O'Neill, Paul - University of Liverpool

个人简介

Paul M. O'Neill graduated in Chemistry and Pharmacology at the University of Liverpool in 1990 and also obtained a Ph.D degree here in 1995. Following graduation, he was appointed Roche Lecturer in Medicinal Chemistry in the Department of Pharmacology at Liverpool from 1995-96. In 1997 he carried out postdoctoral research with Professor Gary H. Posner at the Johns Hopkins University, Baltimore, USA. In 1998 Paul was appointed to a lectureship between the Departments of Chemistry and Pharmacology at Liverpool and he became Senior Lecturer in 2003 and Reader in 2005.Paul works in several areas of synthetic organic chemistry and pharmacology with a strong emphasis on drug-design, chemical biology and medicinal chemistry of antimalarial and anticancer drugs. Drug Development of 1,2,4,5-Teraoxanes (Invitation to Speak, RSC British High Commission 2011) RSC Malcolm Campbell Award (BMCS Division of The Royal Society of Chemistry 2011) Antimalarial Tetraoxanes; Candidate selection and back-up programme (Invitation to Speak, EU FP6 2011) Update on Tetraoxane Drug Development (Invitation to Speak, St Georges Hospital, London 2010) Medicinal Chemistry of Quinoline and Peroxide Antimalarials (Invitation to Speak, Laboratoire de Chimie de Coordination du CNRS, 205 route de Narbonne, 31077 Toulouse Cedex 4, France 2010) From candidate selection of the first Tetraoxane Drug Candidate RKA 182 to the Discovery of Picomola (Keynote Speech, RSC, London School of Tropical Medicine and Hygiene 2010) Antimalarial Drug Discovery in Academia; Discovery of Isoquine, FAQ4 and RKA182 (Keynote Speech, British High Commission and RSC 2010) Antimalarial Drug Discovery at the University of Liverpool (Invitation to Speak, Pfizer, Sandwich, Kent 2010) From candidate selection of the first Tetraoxane Drug Candidate RKA 182 and Appropriate Back-ups (Keynote Speech, EFMC Sponsored 2nd National Conference on Medicinal Chemistry, Coimbra, Portugal 2010) Synthesis in Medicinal Chemistry (Keynote Speech, Peakdale Molecular Symposium 2010) Antimalarial Drug Discovery in Academia (Keynote Speech, 1st RSC China-UK Symposium on Medicinal Chemistry, Shanghai, China 2009) Synthetic Approaches to Endoperoxide Antimalarials (Invitation to Speak, SCI Conference orgnaised by the SCI Young Chemists Panel 2009) Selection of RKA 182 as the first tetraoxane antimalarial drug candidate (Keynote Speech, Keystone Symposia, Breckenridge Colorado, USA 2009) From the Natural Herb Qinghaosu (Artemisinin) to Orally Active Synthetic Endoperoxide Antima (Invitation to Speak, University of Bangor 2008) Antimalarial Chemotherapy In the 21st Century; Advances in Drugs Targeting the Hemoglobin Degradatio (Invitation to Speak, University of Warwick 2008) Advances in the Medicinal Chemistry of 4-Aminoquinolines (Invitation to Speak, ACS 2007) From the Natural Herb Extract Quinghaosu (Artemisinin) to Orally Active Synthetic Endoperoxide Antim (Invitation to Speak, ESB 2007) Recent Advances in the Development of Drugs Targeting the Hemoglobin Degradation Pathway (Keynote Speech, ACS Medicinal Chemistry & Bioorganic Chemistry Foundation 2007) The Drug Hybrid Approach to Antimalarial Chemotherapy (Invitation to Speak, ISSX 2006) Evidence for a Common Iron Dependent Mechanism of Action for Diverse Endoperoxide Antimalarials (Invitation to Speak, EU COST 2006) A 4-Aminoquinoline Antimalarial for the 21st Century (Invitation to Speak, (IUPHAR) Congress of Pharmacology 2006) Toward a 21st Century Replacement for Chloroquine and Amodiaquine (Invitation to Speak, EU COST Initiative 2005)

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A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum 3D7 Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites Molecular Mechanism of Action of Antimalarial Benzoisothiazolones: Species-Selective Inhibitors of the Plasmodium spp. MEP Pathway enzyme, IspD Optimisation of the synthesis of second generation 1,2,4,5 tetraoxane antimalarials Small Molecule Inhibitors of Cyclophilin D To Protect Mitochondrial Function as a Potential Treatment for Acute Pancreatitis 2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties A Quinoline Carboxamide Antimalarial Drug Candidate Uniquely Targets Plasmodia at Three Stages of the Parasite Life Cycle Antimalarial 4(1H)-pyridones bind to the Q(i) site of cytochrome bc(1) Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials From hybrid compounds to targeted drug delivery in antimalarial therapy Inhibitors of the Plasmodium mitochondrial respiratory chain Integrated transcriptomic and proteomic analyses uncover regulatory roles of Nrf2 in the kidney Plasmodium IspD (2-C-Methyl-D-erythritol 4-Phosphate Cytidyltransferase), an Essential and Druggable Antimalarial Target Quinolone-Hydroxyquinoline Tautomerism in Quinolone 3-Esters. Preserving the 4-Oxoquinoline Structure To Retain Antimalarial Activity Synthesis, structural and conformational analysis, and IR spectra of ethyl 4-chloro-7-iodoquinoline-3-carboxylate Towards depersonalized abacavir therapy: chemical modification eliminates HLA-B*57:01-restricted CD8(+) T-cell activation 4-bromopropofol decreases action potential generation in spinal neurons by inducing a glycine receptor-mediated tonic conductance Identification and quantification of the basal and inducible Nrf2-dependent proteomes in mouse liver: Biochemical, pharmacological and toxicological implications Novel Endoperoxide-Based Transmission-Blocking Antimalarials with Liver- and Blood-Schizontocidal Activities Novel inhibitors of the Plasmodium falciparum electron transport chain Rapid kill of malaria parasites by artemisinin and semi-synthetic endoperoxides involves ROS-dependent depolarization of the membrane potential Tetraoxane-pyrimidine nitrile hybrids as dual stage antimalarials Antimalarial pharmacology and therapeutics of atovaquone