6345-43-3Relevant articles and documents
METHODS OF TREATING CANCER
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Paragraph 00424, (2020/06/10)
The present disclosure relates to methods of treating cancer in a patient using a combination of an inhibitor of an immune checkpoint protein and an indole compound or its phosphate derivative.
Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation
Hugenberg, Verena,Wagner, Stefan,Kopka, Klaus,Sch?fers, Michael,Schuit, Robert C.,Windhorst, Albert D.,Hermann, Sven
, p. 307 - 321 (2017/04/26)
The noninvasive imaging of MMP activity in vivo could have a high impact in basic research as well as in clinical applications. This approach can be established using radiolabeled MMP inhibitors (MMPIs) as tracers for the detection of activated MMPs by means of PET. However, the complexity of diseases associated with dysregulated MMP expression necessitates the imaging of distinct MMPs or MMP subgroups to distinguish their individual role in specific diseases. To this end, selective and potent MMP-13 inhibitors based on a N,N′-bis(benzyl)pyrimidine-4,6-dicarboxamide core have been synthesized and successfully radiolabeled with carbon-11, fluorine-18, and gallium-68. Selected radiolabeled candidates were evaluated in vitro and in vivo regarding their pharmacokinetic properties and metabolic stability.
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
Rose, Nathan R.,Ng, Stanley S.,Mecinovi?, Jasmin,Liénard, Beno?t M. R.,Bello, Simon H.,Sun, Zhe,McDonough, Michael A.,Oppermann, Udo,Schofield, Christopher J.
supporting information; experimental part, p. 7053 - 7056 (2009/11/30)
The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling.