... to determine if BRAF is relevant for human heart failure, whether BRAF promotes cardiomyocyte hypertrophy, and if Type 1 RAF inhibitors developed for cancer (that paradoxically activate ERK1/2 at low concentrations: the ‘RAF paradox') may have the same effect. BRAF was up-regulated in heart samples from...

...). This modification can lead to transcriptional activation or repression of cancer-related genes. To date, a number of inhibitors, based on natural peptide substrates, have been developed for the PRMT family of enzymes. However, because peptides are easily degraded in vivo , the utility of these inhibitors...

...: Sameh S. M. Soliman and Rania Hamdy. 22 4 2020 6 6 2020 11 6 2020 12 6 2020 © 2020 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society 2020 fungal melanin human melanin inhibitors phagocytosis Rhizopus delemar tyrosinase...

..., the therapeutic potential of suppressing the nucleoside phosphorylase activity in either family of enzymes has motivated efforts to design potent inhibitors. Several research groups have synthesized a variety of nucleoside phosphorylase inhibitors that are at various stages of preclinical and clinical evaluation...

... investigated the mode of action of these compounds and we found that: (i) several 4´-thio-2´-deoxyuridines are phosphorylated to the mono- and di-phosphates by HSV-1 thymidine kinase (TK) more efficiently than their corresponding 4´-oxy counterpart; (ii) both are inhibitors of cellular thymidylate synthase...

... 1999 1999 angiostatin inhibitors interleukin-6 plasmin serine proteinase Biochem. J. (1999) 339, 705 712 (Printed in Great Britain) 705 Extrahepatic synthesis of plasminogen in the human cornea is up-regulated by interleukins-1a and -1b Sally S. TWINING1, Patricia M. WILSON and Chatri...

... behaviour for each isoform. Weakly binding inhibitors show variable behaviour in enzyme assays, with apparent inhibitory activity being markedly influenced by experimental conditions; determination of kinetic constants with this class is unreliable and IC 50 values are strongly dependent on assay conditions...