Cox-2-Selective Inhibitors: The New Super Aspirins
... might be sufficient to achieve the therapeutic benefits of NSAID therapy and, conversely, that the indiscriminate inhibition of Cox-1 likely resulted in the side effects commonly associated with NSAIDs stimulated an intense and highly competitive race to identify compounds that would selectively inh ...
... might be sufficient to achieve the therapeutic benefits of NSAID therapy and, conversely, that the indiscriminate inhibition of Cox-1 likely resulted in the side effects commonly associated with NSAIDs stimulated an intense and highly competitive race to identify compounds that would selectively inh ...
Therapeutic Agents for Alzheimer`s Disease
... AChE inhibitors. In terms of structural information for the design of new inhibitors, X-ray analysis of AChE has been most helpful, as shown in (Fig. 1); AChE has a hydrophobic gorge or pocket which contains the catalytic triad (GLU327, HIS440, SER200), and it also has a peripheral anionic site on t ...
... AChE inhibitors. In terms of structural information for the design of new inhibitors, X-ray analysis of AChE has been most helpful, as shown in (Fig. 1); AChE has a hydrophobic gorge or pocket which contains the catalytic triad (GLU327, HIS440, SER200), and it also has a peripheral anionic site on t ...
Covalent inhibitors in drug discovery: from accidental discoveries to
... Most small-molecule drugs are designed to interact with their biological targets under equilibrium binding conditions, where the desired drug–protein interaction is a rapid and reversible process. The ratio of a drug–protein complex to unbound drug and free protein is dependent on the intrinsic affi ...
... Most small-molecule drugs are designed to interact with their biological targets under equilibrium binding conditions, where the desired drug–protein interaction is a rapid and reversible process. The ratio of a drug–protein complex to unbound drug and free protein is dependent on the intrinsic affi ...
Case Report - Thalidomide and hyperkalemia
... proliferation In some tumor types, such as RCC and certain lymphomas, mTOR as key role in tumor cell proliferation and angiogenesis Temsirolimus and everolimus are approved as monotherapy in advanced RCC ...
... proliferation In some tumor types, such as RCC and certain lymphomas, mTOR as key role in tumor cell proliferation and angiogenesis Temsirolimus and everolimus are approved as monotherapy in advanced RCC ...
Discovery of PF-04457845: A Highly Potent
... central tissues, an irreversible inhibitor may be beneficial because the nonequilibrium binding mechanism limits the competition with high endogenous substrate concentrations leading to increased biochemical efficiency.24 Furthermore, the pharmacodynamic effect resulting from covalent inhibition oft ...
... central tissues, an irreversible inhibitor may be beneficial because the nonequilibrium binding mechanism limits the competition with high endogenous substrate concentrations leading to increased biochemical efficiency.24 Furthermore, the pharmacodynamic effect resulting from covalent inhibition oft ...
(HMG-CoA) REDUCTASE INHIBITORS ON THE CYP3A4
... observed increase in clinical situations (Ishigami et al., 2001). However, as far as the water soluble pravastatin was concerned, when administered in the active acid form, there was no evidence suggesting any drug interaction with itraconazole either in clinical situations (Neuvonen and Jalava, 199 ...
... observed increase in clinical situations (Ishigami et al., 2001). However, as far as the water soluble pravastatin was concerned, when administered in the active acid form, there was no evidence suggesting any drug interaction with itraconazole either in clinical situations (Neuvonen and Jalava, 199 ...
Nonsteroidal anti-inflammatory drugs
... ‡ In clinical practice acetylsalicylic acid is used in children with inflammatory diseases of all ages, but it is not recommended in cases with suspected viral etiology because of the increased risk of Reye syndrome. § Indomethacin is used to treat persistent ductus arteriosus in newborns and to con ...
... ‡ In clinical practice acetylsalicylic acid is used in children with inflammatory diseases of all ages, but it is not recommended in cases with suspected viral etiology because of the increased risk of Reye syndrome. § Indomethacin is used to treat persistent ductus arteriosus in newborns and to con ...
Antidiabetic drugs
... of glucose (SGLT2 inhibitors): p.o. •Canagliflozin blocks in renal proximal tubule sodium / glucose co-transporter protein 2 (SGLT2), which re-absorbed 90% of the filtrated glucose. The result is increased glucosuria and plasma glucose levels are lowered. ...
... of glucose (SGLT2 inhibitors): p.o. •Canagliflozin blocks in renal proximal tubule sodium / glucose co-transporter protein 2 (SGLT2), which re-absorbed 90% of the filtrated glucose. The result is increased glucosuria and plasma glucose levels are lowered. ...
Fatty acid amide hydrolase - The Scripps Research Institute
... glycerol (2-AG) as a second endocannabinoid [5,6] has fortified the hypothesis that cannabinoid (CB) receptors are part of the sub-class of GPCRs that recognize lipids as their natural ligands. Consistent with this notion, based on primary structural alignment of the GPCR superfamily, CB receptors a ...
... glycerol (2-AG) as a second endocannabinoid [5,6] has fortified the hypothesis that cannabinoid (CB) receptors are part of the sub-class of GPCRs that recognize lipids as their natural ligands. Consistent with this notion, based on primary structural alignment of the GPCR superfamily, CB receptors a ...
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... Sulfa drugs are an important class of synthetic bacteriostatic antibiotics still used today for the treatment of bacterial infections and those caused by other microorganisms, sulfa drugs achieve this bacteriostatic action by inhibiting the synthesis of folic acid in bacteria. The current study has ...
... Sulfa drugs are an important class of synthetic bacteriostatic antibiotics still used today for the treatment of bacterial infections and those caused by other microorganisms, sulfa drugs achieve this bacteriostatic action by inhibiting the synthesis of folic acid in bacteria. The current study has ...
Structure-based design of enzyme inhibitors and receptor ligands
... peptide with a Pro-Arg sequence and a β-diketone moiety (Figure 3), which readily forms a hemiketal with the hydroxyl group of the catalytically active Ser-195 of thrombin [62]. A first lead structure, 13 (Figure 3) [24,63], including several of these structural elements in a much simpler molecule, ...
... peptide with a Pro-Arg sequence and a β-diketone moiety (Figure 3), which readily forms a hemiketal with the hydroxyl group of the catalytically active Ser-195 of thrombin [62]. A first lead structure, 13 (Figure 3) [24,63], including several of these structural elements in a much simpler molecule, ...
Peptidomimetic Therapeutic Agents Targeting the
... majority of infected individuals (>80%) can remain asymptomatic for as long as 20 years and some (∼20%) are even able to clear the virus. However, those that become chronically infected usually progress to end-stage liver diseases, and some (∼2-4%) eventually develop hepatocellular carcinomas. HCV/H ...
... majority of infected individuals (>80%) can remain asymptomatic for as long as 20 years and some (∼20%) are even able to clear the virus. However, those that become chronically infected usually progress to end-stage liver diseases, and some (∼2-4%) eventually develop hepatocellular carcinomas. HCV/H ...