Darren McKerrecher

Summary

Affiliation: AstraZeneca R and D

Publications

  1. ncbi request reprint Discovery, synthesis and biological evaluation of novel glucokinase activators
    Darren McKerrecher
    Cardiovascular and Gastrointestinal Research Area, AstraZeneca UK, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 15:2103-6. 2005
  2. ncbi request reprint Design of a potent, soluble glucokinase activator with excellent in vivo efficacy
    Darren McKerrecher
    Cardiovascular and Gastrointestinal Research Area, AstraZeneca R and D, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 16:2705-9. 2006
  3. ncbi request reprint Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation
    James S Scott
    Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom
    J Med Chem 55:5361-79. 2012
  4. ncbi request reprint Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life
    Kurt G Pike
    Cardiovascular and Gastrointestinal Research Area, AstraZeneca R and D, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 21:3467-70. 2011
  5. ncbi request reprint Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human
    James S Scott
    Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 23:3175-9. 2013
  6. ncbi request reprint Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists
    James S Scott
    Innovative Medicines Unit, AstraZeneca Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, U K
    J Med Chem 57:8984-98. 2014
  7. ncbi request reprint A chemistry wiki to facilitate and enhance compound design in drug discovery
    Graeme R Robb
    Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca R and D, UK
    Drug Discov Today 18:141-7. 2013
  8. ncbi request reprint Discovery, optimisation and in vivo evaluation of novel GPR119 agonists
    Katy J Brocklehurst
    Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 21:7310-6. 2011

Collaborators

  • Philip A Macfaul
  • Andrew G Leach
  • Clifford D Jones
  • Kurt G Pike
  • Graeme R Robb
  • Alan M Birch
  • James S Scott
  • Katy J Brocklehurst
  • Paul Schofield
  • Hayley S Brown
  • David S Clarke
  • David Laber
  • Kristin Goldberg
  • Joanne Teague
  • Sam D Groombridge
  • Anne Ertan
  • Per H Svensson
  • Julian A Hudson
  • Roger J Butlin
  • Anders Broo
  • Ojvind Davidsson
  • Elizabeth A Martin
  • Suzanne S Bowker
  • Stefan Kavanagh
  • Alison Easter
  • Helen Coe
  • Pernilla Sörme
  • Adrian Pickup
  • Leanne Westgate
  • Matt J M Wood
  • Elizabeth E Kelly
  • Simon Poucher
  • Charles O'Donnell

Detail Information

Publications8

  1. ncbi request reprint Discovery, synthesis and biological evaluation of novel glucokinase activators
    Darren McKerrecher
    Cardiovascular and Gastrointestinal Research Area, AstraZeneca UK, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 15:2103-6. 2005
    ..The interplay between lipophilicity, potency and physical properties is discussed, and compound 22 highlighted as having a suitable balance. In vivo pharmacokinetic and acute efficacy studies on this compound are also presented...
  2. ncbi request reprint Design of a potent, soluble glucokinase activator with excellent in vivo efficacy
    Darren McKerrecher
    Cardiovascular and Gastrointestinal Research Area, AstraZeneca R and D, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 16:2705-9. 2006
    ....
  3. ncbi request reprint Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation
    James S Scott
    Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom
    J Med Chem 55:5361-79. 2012
    ..The compound was shown to be effective in wild-type but not knockout animals, confirming that the biological effects were due to GPR119 agonism...
  4. ncbi request reprint Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life
    Kurt G Pike
    Cardiovascular and Gastrointestinal Research Area, AstraZeneca R and D, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 21:3467-70. 2011
    ..GKA60 maintains an excellent balance of potency and physical properties whilst possessing a significantly different, but complimentary, pre-clinical pharmacokinetic profile compared with the previously disclosed compound GKA50...
  5. ncbi request reprint Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human
    James S Scott
    Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 23:3175-9. 2013
    ..This highlights the large effects on GPCR phamacology that can result from small structural changes in the ligand, together with inter-species differences between receptors...
  6. ncbi request reprint Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists
    James S Scott
    Innovative Medicines Unit, AstraZeneca Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, U K
    J Med Chem 57:8984-98. 2014
    ..Importantly, it was shown to be effective in wild-type (WT) but not GPR119 knockout (KO) animals, consistent with the pharmacology observed being due to agonism of GPR119. ..
  7. ncbi request reprint A chemistry wiki to facilitate and enhance compound design in drug discovery
    Graeme R Robb
    Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca R and D, UK
    Drug Discov Today 18:141-7. 2013
    ..Solutions to these problems were implemented, reducing the time taken from the initial idea stage to the generation of the synthesised compound by more than 50%...
  8. ncbi request reprint Discovery, optimisation and in vivo evaluation of novel GPR119 agonists
    Katy J Brocklehurst
    Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
    Bioorg Med Chem Lett 21:7310-6. 2011
    ..However, further profiling in a GPR119 knock-out (KO) mouse model revealed that the biological effects were not exclusively due to GPR119 agonism, highlighting the value of transgenic animals in drug discovery programs...