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Assessment of Quercetin Isolated from Enicostemma Littorale Against Few Cancer Targets: An in Silico Approach
Published in A. K. Haghi, Ana Cristina Faria Ribeiro, Lionello Pogliani, Devrim Balköse, Francisco Torrens, Omari V. Mukbaniani, Applied Chemistry and Chemical Engineering, 2017
The mammalian target of rapamycin (mTOR) also known as mechanistic target of rapamycin or FK506 binding protein 12-rapamycin associated protein 1 (FRAP1) is a protein encoded by FRAP1 gene. mTOR is a serine/ threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. mTOR belongs to the phosphatidylinositol 3-kinase-related kinase protein family. mTOR integrates the input from upstream pathways, including insulin, growth factors (such as IGF-1 and IGF-2), and amino acids. mTOR also senses cellular nutrient and energy levels and redox status. The mTOR pathway is dysregulated in human diseases, especially in certain cancers. Rapamycin is a bacterial product that can inhibit mTOR by associating with its intracellular receptor FKBP12. The FKBP12-rapamycin complex binds directly to the FKBP12-rapamycin binding (FRB) domain of mTOR. mTOR is the catalytic subunit of two molecular complexes.4
The EluNIRTM Ridaforolimus Eluting Coronary Stent System
Published in Expert Review of Medical Devices, 2019
Panagiotis Savvoulidis, Gidon Perlman, Rodrigo Bagur
The EluNIR™ is the first DES with an elastomeric coating. The stent is coated with a proprietary durable polymer matrix, composed of poly n-butyl methacrylate (PBMA) and CarboSil® (DSM Biomedical, Exton, PA, USA) which is an elastomeric, biocompatible, silicone-modified polyurethane. The elastomeric coating minimizes coating irregularities and polymer damage such as peeling, cracking, and flaking, thereby allowing uniform elution of antiproliferative drug and potentially curbing the probability of inflammatory processes associated with ISR and ST (Figure 1). The coating contains ridaforolimus at a concentration of 1.1 μg/mm2. Ridaforolimus is a high-therapeutic index member of the ‘limus’ family of drugs. It is a non-prodrug analog of Rapamycin (Sirolimus), a macrocyclic lactone produced by Streptomyces hygroscopicus. Like Rapamycin, ridaforolimus permeates the cell membrane, binds to cytosolic FKBP12 and then to mTOR, a P13K-related protein kinase, which acts as a central regulator of protein synthesis, cell proliferation, cell cycle progression, and cell survival. These effects are attributable to the inhibition of the multiple downstream effects of mTOR’s activity: synthesis of components required for macromolecular synthesis (such as ribosomes), cell size increase, and progression through the G1 phase of the cell cycle. Preclinical data suggest that by 90 days, nearly 90% of the drug was released and by 180 days >95% of the drug is eluted (Figure 2). Unlike previous DES, however, an initial peak (burst) concentration followed by diffusion does not occur. Rather, persistently low drug concentrations are measured in the surrounding vascular tissue for 3 months [24].