In vitro metabolism and drug-drug interaction potential of irosustat, a
... developed with these sites of metabolism blocked, thereby slowing metabolic clearance. A second possible consequence of drug metabolism is the formation of active metabolites (those having the desired activity to an extent similar to/or greater than the parent drug). In some of these cases, the drug ...
... developed with these sites of metabolism blocked, thereby slowing metabolic clearance. A second possible consequence of drug metabolism is the formation of active metabolites (those having the desired activity to an extent similar to/or greater than the parent drug). In some of these cases, the drug ...
Recent Advances Towards New Anti-Infective Agents that Inhibit
... enzyme-substrate linkage after breakage of the threonineglycine peptide bond and protonation of the leaving amine group (step 3). The thioacyl intermediate is long-lived and has been directly detected by mass spectrometry [41]. In the transpeptidation reaction, the amine group of the cell wall cross ...
... enzyme-substrate linkage after breakage of the threonineglycine peptide bond and protonation of the leaving amine group (step 3). The thioacyl intermediate is long-lived and has been directly detected by mass spectrometry [41]. In the transpeptidation reaction, the amine group of the cell wall cross ...
Promega`s P450-GloTM Luminescent Cytochrome
... A large group of enzymes known as cytochromes P450 (CYP or P450) are responsible for the oxidative metabolism of many xenobiotic, hydrophobic chemicals, which include most therapeutic drugs1. P450 metabolism can influence the clearance rate of drugs, their toxicity, and their interactions with other ...
... A large group of enzymes known as cytochromes P450 (CYP or P450) are responsible for the oxidative metabolism of many xenobiotic, hydrophobic chemicals, which include most therapeutic drugs1. P450 metabolism can influence the clearance rate of drugs, their toxicity, and their interactions with other ...
View/Open - IUPUI ScholarWorks
... Natural products are characterized by high chemical diversity and biochemical specificity; therefore, they are appealing as lead compounds for drug discovery. Given the importance of angiogenesis to many pathologies, numerous natural products have been explored as potential anti-angiogenic drugs. Oc ...
... Natural products are characterized by high chemical diversity and biochemical specificity; therefore, they are appealing as lead compounds for drug discovery. Given the importance of angiogenesis to many pathologies, numerous natural products have been explored as potential anti-angiogenic drugs. Oc ...
ACRIDINE: A VERSATILE HETEROCYCLIC NUCLEUS
... Abstract: Acridine is a heterocyclic nucleus. It plays an important role in various medicines. A number of therapeutic agents are based on acridine nucleus such as quinacrine (antimalarial), acriflavine and proflavine (antiseptics), ethacridine (abortifacient), amsacrine and nitracine (anticancer), ...
... Abstract: Acridine is a heterocyclic nucleus. It plays an important role in various medicines. A number of therapeutic agents are based on acridine nucleus such as quinacrine (antimalarial), acriflavine and proflavine (antiseptics), ethacridine (abortifacient), amsacrine and nitracine (anticancer), ...
Inhibitory Effects of Neurotransmitters and Steroids on Human
... al., 1998), CYP2C9 (Gervasini et al., 2001), CYP2D6 (Martı́nez et al., 1997), and CYP3A (Martı́nez et al., 2000) activities were inhibited by neurotransmitters and their precursors. The inhibition would be of particular importance, since these P450s are expressed in brain and are involved in the met ...
... al., 1998), CYP2C9 (Gervasini et al., 2001), CYP2D6 (Martı́nez et al., 1997), and CYP3A (Martı́nez et al., 2000) activities were inhibited by neurotransmitters and their precursors. The inhibition would be of particular importance, since these P450s are expressed in brain and are involved in the met ...
The role of metabolic inhibition
... their toxicity by their metabolites. Many factors like life style, chemical nature of xenobiotic, genetics and environment affect upcoming toxicity level (Pelkonen et al. 2008). Chemical exposure can result in different gene expression, which could bring different pharmacodynamics effects. A link be ...
... their toxicity by their metabolites. Many factors like life style, chemical nature of xenobiotic, genetics and environment affect upcoming toxicity level (Pelkonen et al. 2008). Chemical exposure can result in different gene expression, which could bring different pharmacodynamics effects. A link be ...
Protein Proteinase Inhibitors in Male Sex Glands
... Trypsin Resin. The seminal vesicles were freshlycollected and immediately frozen. Greater portions were thawed and extracted with ice water. Proteins of higher molecular weights i n these extracts were precipitated by addition of perchloric acid to a final concentration of 3% (w/w). After neutralisa ...
... Trypsin Resin. The seminal vesicles were freshlycollected and immediately frozen. Greater portions were thawed and extracted with ice water. Proteins of higher molecular weights i n these extracts were precipitated by addition of perchloric acid to a final concentration of 3% (w/w). After neutralisa ...
THESPESIA POPULNEA LINN. Review Article MOHINI A. PHANSE*,
... 10. Anti-inflammatory, analgesic and antipyretic properties T. populnea seeds were successively extracted by using petroleum ether (40–60 ◦ C) and ethanol. Unsaponifiable matter and fatty acids were separated from seed oil. Ethanolic extract was fractionated using CHCl3, EtOAc, n-BuOH and H2O solven ...
... 10. Anti-inflammatory, analgesic and antipyretic properties T. populnea seeds were successively extracted by using petroleum ether (40–60 ◦ C) and ethanol. Unsaponifiable matter and fatty acids were separated from seed oil. Ethanolic extract was fractionated using CHCl3, EtOAc, n-BuOH and H2O solven ...
Enoyl acyl carrier protein reductase inhibitors: a patent review (2006
... The emergence of bacterial resistance to most of the antibiotics currently in clinical use becomes a worldwide concern [1]. In particular, methicillin-resistant Staphylococcus aureus (MRSA) [2], penicillin-resistant Streptococcus pneumoniae [3] and multidrug-resistant tuberculosis (MDR-TB) [4] have ...
... The emergence of bacterial resistance to most of the antibiotics currently in clinical use becomes a worldwide concern [1]. In particular, methicillin-resistant Staphylococcus aureus (MRSA) [2], penicillin-resistant Streptococcus pneumoniae [3] and multidrug-resistant tuberculosis (MDR-TB) [4] have ...
Synthesis and Pharmacological Evaluation of
... Cancer, a disease of worldwide importance, is a group of diseases characterized by uncontrolled growth and spread of abnormal cells. It is now generally accepted that a neoplastic transformation is related to genes alteration or oncogene activation, allowing progress in the development of new treatm ...
... Cancer, a disease of worldwide importance, is a group of diseases characterized by uncontrolled growth and spread of abnormal cells. It is now generally accepted that a neoplastic transformation is related to genes alteration or oncogene activation, allowing progress in the development of new treatm ...
Aldehyde Oxidase Activity in Donor
... activity and creating a custom high-activity pooled lot of cryopreserved hepatocytes are advised to minimize underpredictions of clearance. ...
... activity and creating a custom high-activity pooled lot of cryopreserved hepatocytes are advised to minimize underpredictions of clearance. ...
Evaluation of Diuretic activity of aqueous and alcoholic rhizomes
... P<0.05 is considered as moderately significant, p<0.01 is considered as highly significant. The present study revealed that alcoholic and aqueous extracts of Costus peciosus Linn significantly increased the urinary output as well as urinary electrolyte concentration at dose tested (400mg/kg b.w.oral ...
... P<0.05 is considered as moderately significant, p<0.01 is considered as highly significant. The present study revealed that alcoholic and aqueous extracts of Costus peciosus Linn significantly increased the urinary output as well as urinary electrolyte concentration at dose tested (400mg/kg b.w.oral ...
Levy APS - Indiana University Bloomington
... The synthesis and purification of the nine glucagon analogs was relatively straightforward and each peptide was obtained in total yields in excess of 20% based on the weight of the starting amino acid resin. None of the peptides proved any more problematic than native glucagon in the physical handli ...
... The synthesis and purification of the nine glucagon analogs was relatively straightforward and each peptide was obtained in total yields in excess of 20% based on the weight of the starting amino acid resin. None of the peptides proved any more problematic than native glucagon in the physical handli ...
Pharmacologyonline 3: 319-326 (2009) Sariri et al.
... reaction of tyrosinase on dopamine hydrochloride, its most common substrate. The double reciprocal Lineweaver-Burk plot indicated that values of Km increased while Vmax remained constant, typical kinetic behavior of competitive inhibitors. Numeric values of Ki, calculated from Dixon plots [24], Km a ...
... reaction of tyrosinase on dopamine hydrochloride, its most common substrate. The double reciprocal Lineweaver-Burk plot indicated that values of Km increased while Vmax remained constant, typical kinetic behavior of competitive inhibitors. Numeric values of Ki, calculated from Dixon plots [24], Km a ...
Review of Pharmacological Effects of Glycyrrhiza sp. and its
... generation by neutrophils which are the potent mediator of tissue inflammation in the in vitro study. It was thought that one of its antiinflammatory effect was due to this inhibitory effect (Akamatsu et al., 1991; Wang and Nixon, 2001). Also, the generation of reactive oxygen species was also suppres ...
... generation by neutrophils which are the potent mediator of tissue inflammation in the in vitro study. It was thought that one of its antiinflammatory effect was due to this inhibitory effect (Akamatsu et al., 1991; Wang and Nixon, 2001). Also, the generation of reactive oxygen species was also suppres ...
EVALUATION OF ANTHELMINTIC ACTIVITY OF CAESALPINIA PULCHERRIMA (L). BARK Research Article
... inhibition of spontaneous motility (Paralysis) of earthworms. Albendazole(10mg/ml) is used as standard drug. Both the extracts were found to be more potent than albendazole. As compared to aqueous extract, hydroalcoholic extract took less time to cause paralysis & death of the earthworm. Thus the pr ...
... inhibition of spontaneous motility (Paralysis) of earthworms. Albendazole(10mg/ml) is used as standard drug. Both the extracts were found to be more potent than albendazole. As compared to aqueous extract, hydroalcoholic extract took less time to cause paralysis & death of the earthworm. Thus the pr ...
Selective Inhibitors of Picornavirus Replication
... Numerous studies have been performed in the past decades on a series of compounds developed by Sterling-Winthrop, commonly known as ‘‘WIN compounds.’’ Following lead optimization of an accidentally discovered compound, a drug was developed that would meet most of the criteria of a successful anti-pi ...
... Numerous studies have been performed in the past decades on a series of compounds developed by Sterling-Winthrop, commonly known as ‘‘WIN compounds.’’ Following lead optimization of an accidentally discovered compound, a drug was developed that would meet most of the criteria of a successful anti-pi ...
Morphine - ISpatula
... can be also obtained by simple methylation of S-nor-reticuline. Now, S-reticuline which is obtained by either ways is an important intermediate but still S- series and we need the R one, Nature do it! Nature makes small tricks to do it, First it polishes the stereochemistry by simple 1-2 dehydrogen ...
... can be also obtained by simple methylation of S-nor-reticuline. Now, S-reticuline which is obtained by either ways is an important intermediate but still S- series and we need the R one, Nature do it! Nature makes small tricks to do it, First it polishes the stereochemistry by simple 1-2 dehydrogen ...
(PSD) November 2016 PBAC Meeting - (Word 618KB)
... The submission nominated Bd as the main comparator. The submission noted that Cd might also substitute for Ld but it assumed that the extent of this substitution would be small and that Ld would have the same benefits and patient costs as Bd because lenalidomide was listed on a cost-minimisation bas ...
... The submission nominated Bd as the main comparator. The submission noted that Cd might also substitute for Ld but it assumed that the extent of this substitution would be small and that Ld would have the same benefits and patient costs as Bd because lenalidomide was listed on a cost-minimisation bas ...
a review on the pharmacology of embelia ribes burm.f.
... researched. In vitro, it was seen that embelin combined with radiation suppressed prostate cancer PC-3 cell proliferation that was associated with S and G2/M arrest in the cell cycle. Moreover, the combination treatment promoted caspase-independent apoptosis, but not autophagy. In vivo, embelin sign ...
... researched. In vitro, it was seen that embelin combined with radiation suppressed prostate cancer PC-3 cell proliferation that was associated with S and G2/M arrest in the cell cycle. Moreover, the combination treatment promoted caspase-independent apoptosis, but not autophagy. In vivo, embelin sign ...
Antimicrobial activity of grapefruit seed and pulp ethanolic extract
... and pulp of grapefruit (Citrus paradisi Macf., Rutaceae). Chemical research revealed the presence of flavonoids (1, 2), ascorbic acid, tocopherols, citric acid (3), limonoids (4–6), sterols and minerals (7) in grapefruit seeds and pulp. GSE is commonly reported to have a powerful antimicrobial activ ...
... and pulp of grapefruit (Citrus paradisi Macf., Rutaceae). Chemical research revealed the presence of flavonoids (1, 2), ascorbic acid, tocopherols, citric acid (3), limonoids (4–6), sterols and minerals (7) in grapefruit seeds and pulp. GSE is commonly reported to have a powerful antimicrobial activ ...
Reaction Phenotyping Methods using Recombinant Enzymes and
... • Takes advantage of wide inter-individual variability of CYP expression levels between donors (>100-fold variability in CYP activity between donors) • Most direct method – not prone to experimental artifacts from other Rx Phenotyping systems (e.g. chemical/antibody specificity) • Requires panel of ...
... • Takes advantage of wide inter-individual variability of CYP expression levels between donors (>100-fold variability in CYP activity between donors) • Most direct method – not prone to experimental artifacts from other Rx Phenotyping systems (e.g. chemical/antibody specificity) • Requires panel of ...
Mechanism-based Inhibition: Deriving KI and kinact
... CYP3A4, respectively. Usually, measurements at very early time points are more difficult to obtain (and ...
... CYP3A4, respectively. Usually, measurements at very early time points are more difficult to obtain (and ...
carbapenam and monobactam - Home
... Biapenem is a second generation carbapenem with chemical and microbiological properties similar to those of meropenem. Biapenem is stable to DHP-I and is resistant to most β-lactamases. ...
... Biapenem is a second generation carbapenem with chemical and microbiological properties similar to those of meropenem. Biapenem is stable to DHP-I and is resistant to most β-lactamases. ...
Development of analogs of thalidomide
The development of analogs of thalidomide was precipitated by the discovery of the anti-angiogenic and anti-inflammatory properties of the drug yielding a new way of fighting cancer as well as some inflammatory diseases after it had been banned in 1961. The problems with thalidomide included; teratogenic side effects, high incidence of other adverse reactions, poor solubility in water and poor absorption from the intestines.In 1998 thalidomide was approved by the US Food and Drug Administration (FDA) for use in newly diagnosed multiple myeloma (MM) under strict regulations. This has led to the development of a number of analogs with fewer side effects and increased potency which include; lenalidomide, (currently marketed), pomalidomide and apremilast (currently marketed), all of which are manufactured by Celgene.