Moreover, the desired linkage (ester vs. amide) may be selected to improve stability in vivo. Importantly, an appropriate selection of pro-moiety (targeting ligand) may promote drug specificity and selectivity. In this review article, an attempt has been made to summarize lipophilic prodrugs ...
The advanced drug delivery systems are of valuable role in controlling the drug release rate, preserving the drug concentration within the recommended limits, enhancing the site-specificity, and improving patient compliance [15,16]. Several products, including zeolite, clay minerals (bentonite, ...
Moreover, the fact that C-123 displayed stronger dependence than idarubicin and DMSO on the total cell number suggests that this drug has better pharmacological properties (e.g., specificity, affinity) than idarubicin and DMSO (Figure 5B, solid line). The lack of consistent EC50 values in the...
Current drug optimization overly emphasizes potency/specificity using structure‒activity-relationship (SAR) but overlooks tissue exposure/selectivity in disease/normal tissues using structure‒tissue exposure/selectivity–relationship (STR), which may mislead the drug candidate selection and impact the ...
MYC/MAX control ERK signaling and pluripotency by regulation of dual-specificity phosphatases 2 and 7. Genes Dev. 27, 725–733 (2013). Article CAS PubMed PubMed Central Google Scholar Ariza, A. et al. Study of protein haptenation by amoxicillin through the use of a biotinylated antibiotic...
transcription [47]. Despite its extensive application in gene therapy, several challenges are associated with its application as a therapeutic gene transfer vector. Like other viral vectors, low production yield, target specificity and purity are far reaching milestones that need to be addressed [48]...
Oligosaccharide specificity of galectins: a search by frontal affinity chromatography. Biochim. Biophys. Acta 1572, 1–23 (2002). Google Scholar Blixt, O. et al. Printed covalent glycan array for ligand profiling of diverse glycan binding proteins. Proc. Natl Acad. Sci. USA 101, 17033 (...
and surgery. However, these treatments only address the symptoms and often elicit adverse side effects, potentially in part due to non-specificity. There is an urgent need to identify effective pharmacological treatments for cerebral edema. Currently, ion channels represent the third-largest target cla...
[3]. Unfortunately, the concept of lineage-specificity does not apply to solid tumors, for which antigens expressed are mainly “tumor-associated” instead of “tumor-specific”, i.e., expressed on tumor cells but also on normal cells (weakly or limited to a given tissue type). This ...
The high degree of sequence and pocket similarities between different subtypes demands for novel ligands with superior specificity and selectivity. In this regard, allosteric and biased modulators may offer additional pharmacological benefits. Subtype selectivity...