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Nail Product Rheology
Published in Laba Dennis, Rheological Proper ties of Cosmetics and Toiletries, 2017
A formulation for a gelled nail polish remover (32) is based on hydroxypropyl cellulose acetate used with acetone, ethyl acetate, or acetone/water bases. Other suggested thickeners include ethyl hydroxy-ethyl cellulose, which requires a higher use level, synthetic polymers such as vinyl ether copolymers, and silicas. Another transparent gelled remover is based on the use of a carbonate, such as propylene carbonate thickened by hydroxypropyl cellulose (33). As the hydroxypropyl cellulose requires some water to form a gel, the formulator included l,3-dimethyl-2-imidazolidinone to accommodate water in the formula.
Modifications of Cellular Radiation Damage
Published in Kedar N. Prasad, Handbook of RADIOBIOLOGY, 2020
In 1972, it was reported12 for the first time that prostaglandin E1 (PGE1, a stimulator of adenylate cyclase) and 4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone (R020-1724, an inhibitor of cyclic nucleotide phosphodiesterase) increased the survival of X-irradiated Chinese hamster ovary (CHOK1) cells by about twofold, provided they were given before irradiation (Table 5.1). Both PGE1 and R020-1724 were ineffective when given after irradiation. Based on this study, it was postulated that the intracellular level of cAMP may be inversely related to the radiosensitivity of mammalian cells.12 Although the intracellular level of cAMP was not measured in the initial study,12 other investigators have shown that the level of cAMP in CHO cells increases after treatment with PGE1 and inhibitors of cyclic nucleotide phosphodiesterase.13 The basic observation on the radioprotective role of cAMP has been confirmed and extended by several investigators. For example, it was shown that cAMP-stimulating agents, when given before X-irradiation, increased the survival of irradiated Chinese hamster V-7914-15 and thymocyte16 cells in culture. It was also reported that cAMP-stimulating agents reduced X-ray-induced mitotic delay in human kidney T cells17 and in S-180 ascites tumor cells.18 Again, most of these studies did not assay the level of cAMP in the cells before irradiation. It was further suggested14 that changes in cAMP during the cell cycle may be one of the important factors responsible for the variation in radiosensitivity as a function of stages of cell cycle. In one study,15 it was shown that cells with an increased level of cAMP became more sensitive to irradiation at higher radiation doses. The exact reasons for this are unknown.
Therapeutic targets for enterovirus infections
Published in Expert Opinion on Therapeutic Targets, 2020
Mira Laajala, Dhanik Reshamwala, Varpu Marjomäki
Structural and docking studies complement the in vitro assays in understanding the interaction between the potential antiviral compounds and the target. In addition, they also help to understand why some capsid binders are better at strongly inhibiting the virus compared to others. Moreover, structural and docking studies are useful tools in studying the interactions between the viral capsid and capsid binders analogues to design more effective antivirals against enteroviruses. Tijsma and his colleagues used molecular docking studies to report that vapendavir and pirodavir showed stronger interactions with the EV-A71 capsid in the pocket region whereas pleconaril was unable to reach that deep in the virus pocket, thus explaining its poor antiviral activity against EV-A71 [29]. De Colibus et al. synthesized imidazolidinones using pleconaril backbone/skeleton and performed high resolution structural and in silico studies in addition to in vitro assays to understand the antiviral mechanism of imidazolidinone-based compounds [131]. Abdelnabi et al. found a set of amino acid residues in the viral capsid critical for the anti-viral activity of compound 17 (a benzene sulfonamide derivative), by studying cryo-EM structural data along with the in vitro analysis which helped them to propose the antiviral mechanism of the compound associated with a novel interprotomer pocket. Moreover, their computational studies suggested that this interprotomer pocket binding the compound was conserved across enterovirus species including RV-C and EV-A [36].
Androgen receptor modulators: a review of recent patents and reports (2012-2018)
Published in Expert Opinion on Therapeutic Patents, 2019
Shinya Fujii, Hiroyuki Kagechika
Novartis reported spirohydantoin derivatives as SARMs. These compounds (see examples in Figure 9) [65] exhibited potent AR agonistic activity in reporter gene assay using the mouse muscle myoblast cell line C2C12. Novartis also developed pyrazoline derivatives as SARMs. Compounds 39 and 40 exhibited AR agonistic activity in C2C12 cells, and induced a dose-dependent increase in the weight of levator ani muscles compared to prostate in a rat in vivo model. These SARMs have potential utility for the treatment or prevention of muscle-wasting diseases, osteoporosis, sarcopenia, frailty and cancer cachexia [66]. Novartis also patented cyclic urea derivatives as AR antagonists. The claimed compounds bear a bicyclic 2-imidazolidinone structure instead of the hydantoin core of enzalutamide. The biological activity of these compounds was assessed in terms of antiproliferative activity toward VCaP cells [67], and the most potent compounds exhibited anti-androgenic activity with IC50 values of around 40 nM [68].
N-terminal α-amino group modification of antibodies using a site-selective click chemistry method
Published in mAbs, 2018
De-zhi Li, Bing-nan Han, Rui Wei, Gui-yang Yao, Zhizhen Chen, Jie Liu, Terence C.W. Poon, Wu Su, Zhongyu Zhu, Dimiter S. Dimitrov, Qi Zhao
The N-terminal α-amine is a crucial site of protein post-translational modification that affects protein activation, conversion, and degradation.22 The α-amine has gained attention for in vitro protein modification. In addition, N-terminal serines or threonines can be oxidized to aldehydes and react with amines and alkoxyamine groups.23-26 Recent studies showed that the α-amine of proteins can be modified through ketene without interfering with side chains.27 Nevertheless, the labile property of ketene makes its synthesis difficult. A recent study showed that 2-pyridinecarboxyaldehyde (2-PCA) formed a stable imidazolidinone with N-terminal amines of protein under mild conditions.28 Although the above-mentioned methods are of great interest, they have several limitations, including difficulties in chemical synthesis, unwanted byproducts, and low reaction efficiency. Therefore, a simple and mild method for coupling a small molecule onto a natural amino acid of peptides or proteins with high selectivity is needed.