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Dr. John Gilmer

Associate Professor (Pharmacy)
25/6/7 WESTLAND ROW


  ASPIRIN   BINDING   BIOLOGICAL-MEMBRANES   BUTYRYLCHOLINESTERASE   Design, synthesis and testing of specific enzyme inhibitors   ENZYME SUBSTRATE SPECIFICITIES   HOST-GUEST CHEMISTRY   HYDROLYSIS   IMPROVED DELIVERY   Isosorbide-based therapies for Alzheimer's disease   MOLECULAR RECOGNITION   PRODRUG   Pro-drug design for tissue targeting   RECEPTORS   STEROIDS   Thyrotropin-releasing hormone-degrading ectoenzyme inhibitors in the treatment of CNS disorders
 Investigation into highly potent inhibitors of butyrylcholinesterase
 A new system for targeting steroids to the colon
 Exploiting chemical libraries, structural analysis and biological testing to design thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) inhibitors for use in the treatment of CNS disorders
 Development of novel aspirin prodrugs
 Isosorbide as a building block for novel human butyrylcholinesterase probes

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Details Date
Member, DMMC Cancer Principal Investigators, Trans-institutional grouping of Principal Investigators leading research on Cancer themes
Member, Core Technology PI's, DMMC Principal Investigators leading the development of core technology platforms.
Member, Centre for Research into Global Disease (Proposed), This consortium combines researchers with complementary interests in globally significant infectious disease. Interests include innate immunity, immune regulation, regional immunity, immune evasiob, vaccine & adjuvant development as well as drug & target development.
Invitee, Colorectal & GI Cancer Research Group (Proposed), Speculative idea to cluster PI's around collaborative study on Upper GI and Colon Cancers.Deliberately wide selection of surgeons, pathologists and academic researchers based on stated interest or publication in fields of oesophageal or colorectal cancer.To be reviewed/focused by DK/JR/PMacM.Extracted from DMMC Research Database - 8 Nov 2004.
Member, PHG Funded PI's and Researchers, All Researchers funded under Cycle 3 PRTLI - Programme for Human Genomics
Details Date From Date To
Member of European Federation of Pharmaceutical Scientists
V Voon, C Watson, N Glezeva, M Bermingham, J Wang, R O'Hanlon, J Baugh, K Mc Donald, J Gilmer, M Ledwidge, Doxycycline attenuates matrix metalloproteinase release from inflammatory cells in-vitro and in patients with asymptomatic left ventricular diastolic dysfunction, EUROPEAN JOURNAL OF HEART FAILURE, 16, 2014, pp91-, Conference Paper, PUBLISHED
N Glezeva, M Santos-Martinez, C Watson, K Mcdonald, C Medina, J Gilmer, M Ledwidge, Inhibition of thromboxane pathways in monocytes impedes cell invasiveness, EUROPEAN JOURNAL OF HEART FAILURE, 16, 2014, pp208-209 , Conference Paper, PUBLISHED
Circ Heart Fail. 2014 Feb 3. [Epub ahead of print] Aspirin Use In Heart Failure: Is Low Dose Therapy Associated With Mortality And Morbidity Benefits In A Large Community Population? Bermingham M, Shanahan MK, O'Connell E, Dawkins I, Miwa S, O'Hanlon R, Gilmer J, McDonald K, Ledwidge M., Aspirin Use In Heart Failure: Is Low Dose Therapy Associated With Mortality And Morbidity Benefits In A Large Community Population?, Circulation: Heart Failure, Feb 3, 2014, DOI:10.116, Notes: [Featured on Medscape Heartwire: http://www.medscape.com/viewarticle/820323], Journal Article, PUBLISHED
Paul Matthew O'Byrne , Robert Williams, John Walsh, John Gilmer, Synthesis, screening and pharmacokinetic evaluation of potential prodrugs of bupropion, Pharmaceuticals, Pharmaceuticals-5009, 2014, Notes: [Accepted May 8th 2014], Journal Article, PUBLISHED
Paul Matthew O'Byrne *, Robert Williams, John Walsh, John Gilmer, Evaluation of N-methylbupropion as a potential prodrug of bupropion in the guinea pig, Pharmaceuticals, Manuscript 50097 , 2014, Journal Article, PUBLISHED
Shane O'Sullivan, John F Gilmer and Carlos Medina, Matrix metalloproteinases in inflammatory bowel disease: an update, Mediators of Inflammation, 2014, Review Article, PUBLISHED
SimplĂ­cio AL, Coroadinha AS, Gilmer JF, Lamego J., A methodology for detection and quantification of esterase activity., Methods in Molecular Biology, 984, 2013, p309-19 , Journal Article, PUBLISHED
Marquez Ruiz JF, Kedziora K, Pigott M, Keogh B, Windle H, Gavin J, Kelleher DP, Gilmer JF., A nitrophenyl-based prodrug type for colorectal targeting of prednisolone, budesonide and celecoxib., Bioorg Med Chem Lett, 23, (6), 2013, p1693-8 , Notes: [PMID: 23416011], Journal Article, PUBLISHED
Wang J, Radomski MW, Medina C, Gilmer JF., MMP inhibition by barbiturate homodimers., Bioorganic and Medicinal Chemistry Letters, 23, (2), 2013, p444-7 , Journal Article, PUBLISHED
Gavin J, Ruiz JF, Kedziora K, Windle H, Kelleher DP, Gilmer JF., Structure requirements for anaerobe processing of azo compounds: implications for prodrug design., Bioorganic and Medicinal Chemistry Letters, 22, (24), 2013, Journal Article, PUBLISHED
  

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Gilmer JF, Byrne W, Rynne A, Isosorbide Aspirinate Esters, 1998, WO 9817673 , Patent, PUBLISHED
Gilmer JF, Byrne W, Cardioactive Aspirinates, 1997, WO 9705128, Patent, PUBLISHED

  

i) Enzyme inhibitors . Isosorbide-based inhibitors of butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE): synthesis and biochemistry; the role of BuChE in Alzheimer's disease . Rational design of selective covalent inhibitors of COX-2 . Rational design, synthesis and testing of inhibitors for thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) ii) Prodrugs and metabolic hydrolysis . Design and evaluation of aspirin-based antiplatelet agents with reduced gastric toxicity relative to aspirin . Intelligent prodrug carrier systems for targeting corticosteroids to the colon . Exploring metabolic vectors for site specific drug delivery