a tetrahydroisoquinoline (THIQ) scaffold were profiled for their CYP3A4 induction potentials. It was found that the length of the linker at the
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::235e3097a1370103592da8513873ee9b
https://doi.org/10.1021/acs.jcim.2c01175
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6
Development of a Scalable Synthesis of Mevidalen (LY3154207), an Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor
Autor: Katarina Kadlecikova, John R. Rizzo, Mo Jia, Peter G. Houghton, Conchita Fernandez Garcia, Kevin P. Cole, Jeffery Richardson, Jared L. Piper, Junliang Hao, Amy C. DeBaillie, Peng Liu, Daniel S. Richards, Ping Huang
Publikováno v: Organic Process Research & Development. 24:2549-2564
The evolution from early medicinal chemistry to large-scale production of the chemical synthesis of Lilly D1 positive allosteric modulator mevidalen (LY3154207) and its hydroxybenzoate cocrystal is...
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::20e6fb959778af8ddfb00a678ada3a5c
https://doi.org/10.1021/acs.oprd.0c00229
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A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk
Autor: Tao Liu, James P. Beck, Junliang Hao
Publikováno v: RSC Med Chem
The human pregnane X receptor (hPXR) regulates the expression of major drug metabolizing enzymes. A wide range of drug candidates bind and activate hPXR, and hence are at risk of increasing drug–drug interactions and reducing clinical efficacy. hPX
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::854c802409d9519e0dffcd491d76aaf5
https://pubmed.ncbi.nlm.nih.gov/35308029
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Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor
Autor: Robert F. Bruns, Qi Chen, Paloma Vidal, John Mehnert Schaus, Charles R. Yang, Stephen N. Mitchell, Steven Marc Massey, Nuria Diaz, Xushan Wang, David Andrew Coates, Rebecca A. Wright, Beverly A. Heinz, Kevin Matthew Gardinier, Greg Stephenson, James P. Beck, Rajni M. Bhardwaj, Julie F. Falcone, Bruce A. Dressman, Deanna L Maren, Anette M. Johansson, David Michael Remick, Jeff W. Cramer, Cohen Michael Philip, Brian Morgan Watson, Jeffery Richardson, Kjell Svensson, Xin Zhou, Erik James Hembre, Serge Louis Boulet, Reinhard Matthew Robert, Daniel S. Richards, Junliang Hao, David M. Bender, Guy Carter, Christopher David Beadle, Brian G. Getman, Wolfangel Craig Daniel, Diseroad Benjamin Alan, Jason K. Myers, Joseph H. Krushinski, David Edward Tupper
Publikováno v: Journal of Medicinal Chemistry. 62:8711-8732
Clinical development of catechol-based orthosteric agonists of the dopamine D1 receptor has thus far been unsuccessful due to multiple challenges. To address these issues, we identified LY3154207 (...
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5a353395d3c6f7ca6dfa78c95a347dd4
https://doi.org/10.1021/acs.jmedchem.9b01234
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9
The allosteric dopamine D1 receptor potentiator, DETQ, ameliorates subchronic phencyclidine-induced object recognition memory deficits and enhances cortical acetylcholine efflux in male humanized D1 receptor knock-in mice
Autor: Junliang Hao, Francesco Matrisciano, Kjell A. Svensson, Lakshmi Rajagopal, Herbert Y. Meltzer, Mei Huang
Publikováno v: Behavioural Brain Research. 361:139-150
Diminished dopamine D1 stimulation may contribute to cognitive impairment in Alzheimer's and Parkinson's diseases, schizophrenia, and other neuropsychiatric disorders. However, orthosteric D1 receptor (D1R) agonists produce receptor desensitization a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80414d225c9a9bc450633780bf7f652d
https://doi.org/10.1016/j.bbr.2018.12.006
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10
Structural Basis for (S)-3,4-Dicarboxyphenylglycine (DCPG) As a Potent and Subtype Selective Agonist of the mGlu8 Receptor
Autor: Joseph D. Ho, Michelle C. Vargas, Jing Wang, Junliang Hao, Shane Atwell, James A. Monn, Sheela Ashok, Mark G. Bures, Qi Chen, Jeffery M. Schkeryantz
Publikováno v: Journal of Medicinal Chemistry. 61:10040-10052
( S)-3,4-Dicarboxyphenylglycine (DCPG) was first reported in 2001 as a potent orthosteric agonist with high subtype selectivity for the mGlu8 receptor, but the structural basis for its high selectivity is not well understood. We have solved a cocryst
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::33be9a640f18a032be5e1bd51cd0d5b7
https://doi.org/10.1021/acs.jmedchem.8b01120
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