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All these inhibitors, used at doses described to be selective for the indicated kinase, were verified for efficiency in inhibiting the corresponding kinase phosphorylation by immunoblot or flow cytometry.
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As mitochondrial Bax/Bak release pores were described to be rather non-selective [ 13], spatial MOMP waves can also be expected for other pro-apoptotic proteins besides cyt-c which are released from mitochondria, such as the XIAP antagonists Smac/DIABLO and HtrA2/Omi [ 14- 16].
I need to be selective on how I describe myself.
2-Cyanopyrrolidines were described as selective cathepsin L inhibitors, the most potent compound (51, Ki=5.3 µmol/L, Fig. 8) was reported to be selective against cathepsin B. The 1,3,5-triazine-2-carbonitrile 1,3,5-triazine-2-carbonitrile 1,3,5-triazine-2-carbonitrile 1,3,5-triazine-2-carbonitrileg potent inhibitorepresents 52 (Fig. 8; Ki=9 nmol/L, rhodesanothernmol/L, capproach L).
Crucially, none of the inhibitors described to date is selective for binding BRD4 bromodomains over those of its paralogs BRD2 and BRD3.
Eleven PDE families are described to date, and selective inhibitors of some PDEs families are currently used in clinic for treating cardiovascular disorders, erectile dysfunction, and pulmonary hypertension.
It is noteworthy that all substrate selective GSIs described to date are based on sulfonamide pharmacophore ([ 47, 79, 85- 87], and this report).
CD38 ligation has been described to result in selective induction of CD73 expression [37], which in turn is critical for Treg-mediated suppression [11].
The ESCRT machinery has recently been described to contribute to selective micro-autophagy on late endosomes in mammalian cells (Sahu et al., 2011).
We have changed the text in the Discussion accordingly: "Interestingly, the ESCRT machinery has recently been described to contribute to selective micro-autophagy on late endosomes in mammalian cells (Sahu et al., 2011).
Given that inhibition of VEGF pathway has been described to prevent BAT/browning activation12,13,14, selective ablation (pharmacologically or genetically) of VEGF in Bmp8b TG mice may provide further support to this conclusions.
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