1. The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats.

    PLoS ONE 9(5):e97139 (2014) PMID 24858947 PMCID PMC4032240

    Hyperglycemia resulting from type 2 diabetes mellitus (T2DM) is the main cause of diabetic complications such as retinopathy and neuropathy. A reduction in hyperglycemia has been shown to prevent these associated complications supporting the importance of glucose control. Glucokinase converts gl...
  2. The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats.

    PLoS ONE 9(5):e97139 (2014) PMID 24858947 PMCID PMC4032240

    Hyperglycemia resulting from type 2 diabetes mellitus (T2DM) is the main cause of diabetic complications such as retinopathy and neuropathy. A reduction in hyperglycemia has been shown to prevent these associated complications supporting the importance of glucose control. Glucokinase converts gl...
  3. Corrigendum to “The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus” [Bioorg. Med. Chem. Lett. 22 (2012) 7100–7105]

    Bioorganic & Medicinal Chemistry Letters 23(17):5022 (2013)

  4. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus

    Bioorganic & Medicinal Chemistry Letters 22(23):7100 (2012)

  5. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.

    Bioorganic & Medicinal Chemistry Letters 22(23):7100 (2012) PMID 23089526

    Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identification of 4-(6-(azetidine-1-carbonyl)-5-fluoropyrid...
  6. Targeting conserved water molecules: Design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization

    Bioorganic & Medicinal Chemistry 20(22):6770 (2012)

  7. Targeting conserved water molecules: design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization.

    Bioorganic & Medicinal Chemistry 20(22):6770 (2012) PMID 23018093

    Inhibitors of the Hsp90 molecular chaperone are showing promise as anti-cancer agents. Here we describe a series of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine ATP competitive Hsp90 inhibitors that were identified following structure-driven optimization of purine hits revealed by NMR based screening ...
  8. Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity.

    Bioorganic & Medicinal Chemistry Letters 22(2):901 (2012) PMID 22209458

    We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration ...
  9. Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity

    Bioorganic & Medicinal Chemistry Letters 22(2):901 (2012)

    VER-156084 ( 1) shows dose-dependant in vivo FAAH inhibition in an anandamide-loading study in the rat.
  10. Are doctors justified in taking industrial action in defence of their pensions? Yes.

    British Medical Journal (Abstracts) 344:e3242 (2012) PMID 22569869

  11. Evidence-based drainage of infected hydronephrosis secondary to ureteric calculi.

    Journal of Endourology 24(2):185 (2010) PMID 20063999

    The obstructed, infected kidney is a urological emergency. It has been accepted that the management of infected hydronephrosis secondary to ureteric stones is through prompt decompression of the collecting system. However, the optimal method of decompression has yet to be established. A PubMed a...
  12. Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.

    Journal of medicinal and pharmaceutical chemistry 52(15):4794 (2009) PMID 19610616

    Inhibitors of the Hsp90 molecular chaperone are showing considerable promise as potential molecular therapeutic agents for the treatment of cancer. Here we describe novel 2-aminothieno[2,3-d]pyrimidine ATP competitive Hsp90 inhibitors, which were designed by combining structural elements of dist...
  13. Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas

    Bioorganic & Medicinal Chemistry Letters 19(15):4241 (2009)

  14. Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.

    Bioorganic & Medicinal Chemistry Letters 19(15):4241 (2009) PMID 19515560

    We report the discovery of a novel, chiral azetidine urea inhibitor of Fatty Acid Amide Hydrolase (FAAH,) and describe the surprising species selectivity of VER-156084 versus rat and human FAAH and also hCB1.
  15. An unusual cause of syncope.

    BMJ Case Reports 2009 (2009) PMID 22171228 PMCID PMC3027396

    We present an unusual cause of recurrent syncope in a man in his 50s. He worked as a metallurgist and suffered syncopal events in his poorly ventilated workshop. A detailed history revealed that he used several solvents and chemicals at work and often kept workplace windows closed; he also smoke...
  16. The effect of linkage on limits to artificial selection.

    PMID 18976519

  17. Inbreeding in artificial selection programmes.

    PMID 18976515

  18. Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.

    Bioorganic & Medicinal Chemistry Letters 16(5):1353 (2006) PMID 16325401

    Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One example ...
  19. Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: Protein structure-guided design and SAR

    Bioorganic & Medicinal Chemistry Letters 16(5):1353 (2006)

    Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3β (GSK-3β). One example h...
  20. An audit of Chlamydia trachomatis screening in colposcopy--Hartlepool experience.

    International Journal of STD & AIDS 16(7):500 (2005) PMID 16004631

    This study aims to detect the prevalence of Chlamydia trachomatis in women attending the colposcopy clinic. The aim of the study is to evaluate whether routine screening for C. trachomatis should be continued as part of the colposcopy examination. All new patients attending the colposcopy clinic...