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  • characterization
  • We here show for the first time the pharmacological characterization of BAY-876, comprising inhibition of glucose-uptake, anti-proliferative activity in vitro, and anti-tumor efficacy in vivo in models of different tumor indications in monotherapy as well as first results on the combinability of BAY-876. (aacrjournals.org)
  • insulin
  • However, it is important that regimens of insulin therapy are designed not only to aim at near-normalizing blood glucose, but also to minimize the risk of hypoglycemia. (diabetesjournals.org)
  • The goal of minimizing the risk of hypoglycemia while achieving good glycemic control is feasible as long as 1 ) a rational plan of insulin therapy is adopted, 2 ) blood glucose is properly monitored, 3 ) blood glucose targets are individualized, and 4 ) education programs are widely implemented. (diabetesjournals.org)
  • In the fasting state, this is due to the continuous release of insulin from the pancreas, which results in steady plasma insulin, thus restraining hepatic glucose production and thereby preventing fasting hyperglycemia. (diabetesjournals.org)
  • Currently we are studying the acute effects of HIV protease inhibitors on peripheral glucose disposal, hepatic glucose production, and insulin secretion using both in vitro and in vivo model systems. (wustl.edu)
  • HIV protease inhibitors acutely impair glucose-stimulated insulin release. (wustl.edu)
  • 2 Under normal conditions, fluctuations in glucose and insulin levels are tightly regulated through feedback mechanisms that inhibit IR/IGF-1R signaling and ensure that metabolic homeostasis is maintained. (pubmedcentralcanada.ca)
  • 1 The mechanism by which metformin acts to reduce cancer risk is thought to be through its ability to lower blood glucose and insulin levels and restore metabolic homeostasis. (pubmedcentralcanada.ca)
  • SGLT proteins cause the glucose reabsorption from the glomerular filtrate, independent of insulin. (wikipedia.org)
  • They work independently of insulin and can reduce glucose levels without causing hypoglycemia or weight gain. (wikipedia.org)
  • side of the plasma membrane
  • Following binding, and while the binding site is facing the same way, the carrier will capture or occlude (take in and retain) the substrate within its molecular structure and cause an internal translocation so that the opening in the protein now faces the other side of the plasma membrane. (wikipedia.org)
  • endoplasmic reticulum
  • Class II comprises: GLUT5 (SLC2A5), a fructose transporter in enterocytes GLUT7 - SLC2A7 - (SLC2A7), found in the small and large intestine, transporting glucose out of the endoplasmic reticulum GLUT9 - SLC2A9 - (SLC2A9) GLUT11 (SLC2A11) Class III comprises: GLUT6 (SLC2A6), GLUT8 (SLC2A8), GLUT10 (SLC2A10), GLUT12 (SLC2A12), and GLUT13, also H+/myoinositol transporter HMIT (SLC2A13), primarily expressed in brain. (wikipedia.org)
  • These membrane proteins were co-expressed with a fluorescent FRET (Förster resonance energy transfer) glucose sensor localized to the endoplasmic reticulum (ER). (wikipedia.org)
  • substrate
  • Transport is mediated via a series of conformation changes, switching between a conformation where the substrate-binding cavity is accessible from the outside, and a another conformation where it is accessible from the cytoplasm. (rcsb.org)
  • These two halves come together to form a pore for substrate transport, in GalP, the substrates are primarily galactose, glucose, and H+. (wikipedia.org)
  • These protein energetically drive transport utilizing the electrochemical gradient of the target substrate (uniporter), or act as a cotransporter where transport is coupled to the movement of a second substrate. (wikipedia.org)
  • While one substrate of particular biological importance is often used to name the transporter or family, there may also be co-transported or leaked ions or molecules. (wikipedia.org)
  • galactose
  • The galactose permease or GalP found in Escherichia coli is an integral membrane protein involved in the transport of monosaccharides, primarily hexoses, for utilization by E. coli in glycolysis and other metabolic and catabolic pathways (3,4). (wikipedia.org)
  • Glucose, galactose and other hexoses are transported by GalP by the use of the proton gradient produced by the electron transport chain and reversible ATPase (1). (wikipedia.org)
  • GalP can bind specifically to the hexoses with preferential binding of galactose and glucose through the pores in each monomer (2,3). (wikipedia.org)
  • The syndrome results in hepatomegaly secondary to glycogen accumulation, glucose and galactose intolerance, fasting hypoglycaemia, a characteristic proximal tubular nephropathy and severe short stature. (wikipedia.org)
  • inhibitor
  • The peptide oxybenzylcarbonyl-His-Phe-Phe- O -ethyl ester (zHFFe) was identified as a potent inhibitor of zero-trans glucose flux with a K i of 26 μM. (pubmedcentralcanada.ca)
  • Phlorizin was first isolated in 1835 and was subsequently found to be a potent but rather non-selective inhibitor of both SGLT-1 and SGLT-2 proteins. (wikipedia.org)
  • amino
  • 6 Metformin mediates its inhibitory function by activating the tumor suppressor LKB1 and its downstream target AMP-activated protein kinase (AMPK) and by inhibiting the RagGTPases that are essential for mTORC1 activation by amino acids. (pubmedcentralcanada.ca)
  • This is usually to accumulate high concentrations of molecules that a cell needs, such as glucose or amino acids. (wikipedia.org)
  • Proteins are made of amino acids arranged in a linear chain joined together by peptide bonds. (wikipedia.org)
  • GLUT2
  • It is associated with GLUT2, a glucose transport protein which, when functioning normally, allows glucose to exit several tissues, including the liver, nephrons, and enterocytes of the intestines, and enter the blood. (wikipedia.org)
  • In drug-treated diabetic pregnancies in which glucose levels in the woman are uncontrolled, neural tube and cardiac defects in the early-developing brain, spine, and heart depend upon functional GLUT2 carriers, and defects in the GLUT2 gene have been shown to be protective against such defects in rats. (wikipedia.org)
  • GLUT2 could reasonably be referred to as the "diabetic glucose transporter" or a "stress hyperglycemia glucose transporter. (wikipedia.org)
  • solutes
  • In contrast, a channel can be open to both environments at the same time, allowing the solutes it transports to diffuse without interruption. (wikipedia.org)
  • Solutes that are transported by the various SLC group members are extraordinarily diverse and include both charged and uncharged organic molecules as well as inorganic ions and the gas ammonia. (wikipedia.org)
  • The major facilitator superfamily (MFS) is a superfamily of membrane transport proteins that facilitate movement of small solutes across cell membranes in response to chemiosmotic gradients. (wikipedia.org)