Keisuke Hirai, PhD, Osaka University - Related publications

Takeda Chemical Industries 
Neurodegenerative diseases
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50 most relevant papers in past 60 days:
Year Citation  Score
2020 Paudel P, Shrestha S, Park SE, Seong SH, Fauzi FM, Jung HA, Choi JS. Emodin Derivatives as Multi-Target-Directed Ligands Inhibiting Monoamine Oxidase and Antagonizing Vasopressin V Receptors. Acs Omega. 5: 26720-26731. PMID 33110998 DOI: 10.1021/acsomega.0c03649   
2020 de Luna Martins D, Borges AA, E Silva NADA, Faria JV, Hoelz LVB, de Souza HVCM, Bello ML, Boechat N, Ferreira VF, Faria RX. P2X7 receptor inhibition by 2-amino-3-aryl-1,4-naphthoquinones. Bioorganic Chemistry. 104: 104278. PMID 33010623 DOI: 10.1016/j.bioorg.2020.104278   
2020 Xie XY, Li YY, Ma WH, Chen AF, Sun YT, Lee JY, Riad A, Xu DH, Mach RH, Huang YS. Synthesis, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective σR/TMEM97 ligands. European Journal of Medicinal Chemistry. 209: 112906. PMID 33049607 DOI: 10.1016/j.ejmech.2020.112906   
2020 Cerda-Cavieres C, Quiroz G, Iturriaga-Vásquez P, Rodríguez-Lavado J, Alarcón-Espósito J, Saitz C, Pessoa-Mahana CD, Chung H, Araya-Maturana R, Mella-Raipán J, Cabezas D, Ojeda-Gómez C, Reyes-Parada M, Pessoa-Mahana H. Synthesis, Docking, 3-D-Qsar, and Biological Assays of Novel Indole Derivatives Targeting Serotonin Transporter, Dopamine D2 Receptor, and Mao-A Enzyme: In the Pursuit for Potential Multitarget Directed Ligands. Molecules (Basel, Switzerland). 25. PMID 33050524 DOI: 10.3390/molecules25204614   
2020 Boutin JA, Witt-Enderby PA, Sotriffer C, Zlotos DP. Melatonin receptor ligands: A pharmaco-chemical perspective. Journal of Pineal Research. 69: e12672. PMID 32531076 DOI: 10.1111/jpi.12672   
2020 Pieterse L, van der Walt MM, Terre'Blanche G. C2-substituted quinazolinone derivatives exhibit A and/or A adenosine receptor affinities in the low micromolar range. Bioorganic & Medicinal Chemistry Letters. 30: 127274. PMID 32631506 DOI: 10.1016/j.bmcl.2020.127274   
2020 Wang Y, Wang J, Fu Z, Sheng R, Wu W, Fan J, Guo R. Syntheses and evaluation of daphnetin derivatives as novel G protein-coupled receptor inhibitors and activators. Bioorganic Chemistry. 104: 104342. PMID 33142412 DOI: 10.1016/j.bioorg.2020.104342   
2020 Gunera J, Baker JG, van Hilten N, Rosenbaum DM, Kolb P. Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor. Journal of Medicinal Chemistry. PMID 32977721 DOI: 10.1021/acs.jmedchem.0c00964   
2020 Jin Y, Qiu CY, Wei S, Han L, Liu TT, Hu WP. Potentiation of P2X3 receptor mediated currents by endothelin-1 in rat dorsal root ganglion neurons. Neuropharmacology. 108356. PMID 33069757 DOI: 10.1016/j.neuropharm.2020.108356   
2020 Ferlenghi F, Maccioni P, Mugnaini C, Brizzi A, Fara F, Mostallino R, Castelli MP, Colombo G, Mor M, Vacondio F, Corelli F. The GABA receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation For Pharmaceutical Sciences. 155: 105544. PMID 32927068 DOI: 10.1016/j.ejps.2020.105544   
2020 Haspula D, Clark MA. Cannabinoid Receptors: An Update on Cell Signaling, Pathophysiological Roles and Therapeutic Opportunities in Neurological, Cardiovascular, and Inflammatory Diseases. International Journal of Molecular Sciences. 21. PMID 33080916 DOI: 10.3390/ijms21207693   
2020 Iman S, Saleem U, Ahmad B. Pharmacological Screening of Seeds for Antidepressant-like Action Along with a Mechanistic Study. Acs Omega. 5: 26924-26932. PMID 33111019 DOI: 10.1021/acsomega.0c04187   
2020 Noumi E, Snoussi M, Anouar EH, Alreshidi M, Veettil VN, Elkahoui S, Adnan M, Patel M, Kadri A, Aouadi K, De Feo V, Badraoui R. HR-LCMS-Based Metabolite Profiling, Antioxidant, and Anticancer Properties of L. Methanolic Extract: Computational and In Vitro Study. Antioxidants (Basel, Switzerland). 9. PMID 33167507 DOI: 10.3390/antiox9111089   
2020 Li M, Huang C, Wu X, Ding F, Hu Z, Zhu Y, Zhao L, Hou L, Chen H, Wang H, Xu J, Tang D. The optimization of a novel selective antagonist for human M muscarinic acetylcholine receptor. Bioorganic & Medicinal Chemistry Letters. 30: 127632. PMID 33132116 DOI: 10.1016/j.bmcl.2020.127632   
2020 Mercer SE, Chaturvedula PV, Conway CM, Cook DA, Davis CD, Pin SS, Macci R, Schartman R, Signor LJ, Widmann KA, Whiterock VJ, Chen P, Xu C, Herbst JJ, Kostich WA, et al. Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 127624. PMID 33096162 DOI: 10.1016/j.bmcl.2020.127624   
2020 Corboz MR, Salvail W, Gagnon S, LaSala D, Laurent CE, Salvail D, Chen KJ, Cipolla D, Perkins WR, Chapman RW. Prostanoid receptor subtypes involved in treprostinil-mediated vasodilation of rat pulmonary arteries and in treprostinil-mediated inhibition of collagen gene expression of human lung fibroblasts. Prostaglandins & Other Lipid Mediators. 106486. PMID 33011365 DOI: 10.1016/j.prostaglandins.2020.106486   
2020 Grosicki M, Adami M, Micheloni C, Głuch-Lutwin M, Siwek A, Latacz G, Łażewska D, Więcek M, Reiner D, Stark H, Chlopicki S, Kieć-Kononowicz K. Eosinophils adhesion assay as a tool for phenotypic drug screening - The pharmacology of 1,3,5 - Triazine and 1h-indole like derivatives against the human histamine H receptor. European Journal of Pharmacology. 173611. PMID 33017589 DOI: 10.1016/j.ejphar.2020.173611   
2020 Velard F, Chatron-Colliet A, Côme D, Ah-Kioon MD, Lin H, Hafsia N, Cohen-Solal M, Ea HK, Lioté F. Adrenomedullin and truncated peptide adrenomedullin(22-52) affect chondrocyte response to apoptotis in vitro: downregulation of FAS protects chondrocyte from cell death. Scientific Reports. 10: 16740. PMID 33028903 DOI: 10.1038/s41598-020-73924-1   
2020 Wang Y, Meagher RB, Ambati S, Ma P, Phillips BG. Patients with obstructive sleep apnea have suppressed levels of soluble cytokine receptors involved in neurodegenerative disease, but normal levels with airways therapy. Sleep & Breathing = Schlaf & Atmung. PMID 33037528 DOI: 10.1007/s11325-020-02205-y   
2020 Eissa IH, El-Helby AA, Mahdy HA, Khalifa MM, Elnagar HA, Mehany ABM, Metwaly AM, Elhendawy MA, Radwan MM, ElSohly MA, El-Adl K. Discovery of new quinazolin-4(3H)-ones as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative evaluation. Bioorganic Chemistry. 105: 104380. PMID 33128967 DOI: 10.1016/j.bioorg.2020.104380   
2020 Karra AG, Tziortziou M, Kylindri P, Georgatza D, Gorgogietas VA, Makiou A, Krokida A, Tsialtas I, Kalousi FD, Papadopoulos GE, Papadopoulou KΚ, Psarra AG. Boswellic acids and their derivatives as potent regulators of glucocorticoid receptor actions. Archives of Biochemistry and Biophysics. 695: 108656. PMID 33127380 DOI: 10.1016/   
2020 Buñay J, Fouache A, Trousson A, de Joussineau C, Bouchareb E, Zhekun Z, Kocer A, Morel L, Baron S, Lobaccaro JMA. Screening for Liver X Receptor modulators: where are we and for what use? British Journal of Pharmacology. PMID 33080050 DOI: 10.1111/bph.15286   
2020 Zhu C, Li X, Peng W, Fu W. Discovery of Novel Indolealkylpiperazine Derivatives as Potent 5-HT Receptor Agonists for the Potential Future Treatment of Depression. Molecules (Basel, Switzerland). 25. PMID 33139658 DOI: 10.3390/molecules25215078   
2020 Kopp N, Holtschulte C, Börgel F, Lehmkuhl K, Friedland K, Civenni G, Laurini E, Catapano CV, Pricl S, Humpf HU, Schepmann D, Wünsch B. Novel σ antagonists designed for tumor therapy: Structure - activity relationships of aminoethyl substituted cyclohexanes. European Journal of Medicinal Chemistry. 112950. PMID 33148494 DOI: 10.1016/j.ejmech.2020.112950   
2020 Tapia C, Zamarreño F, Salvador GA, Casali CI, Viso J, Fernandez MDC, White JH, González-Pardo V. Down-regulation of COX-2 activity by 1α,25(OH)D is VDR dependent in endothelial cells transformed by Kaposi's sarcoma-associated herpesvirus G protein-coupled receptor. Heliyon. 6: e05149. PMID 33072916 DOI: 10.1016/j.heliyon.2020.e05149   
2020 Masih A, Agnihotri AK, Srivastava JK, Pandey N, Bhat HR, Singh UP. Discovery of novel 1,3,5-triazine as adenosine A receptor antagonist for benefit in Parkinson's disease. Journal of Biochemical and Molecular Toxicology. e22659. PMID 33156955 DOI: 10.1002/jbt.22659   
2020 Préville C, Bonaventure P, Koudriakova T, Lord B, Nepomuceno D, Rizzolio M, Mani N, Coe KJ, Ndifor A, Dugovic C, Dvorak CA, Coate H, Pippel DJ, Fitzgerald A, Allison B, et al. Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793. Acs Medicinal Chemistry Letters. 11: 2002-2009. PMID 33062185 DOI: 10.1021/acsmedchemlett.0c00085   
2020 Lyons EL, Leone-Kabler S, Kovach AL, Thomas BF, Howlett AC. Cannabinoid receptor subtype influence on neuritogenesis in human SH-SY5Y cells. Molecular and Cellular Neurosciences. 103566. PMID 33049367 DOI: 10.1016/j.mcn.2020.103566   
2020 da Silva MG, Daros GC, de Bitencourt RM. Anti-inflammatory activity of ayahuasca and its implications for the treatment of neurological and psychiatric diseases. Behavioural Brain Research. 113003. PMID 33166569 DOI: 10.1016/j.bbr.2020.113003   
2020 Akabori H, Yamamoto H, Shimizu T, Endo Y, Tani T, Tani M. Involvement of TRPV1-containing peripheral sensory efferents in hemodynamic responses in a rat hemorrhagic shock model. Surgery. PMID 33092809 DOI: 10.1016/j.surg.2020.09.007   
2020 Vadukoot AK, Sharma S, Aretz CD, Kumar S, Gautam N, Alnouti Y, Aldrich AL, Heim CE, Kielian T, Hopkins CR. Synthesis and SAR Studies of 1-Pyrrolo[2,3-]pyridine-2-carboxamides as Phosphodiesterase 4B (PDE4B) Inhibitors. Acs Medicinal Chemistry Letters. 11: 1848-1854. PMID 33062163 DOI: 10.1021/acsmedchemlett.9b00369   
2020 Ye N, Qin W, Tian S, Xu Q, Wold EA, Zhou J, Zhen XC. Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. Journal of Medicinal Chemistry. PMID 33111525 DOI: 10.1021/acs.jmedchem.0c01192   
2020 Li L, Sluter MN, Yu Y, Jiang J. Prostaglandin E receptors as targets for ischemic stroke: Novel evidence and molecular mechanisms of efficacy. Pharmacological Research. 105238. PMID 33053444 DOI: 10.1016/j.phrs.2020.105238   
2020 Yang Q, Lin JN, Sui X, Li H, Kan M, Wang JF, Li J, Zhang Z, Liu XR, Ming ST, Qu XB, Li N. Antiapoptotic effects of velvet antler polypeptides on damaged neurons through the hypothalamic-pituitary-adrenal axis. Journal of Integrative Neuroscience. 19: 469-477. PMID 33070526 DOI: 10.31083/j.jin.2020.03.167   
2020 Sánchez-Pastor E, Trujillo X, Ramos-Flores C, Ríos-Silva M, Andrade F, Cárdenas Y, Castro E, Urzúa Z, Newton-Sánchez O, Huerta M. Type 2 Diabetes Alters Vascular Cannabinoid Receptor 1 Expression, Phosphorylation Status, and Vasorelaxation in Rat Aorta. Molecules (Basel, Switzerland). 25. PMID 33114620 DOI: 10.3390/molecules25214948   
2020 Bergougnan L, Andersen G, Plum-Mörschel L, Evaristi MF, Poirier B, Tardat A, Ermer M, Herbrand T, Arrubla J, Coester HV, Sansone R, Heiss C, Vitse O, Hurbin F, Boiron R, et al. Endothelial-protective effects of a G-protein-biased S1P agonist, SAR247799, in type-2 diabetes rats and a randomized placebo-controlled patient trial. British Journal of Clinical Pharmacology. PMID 33125753 DOI: 10.1111/bcp.14632   
2020 Akhoon BA, Choudhary S, Tiwari H, Kumar A, Barik MR, Rathor L, Pandey R, Nargotra A. Discovery of a new donepezil-like acetylcholinesterase inhibitor for targeting Alzheimer's disease: computational studies with biological validation. Journal of Chemical Information and Modeling. PMID 32955256 DOI: 10.1021/acs.jcim.0c00496   
2020 Agrawal A, Kruse LS, Vangsted AJ, Gartland A, Jørgensen NR. Human P2X7 Receptor Causes Cycle Arrest in RPMI-8226 Myeloma Cells to Alter the Interaction with Osteoblasts and Osteoclasts. Cells. 9. PMID 33105696 DOI: 10.3390/cells9112341   
2020 Reeh K, Summers PA, Gould IR, Woscholski R, Vilar R. Design, synthesis and evaluation of a tripodal receptor for phosphatidylinositol phosphates. Scientific Reports. 10: 18450. PMID 33116198 DOI: 10.1038/s41598-020-75484-w   
2020 Huerga-Gómez A, Aguado T, Sánchez-de la Torre A, Bernal-Chico A, Matute C, Mato S, Guzmán M, Galve-Roperh I, Palazuelos J. Δ -Tetrahydrocannabinol promotes oligodendrocyte development and CNS myelination in vivo. Glia. PMID 32956517 DOI: 10.1002/glia.23911   
2020 Tobinaga H, Kameyama T, Asahi K, Horiguchi T, Oohara M, Taoda Y, Hata K, Hasegawa T, Tada Y, Kurihara N, Kanda Y, Yagi S, Tomari M, Tanaka Y, Takahashi F, et al. Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 3: Structure-activity relationships of pyrropyrazolone derivatives. Bioorganic & Medicinal Chemistry Letters. 30: 127636. PMID 33132115 DOI: 10.1016/j.bmcl.2020.127636   
2020 Xin M, Sun J, Huang W, Tang F, Liu Z, Jin Q, Wang J. Design and synthesis of novel phthalazinone derivatives as potent poly(ADP-ribose)polymerase 1 inhibitors. Future Medicinal Chemistry. PMID 33012191 DOI: 10.4155/fmc-2020-0009   
2020 Eriksson O, Haack T, Hijazi Y, Teichert L, Tavernier V, Laitinen I, Berglund JE, Antoni G, Velikyan I, Johansson L, Pierrou S, Wagner M, Tillner J. Receptor occupancy of dual glucagon-like peptide 1/glucagon receptor agonist SAR425899 in individuals with type 2 diabetes. Scientific Reports. 10: 16758. PMID 33028880 DOI: 10.1038/s41598-020-73815-5   
2020 Vazquez-Rodriguez S, Vilar S, Kachler S, Klotz KN, Uriarte E, Borges F, Matos MJ. Adenosine Receptor Ligands: Coumarin-Chalcone Hybrids as Modulating Agents on the Activity of ARs. Molecules (Basel, Switzerland). 25. PMID 32961824 DOI: 10.3390/molecules25184306   
2020 Sałaciak K, Głuch-Lutwin M, Siwek A, Szafarz M, Kazek G, Bednarski M, Nowiński L, Mitchell E, Jastrzębska-Więsek M, Partyka A, Wesołowska A, Kołaczkowski M, Szkaradek N, Marona H, Sapa J, et al. The antidepressant-like activity of chiral xanthone derivatives may be mediated by 5-HT1A receptor and β-arrestin signalling. Journal of Psychopharmacology (Oxford, England). 269881120959605. PMID 33103555 DOI: 10.1177/0269881120959605   
2020 Divani AA, Andalib S, Biller J, Napoli DM, Moghimi N, Rubinos CA, Nobleza CO, Sylaja PN, Toledano M, Lattanzi S, McCullough LD, Cruz-Flores S, Torbey M, Azarpazhooh MR. Central Nervous System Manifestations Associated with COVID-19. Current Neurology and Neuroscience Reports. 20: 60. PMID 33128130 DOI: 10.1007/s11910-020-01079-7   
2020 Devenish SO, Winters BL, Anderson LL, Arnold JC, McGregor IS, Vaughan CW, Chebib M, Absalom NL. The anticonvulsant zonisamide positively modulates recombinant and native glycine receptors at clinically relevant concentrations. Neuropharmacology. 108371. PMID 33122032 DOI: 10.1016/j.neuropharm.2020.108371   
2020 Medak KD, Shamshoum H, Peppler WT, Wright DC. GLP1 Receptor Agonism Protects Against Acute Olanzapine Induced Hyperglycemia. American Journal of Physiology. Endocrinology and Metabolism. PMID 33017220 DOI: 10.1152/ajpendo.00309.2020   
2020 Song J, Li Y, Zhao C, Zhou Q, Zhang J. Interaction of BDE-47 with nuclear receptors (NRs) based on the cytotoxicity: In vitro investigation and molecular interaction. Ecotoxicology and Environmental Safety. 208: 111390. PMID 33049448 DOI: 10.1016/j.ecoenv.2020.111390   
2020 Chen H, Wang F, Ni X, Rigui Y, Bai Y, Xu L, Yang J, Zhang X, Deng J, Li J, Yin X, Ao W, Kwok KWH, Dong W. Aconitine disrupts serotonin neurotransmission via 5-hydroxytryptamine receptor in zebrafish embryo. Journal of Applied Toxicology : Jat. PMID 33085127 DOI: 10.1002/jat.4059