Biron_JSBMB_2015_rev - Corpus UL
... The androgen receptor (AR) is a member of the nuclear receptor (NR) superfamily of ligand regulated transcription factors that plays an integral role in primary and secondary male sexual development. As a key regulator for the growth, terminal differentiation and function of the prostate gland, exce ...
... The androgen receptor (AR) is a member of the nuclear receptor (NR) superfamily of ligand regulated transcription factors that plays an integral role in primary and secondary male sexual development. As a key regulator for the growth, terminal differentiation and function of the prostate gland, exce ...
CDAS|Safety Pharmacology
... Client compound(s) are profiled through the same SED assay set and the profile data are then compared with the compounds in the CDAS side effect database. ...
... Client compound(s) are profiled through the same SED assay set and the profile data are then compared with the compounds in the CDAS side effect database. ...
Laboratory Testing for HIV Tropism
... Next Review Date: 05/17 Review Dates: 05/09, 03/10, 03/11, 03/12, 03/13, 03/14, 03/15, 05/15, 05/16 Preauthorization is not required. ...
... Next Review Date: 05/17 Review Dates: 05/09, 03/10, 03/11, 03/12, 03/13, 03/14, 03/15, 05/15, 05/16 Preauthorization is not required. ...
Memorandum
... the submission. The “active ingredient” in Salacia Oblonga was presented as CgHr&09. However, throughout the notification, the SaZacia oblonga (Celastraceae) extract was referred to as “Novel Compound S,” “Novel Compound SP,” “the test drug,” and “Product of the present invention.” These description ...
... the submission. The “active ingredient” in Salacia Oblonga was presented as CgHr&09. However, throughout the notification, the SaZacia oblonga (Celastraceae) extract was referred to as “Novel Compound S,” “Novel Compound SP,” “the test drug,” and “Product of the present invention.” These description ...
Strategies and Challenges Involved in the Discovery of
... success has been seen with the development of the nitroimidazoles PA824 10 (Figure 4) [27] and OPC-67683 (delamanid) 11 (Figure 4) [28] and the diamine SQ-109 12 [29], which are also in phase 2 clinical trials. In the early discovery phase of drug development, other recent examples of novel active s ...
... success has been seen with the development of the nitroimidazoles PA824 10 (Figure 4) [27] and OPC-67683 (delamanid) 11 (Figure 4) [28] and the diamine SQ-109 12 [29], which are also in phase 2 clinical trials. In the early discovery phase of drug development, other recent examples of novel active s ...
(12)Indian Patent Application ______________________________________________________________
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...
Screening and hit evaluation of a chemical library against blood
... Methods: The selection cascade used for the triaging of hits from the chemical library started with a robust threestep in vitro assay followed by an in silico analysis of the resulting confirmed hits. Upon reaching the predefined requirements for selectivity and potency, the set of hits was subjecte ...
... Methods: The selection cascade used for the triaging of hits from the chemical library started with a robust threestep in vitro assay followed by an in silico analysis of the resulting confirmed hits. Upon reaching the predefined requirements for selectivity and potency, the set of hits was subjecte ...
New Insights for Drug Design from the X
... 2007; Rasmussen et al., 2007; Rosenbaum et al., 2007). These landmark studies were followed by the determination of other GPCRs (Table 1), and the rapid pace of these reports is continuing. Biogenic amine receptor complexes (epinephrine, dopamine, histamine, muscarinic), nucleoside (adenosine) recep ...
... 2007; Rasmussen et al., 2007; Rosenbaum et al., 2007). These landmark studies were followed by the determination of other GPCRs (Table 1), and the rapid pace of these reports is continuing. Biogenic amine receptor complexes (epinephrine, dopamine, histamine, muscarinic), nucleoside (adenosine) recep ...
Permeability Fundamentals
... Optimizing passive diffusion is productive because it is the predominant mechanism for absorption of most commercial drugs. Permeability is increased by removing ionizable groups, increasing Log P, and decreasing size and polarity. ...
... Optimizing passive diffusion is productive because it is the predominant mechanism for absorption of most commercial drugs. Permeability is increased by removing ionizable groups, increasing Log P, and decreasing size and polarity. ...
Problem Set 2: Cephalosporins: KEY Answer the following
... Which exists as anions at physiologic pH? Answer A, B, D, F and maybe C, if you consider it to have hydrolyzed to the acid. Compounds A, B, D and F are acids or diacids with pKas in the 3-5 range and thus will be ionized at physiologic pH. Compound E is a zwitterion and will exist as a zwitterion, n ...
... Which exists as anions at physiologic pH? Answer A, B, D, F and maybe C, if you consider it to have hydrolyzed to the acid. Compounds A, B, D and F are acids or diacids with pKas in the 3-5 range and thus will be ionized at physiologic pH. Compound E is a zwitterion and will exist as a zwitterion, n ...
13. chapter - vi
... role of drugs in living organisms. Biological evaluation depends upon the study of various bacteria present in cell membrane of living system. In fact first life on the earth was started by bacteria called cyanobacteria,, later to it eukaryotic life started and evolved biological life like animals a ...
... role of drugs in living organisms. Biological evaluation depends upon the study of various bacteria present in cell membrane of living system. In fact first life on the earth was started by bacteria called cyanobacteria,, later to it eukaryotic life started and evolved biological life like animals a ...
SERIES ‘‘GENETICS OF ASTHMA AND COPD IN THE POSTGENOME ERA’’
... While the presence of linkage disequilibrium can sometimes make genetic analyses in populations easier, it can also cause difficulty. To understand this, it is useful to consider two possible scenarios. In the first scenario, there is one functionally relevant polymorphism but strong linkage disequi ...
... While the presence of linkage disequilibrium can sometimes make genetic analyses in populations easier, it can also cause difficulty. To understand this, it is useful to consider two possible scenarios. In the first scenario, there is one functionally relevant polymorphism but strong linkage disequi ...
accuracy of biological activity spectra predicting
... Activity Spectra for Substances) 11-14 predicts simultaneously several hundreds of various biological activities. These are pharmacological effects, mechanisms of action, mutagenicity, carcinogenicity, teratogenicity and embryotoxicity. PASS prediction is based on the analysis of structure-activity ...
... Activity Spectra for Substances) 11-14 predicts simultaneously several hundreds of various biological activities. These are pharmacological effects, mechanisms of action, mutagenicity, carcinogenicity, teratogenicity and embryotoxicity. PASS prediction is based on the analysis of structure-activity ...
2002
... the absence and presence of 10M naloxone. The potency of the drugs in displacing the specific binding of the 3Hligand is determined from data using Graphpad Prism (GraphPAD, San Diego, CA) and converted to Ki values by the method of Cheng and Prussoff (1973). Opioid binding is performed in membrane ...
... the absence and presence of 10M naloxone. The potency of the drugs in displacing the specific binding of the 3Hligand is determined from data using Graphpad Prism (GraphPAD, San Diego, CA) and converted to Ki values by the method of Cheng and Prussoff (1973). Opioid binding is performed in membrane ...
Full-Text PDF
... Moreover, the expression and activities of the PDKs are strongly regulated by oncogenes [17–19]. Type 2 diabetes and obesity are characterized by dysregulation of glucose and lipid metabolism, in which PDC plays a pivotal role [20]. Increasing the activity of PDC through inhibition of PDKs could imp ...
... Moreover, the expression and activities of the PDKs are strongly regulated by oncogenes [17–19]. Type 2 diabetes and obesity are characterized by dysregulation of glucose and lipid metabolism, in which PDC plays a pivotal role [20]. Increasing the activity of PDC through inhibition of PDKs could imp ...
GABA-A receptor subtypes in the brain: a paradigm for CNS drug
... Although the target validation studies described previously are crucial steps in the drug discovery process, clearly there is some way to go and many unanswered questions. For instance, the receptor subtypes that mediate tolerance and dependence remain unknown, and indeed these phenomena might not b ...
... Although the target validation studies described previously are crucial steps in the drug discovery process, clearly there is some way to go and many unanswered questions. For instance, the receptor subtypes that mediate tolerance and dependence remain unknown, and indeed these phenomena might not b ...
Ligand Residence Time at G-protein–Coupled Receptors—Why We
... that the dynamic of a protein can greatly influence ligand dissociation (Teague, 2003; Carroll et al., 2012), or in other words conformational adaptation of the receptor can greatly influence the residence time of a ligand on its receptor or a drug on its target. This is schematically depicted in Fi ...
... that the dynamic of a protein can greatly influence ligand dissociation (Teague, 2003; Carroll et al., 2012), or in other words conformational adaptation of the receptor can greatly influence the residence time of a ligand on its receptor or a drug on its target. This is schematically depicted in Fi ...
From fragment to clinical candidate—a historical perspective
... played a key role in the development of fragment-based drug discovery (FBDD) have been around for over two decades. In 1981, Jencks introduced the idea that large molecules can be considered as the combination of two or more ‘fragments’ that contain all the features necessary for binding to the targ ...
... played a key role in the development of fragment-based drug discovery (FBDD) have been around for over two decades. In 1981, Jencks introduced the idea that large molecules can be considered as the combination of two or more ‘fragments’ that contain all the features necessary for binding to the targ ...
Indirect cholinergic agonists
... -Drugs differ in their CNS effects, scopolamine permeates the blood-brain barrier -At therapeutic doses atropine has negligible effects upon the CNS, scopolamine even at low doses has prominent CNS effects. ...
... -Drugs differ in their CNS effects, scopolamine permeates the blood-brain barrier -At therapeutic doses atropine has negligible effects upon the CNS, scopolamine even at low doses has prominent CNS effects. ...
Investigator`s brochure
... Briefly state the investigational product (IP) chemical name, generic name (if approved) and trade name (if approved). List the active ingredients and confirm which pharmacological class the IP is in. Briefly discuss its expected position within this class (i.e., the advantages it is expected to hav ...
... Briefly state the investigational product (IP) chemical name, generic name (if approved) and trade name (if approved). List the active ingredients and confirm which pharmacological class the IP is in. Briefly discuss its expected position within this class (i.e., the advantages it is expected to hav ...
Antiviral Agents: Structural Basis of Action and Rational Design
... assembly is a complex process which involves multiple molecular recognition steps and conformational transitions. The viral capsid is assembled in a multimerization reaction, with or without the help of scaffolding proteins or viral nucleic acids (see Chaps. 10, 11 and 19). The viral nucleic acids a ...
... assembly is a complex process which involves multiple molecular recognition steps and conformational transitions. The viral capsid is assembled in a multimerization reaction, with or without the help of scaffolding proteins or viral nucleic acids (see Chaps. 10, 11 and 19). The viral nucleic acids a ...
PharmII Block I Handouts
... ○ Because the ions can be partially absorbed, laxatives containing magnesium and phosphorous are contraindicated in patients with impaired renal function ○ Avoid sodium phosphate-containing formulations in patients with congestive heart failure, liver failure – severe electrolyte abnormalities can o ...
... ○ Because the ions can be partially absorbed, laxatives containing magnesium and phosphorous are contraindicated in patients with impaired renal function ○ Avoid sodium phosphate-containing formulations in patients with congestive heart failure, liver failure – severe electrolyte abnormalities can o ...
Interaction of Plant Extracts with Central Nervous System Receptors
... Both G protein-coupled receptors (GPCRs) and ion channels possess important functions in the CNS [11,12]. They mediate signal transduction events in the CNS, which are triggered by neurotransmitters and other types of molecules and dysfunction results in inactive, overexpressed or constitutively act ...
... Both G protein-coupled receptors (GPCRs) and ion channels possess important functions in the CNS [11,12]. They mediate signal transduction events in the CNS, which are triggered by neurotransmitters and other types of molecules and dysfunction results in inactive, overexpressed or constitutively act ...
DOPAMINE ANTAGONISTS: PHENOTHIAZINE/THIOXANTHENE SAR
... affinities on nondopaminergic sites, such as cholinergic (muscarinic), alpha-1adrenergic and histamine-1 receptors, which can partially explain the varied side effect profiles for each agent. Typical antipsychotics have similar efficacies when used in equipotent doses and are likely to induce extrap ...
... affinities on nondopaminergic sites, such as cholinergic (muscarinic), alpha-1adrenergic and histamine-1 receptors, which can partially explain the varied side effect profiles for each agent. Typical antipsychotics have similar efficacies when used in equipotent doses and are likely to induce extrap ...
CCR5 receptor antagonist
CCR5 receptor antagonists are a class of small molecules that antagonize the CCR5 receptor. The C-C motif chemokine receptor CCR5 is involved in the process by which HIV, the virus that causes AIDS, enters cells. Hence antagonists of this receptor are entry inhibitors and have potential therapeutic applications in the treatment of HIV infections.The life cycle of the HIV presents potential targets for drug therapy, one of them being the viral entry pathway. The C-C motif chemokine receptors CCR5 and CXCR4 are the main chemokine receptors involved in the HIV entry process. These receptors belong to the seven transmembrane G-protein-coupled receptor (GPCR) family and are predominantly expressed on human T-cells, dendritic cells and macrophages, Langerhans cells. They play an important role as co-receptors that HIV type 1 (HIV-1) uses to attach to cells before viral fusion and entry into host cells. HIV isolates can be divided into R5 and X4 strains. R5 strain is when the virus uses the co-receptor CCR5 and X4 strain is when it uses CXCR4. The location of CCR5 receptors at the cell surface, both large and small molecules have the potential to interfere with the CCR5-viral interaction and inhibit viral entry into human cells.