Cytoskeletal Regulation by the Nedd8 Ubiquitin-Like
... The Nedd8 ubiquitin-like protein modification pathway regulates cell-cycle progression. Our analysis of Nedd8 requirements during Caenorhabditis elegans embryogenesis indicates that the cytoskeleton is another target. Nedd8 conjugation negatively regulated contractility of the microfilament-rich cel ...
... The Nedd8 ubiquitin-like protein modification pathway regulates cell-cycle progression. Our analysis of Nedd8 requirements during Caenorhabditis elegans embryogenesis indicates that the cytoskeleton is another target. Nedd8 conjugation negatively regulated contractility of the microfilament-rich cel ...
Articles - The Vespiary
... somewhat offset by the more effective hydrogen-bonding of the constrained heterocyclic oxygens) would enhance their in vivo activity. Nevertheless, in the behavioral assays, the rank order of potency for this series decreased with increasing molecular hydrophobicity. In view of the somewhat greater ...
... somewhat offset by the more effective hydrogen-bonding of the constrained heterocyclic oxygens) would enhance their in vivo activity. Nevertheless, in the behavioral assays, the rank order of potency for this series decreased with increasing molecular hydrophobicity. In view of the somewhat greater ...
International Journal of Universal Pharmacy and Life Sciences
... antifungal activity 9, 10 &11. Similarly the preliminary phytochemical constituents studies showed the presence of triterpenoids and alkaloids could have responsible for the activity. Since prehistoric times, people have used natural resources for medicinal purposes. Folk medicines employ many plant ...
... antifungal activity 9, 10 &11. Similarly the preliminary phytochemical constituents studies showed the presence of triterpenoids and alkaloids could have responsible for the activity. Since prehistoric times, people have used natural resources for medicinal purposes. Folk medicines employ many plant ...
basic concepts and importance of various pharmacokinetic parameters
... Drug can bind with plasma proteins (eg. Albumin, AAG, etc). Or tissue components One measure is free fraction (fu) ...
... Drug can bind with plasma proteins (eg. Albumin, AAG, etc). Or tissue components One measure is free fraction (fu) ...
Open PDF File - Array BioPharma
... Literature compounds with a greater than 10-fold preference for AAG demonstrated a greater than three-fold decrease in the free fraction with increasing AAG levels: ritonavir, imatinib, nelfinavir, docetaxel, chlorpromazine, imipramine, erythromycin, and propranolol. Test compounds that had a modera ...
... Literature compounds with a greater than 10-fold preference for AAG demonstrated a greater than three-fold decrease in the free fraction with increasing AAG levels: ritonavir, imatinib, nelfinavir, docetaxel, chlorpromazine, imipramine, erythromycin, and propranolol. Test compounds that had a modera ...
Effect of Ethanolic Pod Extract of Canavalia gladiata
... extract of Canavalia gladiate pods showed significant (P<0.001) decrease in number of ulcers ulcer score index and increase in the percentage protection in aspirin- induced ulceration models. The ethanolic extract of Canavalia gladiate pods possesses significant antiulcer properties. In conclusion t ...
... extract of Canavalia gladiate pods showed significant (P<0.001) decrease in number of ulcers ulcer score index and increase in the percentage protection in aspirin- induced ulceration models. The ethanolic extract of Canavalia gladiate pods possesses significant antiulcer properties. In conclusion t ...
Alkaloids Derived from Phenylalanine and Tyrosine
... • The proliferation of products based on mahuang and/or ephedrine has caused an increase in the number of case reports of more or less serious side effects and in 1997, the FDA proposed detailed labeling requirements for ephedra-based dietary supplements: warnings against prolonged used and against ...
... • The proliferation of products based on mahuang and/or ephedrine has caused an increase in the number of case reports of more or less serious side effects and in 1997, the FDA proposed detailed labeling requirements for ephedra-based dietary supplements: warnings against prolonged used and against ...
s - Clayton State University
... COMe could be bio-isosteres) •Choose bio-isosteres based on most important physicochemical property ...
... COMe could be bio-isosteres) •Choose bio-isosteres based on most important physicochemical property ...
ISOLATION AND IDENTIFICATION OF α-GLUCOSIDASE, α-AMYLASE AND LIPASE INHIBITORS
... properties. The importance of the inhibitors of these enzymes have attracted interest because the inhibition of the catalytic activity of αglucosidase leads to retardation of the absorption of glucose and the reduction of postprandial blood glucose level [3,4], therefore they play a significant role ...
... properties. The importance of the inhibitors of these enzymes have attracted interest because the inhibition of the catalytic activity of αglucosidase leads to retardation of the absorption of glucose and the reduction of postprandial blood glucose level [3,4], therefore they play a significant role ...
Protein Ligand Interactions: A Method and its Application to Drug Discovery
... Cataracts result from TG1 inhibited SERCA up-regulation EDS increases intracellular calcium in lens epithelial cells by inhibiting SERCA in silico Studies Ligand binding site similarity Binding affinity correlation ...
... Cataracts result from TG1 inhibited SERCA up-regulation EDS increases intracellular calcium in lens epithelial cells by inhibiting SERCA in silico Studies Ligand binding site similarity Binding affinity correlation ...
Conventional Cancer Treatment
... biochemical reactions in cells. The mechanism of action of antimetabolites include: competition for binding sites of enzymes that participate in essential biosynthetic processes and incorpo‐ ration into nucleic acids, which inhibits their normal function triggering the apoptosis process. 3.1. Folic ...
... biochemical reactions in cells. The mechanism of action of antimetabolites include: competition for binding sites of enzymes that participate in essential biosynthetic processes and incorpo‐ ration into nucleic acids, which inhibits their normal function triggering the apoptosis process. 3.1. Folic ...
Anti-infective potential of natural products: How
... Infectious diseases caused by bacteria, fungi, viruses and parasites are still a major threat to public health, despite the tremendous progress in human medicine. Their impact is particularly large in developing countries due to the relative unavailability of medicines and the emergence of widesprea ...
... Infectious diseases caused by bacteria, fungi, viruses and parasites are still a major threat to public health, despite the tremendous progress in human medicine. Their impact is particularly large in developing countries due to the relative unavailability of medicines and the emergence of widesprea ...
Rational Drug Design Approach to Synthesizing HIV-1 Protease Inhibitors
... HIV-1 protease with LY289612 (a peptidomimetic inhibitor). As their base design they retained only the non-peptidic hydroxyethyl-t-butylbenzamide portion of the original inhibitor. From here, the researchers synthesized and attached a variety of substituents to fit into the various active site pocke ...
... HIV-1 protease with LY289612 (a peptidomimetic inhibitor). As their base design they retained only the non-peptidic hydroxyethyl-t-butylbenzamide portion of the original inhibitor. From here, the researchers synthesized and attached a variety of substituents to fit into the various active site pocke ...
P-Glycoprotein in the Blood-Brain Barrier of Mice Influences the
... tightly joined endothelial cells in the brain. Recently, quite effective inhibitors of P-GP such as PSC 833 have been described (15), and these so-called reversal agents are currently administered to patients in clinical trials to reverse the chemotherapy resistance of P-GP–expressing tumors (see re ...
... tightly joined endothelial cells in the brain. Recently, quite effective inhibitors of P-GP such as PSC 833 have been described (15), and these so-called reversal agents are currently administered to patients in clinical trials to reverse the chemotherapy resistance of P-GP–expressing tumors (see re ...
Pathway-Dependent Inhibition of Paclitaxel Hydroxylation by Kinase
... Pharmacokinetic variability of paclitaxel in patients has been thought to be associated with different expressions and activities of CYP2C8, CYP3A4, and P-gp, and numerous studies have been conducted to examine the role of polymorphisms in CYP enzymes and their relationship with intersubject variabi ...
... Pharmacokinetic variability of paclitaxel in patients has been thought to be associated with different expressions and activities of CYP2C8, CYP3A4, and P-gp, and numerous studies have been conducted to examine the role of polymorphisms in CYP enzymes and their relationship with intersubject variabi ...
Central Nervous System Activity Studies of Baptisia tinctoria (L.) R
... Abstract. The present investigations were undertaken with a view to evaluate Baptisia tinctoria roots (Wild Indigo; family – Fabaceae) systematically for neuropharmacological activities. The methanol extract (ME) of plant was prepared by extracting properly identified plant in a Soxhlet apparatus wi ...
... Abstract. The present investigations were undertaken with a view to evaluate Baptisia tinctoria roots (Wild Indigo; family – Fabaceae) systematically for neuropharmacological activities. The methanol extract (ME) of plant was prepared by extracting properly identified plant in a Soxhlet apparatus wi ...
Assessment of Drug−Lipid Complex Formation by a High
... animals and cells.34,35 The gene expression microarrays may suffer from the high complexity of the assay and from the fact that the drugs may influence gene expression by mechanisms, which poorly reflect their potency to induce PLD. In addition, the primary problem is unlikely the expression of gene ...
... animals and cells.34,35 The gene expression microarrays may suffer from the high complexity of the assay and from the fact that the drugs may influence gene expression by mechanisms, which poorly reflect their potency to induce PLD. In addition, the primary problem is unlikely the expression of gene ...
Rib_Inh_15
... • Spectrum of Activity -Many gram-negative and some gram-positive bacteria; Not useful for anaerobic (oxygen required for uptake of antibiotic) or intracellular bacteria. ...
... • Spectrum of Activity -Many gram-negative and some gram-positive bacteria; Not useful for anaerobic (oxygen required for uptake of antibiotic) or intracellular bacteria. ...
CURRENT STATUS OF DESIGNER DRUGS
... CURRENT STATUS OF DESIGNER DRUGS Bert Toivola, Ph.D. Scientific Director Norchem Drug Testing Laboratory Cordant Forensic Solutions Flagstaff, Arizona ...
... CURRENT STATUS OF DESIGNER DRUGS Bert Toivola, Ph.D. Scientific Director Norchem Drug Testing Laboratory Cordant Forensic Solutions Flagstaff, Arizona ...
- Biomacromolecular Journal
... of RMSD value of protein in complex with respect to free protein. As it’s seen in Fig. 2, all these simulations as the same other biolgycal systems have the same logical manner in their fluctuations (rmsd: 0.3-0.6 nm) and probably the structure of the protein was more destabilized in the binding to ...
... of RMSD value of protein in complex with respect to free protein. As it’s seen in Fig. 2, all these simulations as the same other biolgycal systems have the same logical manner in their fluctuations (rmsd: 0.3-0.6 nm) and probably the structure of the protein was more destabilized in the binding to ...
challenges in adc development
... GEMTUZUMAB OZOOGAMICIN (GO, MYLOTARG, PFIZER) First ADC to be approved by FDA in 2000 – positive results were from the first single-agent phase II studies achieving 30% remissions (Tsimberidou et al, 2006). Consisted of a humanised IgG4 mAb directed against CD33 (a surface antigen present in 85 ...
... GEMTUZUMAB OZOOGAMICIN (GO, MYLOTARG, PFIZER) First ADC to be approved by FDA in 2000 – positive results were from the first single-agent phase II studies achieving 30% remissions (Tsimberidou et al, 2006). Consisted of a humanised IgG4 mAb directed against CD33 (a surface antigen present in 85 ...
Invited Review - International Journal of Pharmaceutical Science
... showed that the anti-fungal activity of the substituents at the phenyl ring is H, Cl, Br, o,p-diCl > F, NO2 for benzylic 2,4TZD compounds. As for phenacyl 2,4-TZD compounds, it is Cl, Br > H, F, o,p-di-Cl, NO2. Cukurovali et al [25] reported a series of Schiff bases containing 2, 4-disubstituted thi ...
... showed that the anti-fungal activity of the substituents at the phenyl ring is H, Cl, Br, o,p-diCl > F, NO2 for benzylic 2,4TZD compounds. As for phenacyl 2,4-TZD compounds, it is Cl, Br > H, F, o,p-di-Cl, NO2. Cukurovali et al [25] reported a series of Schiff bases containing 2, 4-disubstituted thi ...
Antiviral Agents: Structural Basis of Action and Rational Design
... Drug discovery programs start with the identification of suitable drug targets (Fig. 20.1). A drug target can be defined as a biomolecule (usually a single protein or a protein complex) linked to a disease and containing a suitable binding site that can be exploited to modulate its function. These t ...
... Drug discovery programs start with the identification of suitable drug targets (Fig. 20.1). A drug target can be defined as a biomolecule (usually a single protein or a protein complex) linked to a disease and containing a suitable binding site that can be exploited to modulate its function. These t ...
Phyto-phospholipid complex vesicles for phytoconstituents and
... and bioavailability. Phytosome process produces a cell which is a valuable component of herbal extract which protected from destruction by digestive secretion and gut bacteria. Phytosomes are better able to transform from a hydrophilic environment into the lipid friendly environment of the enterocyt ...
... and bioavailability. Phytosome process produces a cell which is a valuable component of herbal extract which protected from destruction by digestive secretion and gut bacteria. Phytosomes are better able to transform from a hydrophilic environment into the lipid friendly environment of the enterocyt ...