Inhibiting its activity with CCR1 antagonists has been proved to be effective in preventing some diseases. A number of in vivo experiments have been carried out to shed light on the underlying mechanism of the interactions between the CCR1 and its ligands. However, their conclusions are still controversial. In this study, ligand-based computational drug design is applied as a new and effective way to study the structure-activity relationship
of CCR1 antagonists. Three-dimensional pharmacophore models were generated for CCR1 antagonists, using both HypoGen and HipHop algorithms in Catalyst software. Two optimal pharmacophore models were defined through careful qualification processes. Both of them have four features: one hydrogen-bond KPT-8602 cost acceptor, one positive ionable and two hydrophobic FK228 cost groups. Additional information was obtained through comparison between the two models. Our results can be valuable tools for the discovery and development
of specific, highly potent CCR1 antagonists. For Supplement material, please see the online version of the article.”
“Background Melasma is an acquired pigmentary disorder classically manifesting as symmetric hyperpigmented macules and patches on the face. It most commonly affects women of reproductive age with darker skin tones but may also affect adolescents, older women, and men. Although its pathogenesis remains unclear, known risk factors include ultraviolet radiation, hormonal variations of pregnancy, thyroid disease, oral contraceptives, and antiseizure medications. Hydroquinone-containing topical agents are the current standard for melasma treatment, but concern about side effects and long-term safety has spurred efforts to develop alternative treatment options. Objectives To review recent advances in melasma treatment. Materials and Methods MEDLINE was searched from 2006 to the present for randomized controlled trials (RCTs) of melasma
treatments. Results Nineteen published RCTs were found covering interventions such as topical therapies, chemical peels, and electromagnetic devices. see more The outcomes of the studies were summarized into tabular form for easy reference and comparison. Conclusions Although melasma is difficult to treat, novel therapeutic modalities have emerged. Further RCT need to be performed to better assess the safety and efficacy of these novel treatment modalities, especially for the long-term maintenance of melasma.”
“The charging phenomenon in the insulating dielectrics often occurs in the radiative environments such as in the outer space and in the nuclear reactor. Both surface charging and bulk charging have various influences on the dielectric properties. Understanding electrical properties of e-beam irradiated dielectrics is of great significance in order to maintain the stability and reliability of the related operating system.