2020
Hydroxamate-Based Selective Macrophage Elastase (MMP-12) Inhibitors and Radiotracers for Molecular Imaging
Gona K, Toczek J, Ye Y, Sanzida N, Golbazi A, Boodagh P, Salarian M, Jung JJ, Rajendran S, Kukreja G, Wu TL, Devel L, Sadeghi MM. Hydroxamate-Based Selective Macrophage Elastase (MMP-12) Inhibitors and Radiotracers for Molecular Imaging. Journal Of Medicinal Chemistry 2020, 63: 15037-15049. PMID: 33206510, PMCID: PMC8010999, DOI: 10.1021/acs.jmedchem.0c01514.Peer-Reviewed Original ResearchConceptsAbdominal aortic aneurysmMMP-12 inhibitorsSelective MMP-12 inhibitorMurine abdominal aortic aneurysmsRadiochemical stabilityFast blood clearanceMolecular imagingAortic aneurysmAAA progressionMMP-12Blood clearanceUpregulated MMPsAortic regionElastase inhibitorLead tracerNovel familyRupture riskMacrophage elastaseInhibitorsSelectivitySpecific bindingSynthesisVivo competitionImaging
2019
Novel Matrix Metalloproteinase 12 Selective Radiotracers for Vascular Molecular Imaging
Toczek J, Bordenave T, Gona K, Kim HY, Beau F, Georgiadis D, Correia I, Ye Y, Razavian M, Jung J, Lequin O, Dive V, Sadeghi MM, Devel L. Novel Matrix Metalloproteinase 12 Selective Radiotracers for Vascular Molecular Imaging. Journal Of Medicinal Chemistry 2019, 62: 9743-9752. PMID: 31603669, PMCID: PMC7054845, DOI: 10.1021/acs.jmedchem.9b01186.Peer-Reviewed Original ResearchConceptsAbdominal aortic aneurysmVascular molecular imagingMurine abdominal aortic aneurysmsMMP-12 gene expressionMatrix metalloproteinase-12Aortic aneurysmInflammatory diseasesAdjacent aortaH postinjectionMMP-12Blood clearanceMetalloproteinase-12Selective radiotracerFurther evaluationMMP-12 inhibitorsMouse bloodHigh uptakeAortaDiseaseMolecular imagingHuman metalloproteasesRadiotracer