Publications by authors named "Mitch Brenner"
The utility of hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitors as a therapeutic means of treating patients suffering from anaemia has been demonstrated for various clinical settings. However, besides this intended use, HIF stabilizers can be the subject of misuse in amateur and elite sports due to their erythropoietic properties, as recently proven by several cases of adverse analytical findings in doping control testing. Consequently, to allow for adequate and comprehensive test methods, knowledge of the drug candidates' metabolism and analytical options enabling appropriate detection windows in sports drug testing samples (i.
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- Researchers developed non-peptidic inhibitors for procollagen C-proteinase (PCP) using substrate leads as a foundation.
- The most effective compounds identified were N-substituted aryl sulfonamide hydroxamates, showcasing strong potency and selectivity.
- Specifically, compounds 89 and 60 exhibited impressive IC(50) values of 10 and 80 nM against PCP and demonstrated excellent selectivity over certain matrix metalloproteinases (MMPs) while being effective in cell-based assays for collagen deposition.
Cooperative interaction of CTGF and TGF-β in animal models of fibrotic disease.
Fibrogenesis Tissue Repair
February 2011
Background: Connective tissue growth factor (CTGF) is widely thought to promote the development of fibrosis in collaboration with transforming growth factor (TGF)-β; however, most of the evidence for its involvement comes from correlative and culture-based studies. In this study, the importance of CTGF in tissue fibrosis was directly examined in three murine models of fibrotic disease: a novel model of multiorgan fibrosis induced by repeated intraperitoneal injections of CTGF and TGF-β2; the unilateral ureteral obstruction (UUO) renal fibrosis model; and an intratracheal bleomycin instillation model of pulmonary fibrosis.
Results: Intraperitoneal coadministration of CTGF and TGF-β2 elicited a profound fibrotic response that was inhibited by the human anti-CTGF antibody FG-3019, as indicated by the ability of FG-3019 to ameliorate the histologic signs of fibrosis and reduce the otherwise increased hydroxyproline:proline (Hyp:Pro) ratios by 25% in kidney (P < 0.