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Methods for identifying microRNA binding motifs
Methods for identifying microRNA binding motifs

... Mammalian (RNAi); Bacteria (CRISPR) Post-transcriptional modulation of gene expression Mediated by formation of RNA-induced silencing complex (RISC) with small non-coding (ncRNA) as guide RNA Binding of microRNA to mRNA either results in mRNA cleavage or reduce mRNA stability through deadenylation a ...
A hypothesis on peculiar pharmacological behaviour of biologically
A hypothesis on peculiar pharmacological behaviour of biologically

... In this view, the idea that the biological activity of a natural extract is due to one (or more) of its component is surely reductive, because it does not take into account all the possible interactions existing among their components. A natural extract is a mixture of hundreds of neutral organic mo ...
Review Drug chirality: a consideration of the significance
Review Drug chirality: a consideration of the significance

... (2R, 3S)-configuration, and the other laevopropoxyphene ((2S, 3^)-configuration) as an antitussive. In the case of this example not only are the molecules mirror image related but so are their trade names (Darvon/Novrad). Stereoselectivity is also observed in drug disposition particularly for those ...
Modelling and simulation to help define MABEL and Starting
Modelling and simulation to help define MABEL and Starting

... • Determine RO and pharmacological effect relationship. • Extrapolate model to humans using all relevant data (literature, in vitro human etc) • Perform simulations considering both uncertainty in model parameters and in scale-up • This approach should help select a more rational starting dose for F ...
PHL 424 9th S - Home - KSU Faculty Member websites
PHL 424 9th S - Home - KSU Faculty Member websites

...  Clindamycin is a chlorine-substituted derivative of lincomycin, an antibiotic produced by Streptomyces lincolnensis  Lincomycin, although structurally distinct, resembles erythromycin in activity, but it is toxic and no longer used ...
Drug Absorption
Drug Absorption

... • The drug is a modified neutral amino acid, and as such is competitively absorbed with dietary amino acids. • Protein-rich meal (beef meal) reduced both the rate and extend of the bioavailability of methyldopa. • May also explain by an increase of “first-pass” metabolism. Methyldopa is extensively ...
AFFINITY OF WARFARIN WITH CYP2C9 BY MOLECULAR DOCKING STUDY  Original Article
AFFINITY OF WARFARIN WITH CYP2C9 BY MOLECULAR DOCKING STUDY Original Article

... Cytochrome P450 (CYP) 2C9 is the principal isoform of the CYP2C subfamily in the human liver and is involved in the oxidation of several endogenous and xenobiotic compounds, which plays major role in Metabolism of warfarin.Warfarin is Coumarin derivative act as an Oral Anticoagulant,its Molecular Fo ...
8 - Ani-Viral
8 - Ani-Viral

... NRTIs, and from their names they are neither nucleotide triphosphate nor require phosphorylation to be active. ...
Opioid Dependence and Buprenorphine: An Update
Opioid Dependence and Buprenorphine: An Update

... Mu opioid receptors are distributed widely in the brain. While binding in the thalamus produces analgesia, binding in the cortex produces impaired thinking/balance; binding in prefrontal cortex contributes to an individual’s decision about how important use of the drug is to him/her (salient value o ...
Transnasal Drug Delivery
Transnasal Drug Delivery

... problems with the blood–brain barrier observed for drugs administered intravenously; however, this remains to be confirmed and quantified. Another distinct advantage of transnasal drug delivery over conventional oral drug administration in the form of drug-containing tablets and liquids is the avoid ...
PHARMACOKINETIC/PHARMACODYNAMIC (PK/PD) MODELING: AN INVESTIGATIONAL TOOL FOR DRUG DEVELOPMENT Review Article
PHARMACOKINETIC/PHARMACODYNAMIC (PK/PD) MODELING: AN INVESTIGATIONAL TOOL FOR DRUG DEVELOPMENT Review Article

... characterize and evaluate pharmacodynamic (PD) actions. These bio-mathematical models are the simplified forms of the phenomenon described in terms of an algebraic or differential equations. This PK/PD modeling not only describe, but also foretell about the distinct situations like allometric scalin ...
Presentation
Presentation

... Nonlinear fitting of the titration curves: where y – experimental fluorescence, F is a fluorescence scaling factor Kd - dissociation constant, P - total protein concentration (luciferase), Lt - the total ligand concentration (ANS), n – number of binding sites. ...
Study guide for research assistants
Study guide for research assistants

... Plasmodium cannot salvage pyrimidines, it explains why, among the enzymes of the de novo biosynthesis pathway, DHODH may have the most promise as a drug target. Materials and Methods • Chemical Library: The compounds "were selected for drug-like properties." This is important because the ultimate go ...


... excipients were taken as shown in Figure 1 it was found that all the peaks corresponding to the constituents were found to be present in its higher spectra indicating that none of the functional groups of either drug or polymer have undergone any chemical reaction. All functional groups are intact. ...
Class Effects Definition?
Class Effects Definition?

... – Regulatory agencies utilize the concepts of biomarker and outcome subclasses. Drugs are registered whenever possible based upon proven clinical outcomes - that is, membership of a particular outcome subclass. If such outcome data is unavailable drugs may be registered on the basis of biomarkers us ...
Acaisia - Acacia Pharma
Acaisia - Acacia Pharma

... Drug/ delivery ...
3-Hydroxy-N-Methylpyrrolidone and Use as
3-Hydroxy-N-Methylpyrrolidone and Use as

... with agitation and at an elevated temperature, liquid dermal formulation, affects the skin of a human by in bromine is slowly added. The temperature may be con creasing permeability of the skin to allow more of a trolled in the preferred range by the rate of addition of drug to be absorbed in a shor ...
Interaction of cycloheximide with 25S ribosomal RNA from yeast
Interaction of cycloheximide with 25S ribosomal RNA from yeast

... primary structure from that of its counterpart in K. lact i s . The above observations suggest that the ribosomal domain that is, in S.cerevisiae, involved with the interaction of cyclEheximide contains ribosomal protein L41. It is likely, however. that the actual binding site for the drug is locate ...
formulation and evaluation of aceclofenac sodium effervescent taste
formulation and evaluation of aceclofenac sodium effervescent taste

... granules enhanced the disintegration and dissolution rates, along with taste masking of the selected drug. Key words: Aceclofenac sodium, Taste masking, Eudragit E-100, Effervescent Granules. INTRODUCTION Effervescent granules contain acid substances and carbonates or bicarbonates which react rapidl ...
Hemoglobin and Cytochrome c
Hemoglobin and Cytochrome c

... protein (or another protein) which INDUCES a change in shape in another part of the same molecule (or another molecule) Allosteric interactions typically occur when a specific small molecule, called an allosteric modulator or allosteric effector, binds to a protein (often an enzyme) and modulates it ...
Shiseido and Nihon Schering have concluded a joint business
Shiseido and Nihon Schering have concluded a joint business

... beauty foods and over-the-counter drugs) and frontier science business (medical-use pharmaceuticals, aesthetic treatments, chromatography and raw materials). In the pharmaceuticals business, Shiseido established Shiseido Pharmaceuticals Co., Ltd. in 1987 and subsequently entered the over-the-counter ...
Controlled Release of Naproxen Sodium from
Controlled Release of Naproxen Sodium from

Anti-Protozoal and Anthelmintic Drugs
Anti-Protozoal and Anthelmintic Drugs

... Chemotherapy for Malaria: Life cycle of Malaria parasite: An infected female anopheles mosquito injects sporozoites. Sporozoites migrate to the liver, where they form merozoites. Merozoites are released and invade red blood cells. In RBC, the merozoite becomes a trophozoite.The trophozoite multiplie ...
ANGIOTENSIN CONVERTING ENZYME (ACE) INHIBITORS
ANGIOTENSIN CONVERTING ENZYME (ACE) INHIBITORS

... with naturally long-acting drugs or sustained release formulations. Since peripheral oedema is a consequence of disturbance of the microcirculation, prescription of a diuretic is not helpful. The combined pre-capillary and post-capillary action of lercanidipine may reduce the frequency of this side ...
Development and in-vitro characterization of sustained release
Development and in-vitro characterization of sustained release

... systemic circulation, Sustained release tablets come in handy as a solution. A sustained-release dosage form is defined as “any drug or dosage form modification that prolongs the therapeutic activity of the drug” [1]. The primary objectives of sustained drug delivery are to ensure safety and enhance ...
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Drug design



Drug design, sometimes referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target. The drug is most commonly an organic small molecule that activates or inhibits the function of a biomolecule such as a protein, which in turn results in a therapeutic benefit to the patient. In the most basic sense, drug design involves the design of molecules that are complementary in shape and charge to the biomolecular target with which they interact and therefore will bind to it. Drug design frequently but not necessarily relies on computer modeling techniques. This type of modeling is often referred to as computer-aided drug design. Finally, drug design that relies on the knowledge of the three-dimensional structure of the biomolecular target is known as structure-based drug design. In addition to small molecules, biopharmaceuticals and especially therapeutic antibodies are an increasingly important class of drugs and computational methods for improving the affinity, selectivity, and stability of these protein-based therapeutics have also been developed.The phrase ""drug design"" is to some extent a misnomer. A more accurate term is ligand design (i.e., design of a molecule that will bind tightly to its target). Although design techniques for prediction of binding affinity are reasonably successful, there are many other properties, such as bioavailability, metabolic half-life, side effects, etc., that first must be optimized before a ligand can become a safe and efficacious drug. These other characteristics are often difficult to predict with rational design techniques. Nevertheless, due to high attrition rates, especially during clinical phases of drug development, more attention is being focused early in the drug design process on selecting candidate drugs whose physicochemical properties are predicted to result in fewer complications during development and hence more likely to lead to an approved, marketed drug. Furthermore, in vitro experiments complemented with computation methods are increasingly used in early drug discovery to select compounds with more favorable ADME (absorption, distribution, metabolism, and excretion) and toxicological profiles.
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