0000000000808307

AUTHOR

Ilse Daehn

0000-0001-9915-5376

showing 1 related works from this author

Designer Thiopurine-analogues for Optimised Immunosuppression in Inflammatory Bowel Diseases.

2015

Background and Aims: The clinical use of azathioprine and 6-mercaptopurine is limited by their delayed onset of action and potential side effects such as myelosuppression and hepatotoxicity. As these drugs specifically target the Vav1/Rac1 signalling pathway in T lamina propria lymphocytes via their metabolite 6-thio-GTP, we studied expression and optimised suppression of this pathway in inflammatory bowel diseases [IBD]. Methods: Rac1 and Vav1 expressions were analysed in mucosal immune cells in IBD patients. Targeted molecular modelling of the 6-thio-GTP molecule was performed to optimise Rac1 blockade; 44 modified designer thiopurine-analogues were tested for apoptosis induction, potenti…

0301 basic medicinerac1 GTP-Binding Proteinmedicine.medical_treatmentT-LymphocytesAzathioprineApoptosisInflammatory bowel diseaseDesigner Drugs03 medical and health sciences0302 clinical medicineImmune systemIntestinal mucosamedicineHumansIntestinal MucosaProto-Oncogene Proteins c-vavLamina propriaThiopurine methyltransferasebiologybusiness.industryMercaptopurineGastroenterologyImmunosuppressionGeneral Medicinemedicine.diseaseInflammatory Bowel Diseases030104 developmental biologymedicine.anatomical_structureApoptosisCase-Control StudiesDrug DesignImmunologybiology.protein030211 gastroenterology & hepatologybusinessBiomarkersImmunosuppressive Agentsmedicine.drugSignal TransductionJournal of Crohn'scolitis
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