A New Therapeutic Option for Metastatic Breast Cancer
... Microtubules are a core component of the mitotic spindle that separates chromosomes during eukaryotic cell division.[22] Microtubule‑targeted agents such as taxanes (paclitaxel and docetaxel), vinca alkaloids (vinorelbine and vinblastine), and epothilones (ixabepilone) act by inhibiting microtubule ...
... Microtubules are a core component of the mitotic spindle that separates chromosomes during eukaryotic cell division.[22] Microtubule‑targeted agents such as taxanes (paclitaxel and docetaxel), vinca alkaloids (vinorelbine and vinblastine), and epothilones (ixabepilone) act by inhibiting microtubule ...
Beta-Lactam Antibiotics and Vancomycin Beta
... Properties of ß-lactamases - The genes for ß-lactamase expression coevolved with the genes for the PBP’s as both had similar targets. Thus, there are chromosomal enzymes, such as AmpC, which are subject to the same regulatory mechanisms as other bacterial operons: there is a two-component sensing sy ...
... Properties of ß-lactamases - The genes for ß-lactamase expression coevolved with the genes for the PBP’s as both had similar targets. Thus, there are chromosomal enzymes, such as AmpC, which are subject to the same regulatory mechanisms as other bacterial operons: there is a two-component sensing sy ...
P h a rmaceutical industry is short ... drugs. Whereas in past decades about 50-60 new
... steroid hormones and their more selective synthetic analogs. A first breakthrough in the development of bioavailable analogs resulted from the introduction of 17a-residues, especially the ethinyl group, into estrogenic, gestagenic and androgenic steroids, in order to avoid the rapid metabolic conver ...
... steroid hormones and their more selective synthetic analogs. A first breakthrough in the development of bioavailable analogs resulted from the introduction of 17a-residues, especially the ethinyl group, into estrogenic, gestagenic and androgenic steroids, in order to avoid the rapid metabolic conver ...
Exam Two Notes
... - Inhibits HIV-RT, shows synergistic effect with AZT against HIV-1. Also active against HBV. - (-)-enantiomer shows greater antiviral activity & less toxicity compared with (+)-enatiomer, which inhibits more potently the cellular DNA polymerases. - Cellular 3’,5’ -exonuclease was found to cleave ter ...
... - Inhibits HIV-RT, shows synergistic effect with AZT against HIV-1. Also active against HBV. - (-)-enantiomer shows greater antiviral activity & less toxicity compared with (+)-enatiomer, which inhibits more potently the cellular DNA polymerases. - Cellular 3’,5’ -exonuclease was found to cleave ter ...
Determinants of the Sensitivity of Human Small
... were the first to demonstrate that acute rises in intracellular MTX binding capacity could be a determinant ofdrug resistance in patients with acute leukemia. More recently it has been shown that in vivo resistance after MTX treatment may be due to DHFR gene amplification and elevated target enzyme ...
... were the first to demonstrate that acute rises in intracellular MTX binding capacity could be a determinant ofdrug resistance in patients with acute leukemia. More recently it has been shown that in vivo resistance after MTX treatment may be due to DHFR gene amplification and elevated target enzyme ...
The Organic Chemistry of Drug Design and Drug Action
... drug nebivolol, the (+)-isomer is a -blocker; the (-)-isomer causes vasodilation by a different mechanism. Therefore, it is sold as a racemate to take advantage of both vasodilating pathways. ...
... drug nebivolol, the (+)-isomer is a -blocker; the (-)-isomer causes vasodilation by a different mechanism. Therefore, it is sold as a racemate to take advantage of both vasodilating pathways. ...
Main Title Slide — Always use Title Case on
... This is an exciting trial. The agent is an antibody that essentially blocks the interaction between angiopoietin and its receptor, which is commonly found in the endothelium. The favorable effects on progression-free survival that were reported allow it to go to the next level in a Phase III trial a ...
... This is an exciting trial. The agent is an antibody that essentially blocks the interaction between angiopoietin and its receptor, which is commonly found in the endothelium. The favorable effects on progression-free survival that were reported allow it to go to the next level in a Phase III trial a ...
patrick_tb_ch05
... 01) Which of the following statements is not true about receptors? Feedback: Some protein receptors are certainly present inside cells, but the majority are present in the cell membrane. The binding site of receptors is analogous to the active site of enzymes. However, no reaction is catalysed. The ...
... 01) Which of the following statements is not true about receptors? Feedback: Some protein receptors are certainly present inside cells, but the majority are present in the cell membrane. The binding site of receptors is analogous to the active site of enzymes. However, no reaction is catalysed. The ...
CHAPTER 7 DETERMINATION OF THE ANTIMYCOBACTERIAL ACTIVITY OF THE FRACTIONS AND ISOLATED COMPOUNDS
... drug-sensitive TB recommended by WHO consists of a cocktail of four drugs (INH, RIF, PZA and EMB), taken for six to nine months. The first-line drugs are cheap and have few side effects. Second-line or third-line drugs are more expensive, less potent and some are as toxic as cancer chemotherapy and ...
... drug-sensitive TB recommended by WHO consists of a cocktail of four drugs (INH, RIF, PZA and EMB), taken for six to nine months. The first-line drugs are cheap and have few side effects. Second-line or third-line drugs are more expensive, less potent and some are as toxic as cancer chemotherapy and ...
Zebrafish behavioral profiling links drugs to biological targets and
... been described (14). Behavioral profiling revealed that a diverse set of anti-inflammatory compounds increased waking activity during the day with much less effect at night (Fig. 4B and fig. S17). These anti-inflammatory compounds included the steroidal glucocorticoids, the nonsteroidal anti-inflamm ...
... been described (14). Behavioral profiling revealed that a diverse set of anti-inflammatory compounds increased waking activity during the day with much less effect at night (Fig. 4B and fig. S17). These anti-inflammatory compounds included the steroidal glucocorticoids, the nonsteroidal anti-inflamm ...
Self-Emulsifying Drug Delivery Systems: Strategy for Improving Oral De-
... of the human diet, are the main surfactants in formulations of cyclosporine [15]. Similar to phospholipids, galactolipids have good emulsifying properties, but one major difference is that phospholipids are charged, while galactolipids are non-ionic and regarded as being safe for long-term use [15]. ...
... of the human diet, are the main surfactants in formulations of cyclosporine [15]. Similar to phospholipids, galactolipids have good emulsifying properties, but one major difference is that phospholipids are charged, while galactolipids are non-ionic and regarded as being safe for long-term use [15]. ...
Biacore™ concentration and ligand-binding analyses in late
... is defined. In the bioprocess lab, analysis is focused on the control of cell culture (4) and purification (5) procedures. With CPP identified and a control strategy in place, the CQA should be secured and verification should be straightforward. To support this process, requirements on test procedur ...
... is defined. In the bioprocess lab, analysis is focused on the control of cell culture (4) and purification (5) procedures. With CPP identified and a control strategy in place, the CQA should be secured and verification should be straightforward. To support this process, requirements on test procedur ...
From fragment to clinical candidate—a historical perspective
... common in featureless and solvent exposed pockets (e.g. proteases or protein–protein interactions), which are less druggable. A number of alternative definitions of LE have been proposed [57–59] and there is also an increased interest on normalising potency by lipophilicity ...
... common in featureless and solvent exposed pockets (e.g. proteases or protein–protein interactions), which are less druggable. A number of alternative definitions of LE have been proposed [57–59] and there is also an increased interest on normalising potency by lipophilicity ...
Molecular determinants of drug–receptor binding kinetics
... did optimization of binding affinity guide most early-stage discovery efforts. This emphasis on binding affinity — quantified either as Kd, the equilibrium dissociation constant, or its proxies, IC50 or EC50, the drug concentrations giving half-maximal inhibition or effect — is predicated on the ass ...
... did optimization of binding affinity guide most early-stage discovery efforts. This emphasis on binding affinity — quantified either as Kd, the equilibrium dissociation constant, or its proxies, IC50 or EC50, the drug concentrations giving half-maximal inhibition or effect — is predicated on the ass ...
No Slide Title
... •Since Colchicine prevents the formation of microtubules , this could be useful in limiting the mitotic activity of tumors cell : by preventing the formation of mitotic spindles (microtubules .) ...
... •Since Colchicine prevents the formation of microtubules , this could be useful in limiting the mitotic activity of tumors cell : by preventing the formation of mitotic spindles (microtubules .) ...
Phyto Lec 16
... The active constituent is the Colchicine. Colchicine is used for the treatment of hay fever, Mediterranean fever, anti-inflammatory for gout (does not affect uric acid metabolism). Gout is the accumulation of uric acid in the joints. Uric acid is formed from the xanthine by the xanthine oxidase enzy ...
... The active constituent is the Colchicine. Colchicine is used for the treatment of hay fever, Mediterranean fever, anti-inflammatory for gout (does not affect uric acid metabolism). Gout is the accumulation of uric acid in the joints. Uric acid is formed from the xanthine by the xanthine oxidase enzy ...
DESIGN, SYNTHESIS AND MOLECULAR DOCKING STUDIES OF BENZOTHIAZOLE Research Article
... potential pharmacological activities. Benzothiazole is usually prepared by ring closure of o-aminothiophenols with acid chlorides. Due to the immense importance in pharmaceutical utilities, the synthesis of derivative compounds is of considerable interests [2]. The benzothiazole moiety is establishe ...
... potential pharmacological activities. Benzothiazole is usually prepared by ring closure of o-aminothiophenols with acid chlorides. Due to the immense importance in pharmaceutical utilities, the synthesis of derivative compounds is of considerable interests [2]. The benzothiazole moiety is establishe ...
Evaluation of drug release from Abraxane and Doxil in tumor tissue.
... LIST OF FIGURES ............................................................................................................................. vii I. ...
... LIST OF FIGURES ............................................................................................................................. vii I. ...
Pharmacy_Lecture_08_..
... acidic, but not carboxylic acid-containing (salicylic acid) structurally novel compounds. • Measurement of a physical property (pKa) as well as serum half-life in dogs was the guide for the synthesis program. • Several generations of leads were refined and ultimately led to a successful structure wi ...
... acidic, but not carboxylic acid-containing (salicylic acid) structurally novel compounds. • Measurement of a physical property (pKa) as well as serum half-life in dogs was the guide for the synthesis program. • Several generations of leads were refined and ultimately led to a successful structure wi ...
Available
... In active transport, the drug molecule penetrates in the lipid bilayer membrane from lower concentration to the higher concentration of solutes against the concentration gradient with the expenditure of energy and with the help of special carrier proteins. This process has two types of energy depend ...
... In active transport, the drug molecule penetrates in the lipid bilayer membrane from lower concentration to the higher concentration of solutes against the concentration gradient with the expenditure of energy and with the help of special carrier proteins. This process has two types of energy depend ...
Psychology 472 Pharmacology of Psychoactive Drugs
... Distribution Methods • Plasma–more likely with water soluble drugs • Platelets–more likely with lipid soluble drugs • Attached to proteins (e.g., albumin)–bound vs. free ...
... Distribution Methods • Plasma–more likely with water soluble drugs • Platelets–more likely with lipid soluble drugs • Attached to proteins (e.g., albumin)–bound vs. free ...
reviews - Medicina
... formyl-methionine tRNA. In vitro potency against MTB H37Rv is 0.25 μg/mL. LIN is active against MDR M. tuberculosis strains (48). LIN causes reversible myelosuppression (including anemia, leukopenia, pancytopenia, and thrombocytopenia) in patients especially when the drug is administered for prolong ...
... formyl-methionine tRNA. In vitro potency against MTB H37Rv is 0.25 μg/mL. LIN is active against MDR M. tuberculosis strains (48). LIN causes reversible myelosuppression (including anemia, leukopenia, pancytopenia, and thrombocytopenia) in patients especially when the drug is administered for prolong ...
Tutorial - 4: Respiratory Drug Development
... of the aromatic ring form essential hydrogen bonding interaction with the amino acid residues Ser207 and Ser204 at the binding site of the receptor. Alkylammonium ion forms an ionic bond to the binding site (Asp113) of the receptor. Bulkier t-butyl group is responsible for selectivity towards β2 ...
... of the aromatic ring form essential hydrogen bonding interaction with the amino acid residues Ser207 and Ser204 at the binding site of the receptor. Alkylammonium ion forms an ionic bond to the binding site (Asp113) of the receptor. Bulkier t-butyl group is responsible for selectivity towards β2 ...
P. aeruginosa
... The oral second-generation cephalosporins are active against beta-lactamase-producing H. influenzae or Moraxella catarrhalis and have been primarily used to treat sinusitis, otitis, or lower respiratory tract infections, in which these organisms have an important role. Because of their activity aga ...
... The oral second-generation cephalosporins are active against beta-lactamase-producing H. influenzae or Moraxella catarrhalis and have been primarily used to treat sinusitis, otitis, or lower respiratory tract infections, in which these organisms have an important role. Because of their activity aga ...