4-n-butylresorcinol inhibits melanogenesis by enhancing proteolytic degradation of tyrosinase as well as competitive binding to tyrosinase. These findings will help to develop new, effective and safe chemicals for the treatment of hyperpigmentation disorders.
Transglutaminase 2 (TG2) is a Ca 2+ -dependent enzyme, which regulates various cellular processes by catalyzing protein crosslinking or polyamination. Intracellular TG2 is activated and inhibited by Ca 2+ and GTP binding, respectively. Although aberrant TG2 activation has been implicated in the pathogenesis of diverse diseases, including cancer and degenerative and fibrotic diseases, the structural basis for the regulation of TG2 by Ca 2+ and GTP binding is not fully understood.Here, we produced and analyzed a Ca 2+ -containing TG2 crystal, and identified two glutamate residues, E437 and E539, as Ca 2+ -binding sites. The enzymatic analysis of the mutants revealed that Ca 2+ binding to these sites is required for the transamidase activity of TG2. Interestingly, we found that magnesium (Mg 2+ ) competitively binds to the E437 and E539 residues. The Mg 2+ binding to these allosteric sites enhances the GTP binding/hydrolysis activity but inhibits transamidase activity. Furthermore, HEK293 cells transfected with mutant TG2 exhibited higher transamidase activity than cells with wild-type TG2. Cells with wild-type TG2 showed an increase in transamidase activity under Mg 2+ -depleted conditions, whereas cells with mutant TG2 were unaffected. These results indicate that E437 and E539 are Ca 2+ -binding sites contributing to the reciprocal regulation of transamidase and GTP binding/hydrolysis activities of TG2 through competitive Mg 2+ binding.
In South Korea, the evaluation criteria for installing shading devices are defined by regulations, but the standards of design methods are not clearly established. The installation of shading devices has become mandatory for some public buildings due to revised regulations. Therefore, a design of horizontal shading device is required, and indoor environmental problems which may occur due to their installation should also be taken into consideration. This research aimed to propose a design which takes into account the energy consumption which may occur if the horizontal shading device is installed and suggests an improved design method of horizontal shading devices when they are installed. Consequently, it was confirmed that as the protrusion of the horizontal shading device becomes longer, the incoming daylight is reduced and the indoor intensity of illumination becomes lower, and thus more lighting energy may be consumed in a room where the shading device is installed than in the one where it is not. Therefore, annual energy consumption was calculated by applying the lighting control and it was found that the total energy consumption decreased by the reduction of air-conditioning and fans and lighting energy consumption.
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