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Topic 1 Organic Structures and Interactions of Drugs
Topic 1 Organic Structures and Interactions of Drugs

... the cell, preventing the passage of water and polar molecules ...
Lecture 13 M230 Feigon
Lecture 13 M230 Feigon

... Crosspeaks between iminos give sequential connectivities along each ‘strand’. ...
Foundations in Microbiology - Houston Community College System
Foundations in Microbiology - Houston Community College System

... • may block synthesis of nucleotides, inhibit replication, or stop transcription • Sulfonamides and trimethoprim block enzymes required for tetrahydrofolate synthesis needed for DNA & RNA synthesis. • competitive inhibition – drug competes with normal substrate for enzyme’s active site • synergistic ...
HIV and AIDs
HIV and AIDs

... Cytotoxic T cells (also known as killer T cells) bind cells that have been altered, such as by viral infection; they avoid healthy cells. Surface antigens on the altered cell perform the binding. These antigens are specific to the offending agent, and match receptors in the membrane of the specific ...
10-6-2016 PPT
10-6-2016 PPT

...  In the aspirin phenytoin example, aspirin increased the fup of phenytoin. Why was the LD not changed?  In the aspirin phenytoin example, aspirin increase the fup of phenytoin. Why was the MD not changed?  If fu increases, what happens to Clu? CL?  What is CLu a measure of? ...
Pharmacodynamics
Pharmacodynamics

... A macromolecular component of the organism that binds the drug and initiates its effect. ...
(Agonist) of Nuclear Receptor
(Agonist) of Nuclear Receptor

... A macromolecular component of the organism that binds the drug and initiates its effect. ...
WHAT`S THE NEXT STEP?
WHAT`S THE NEXT STEP?

... Ritonavir decreases metabolism of fluticasone which is a CYP3A4 substrate. There is more fluticasone in the body which binds to GR and increases DNA modulation. These modulations can lead to Cushing's Syndrome. ...


... trapped by covalently (but reversibly) linked topoisomerases, the function of which is compromised26–28. As a result of quinolone–topoisomerase–DNA complex formation, the DNA replication machinery becomes arrested at blocked replication forks, leading to inhibition of DNA synthesis, which immediatel ...
P vivax
P vivax

... TE3, a prodrug of a bis-ammonium compound that acts on phospholipid metabolism through the inhibition of de novo phosphatidylcholine synthesis, combined with a putative activity on heme detoxification. This new class of compounds has shown potent in vivo antimalarial activity in the primatemodel Aot ...
HIVART_9 - I-Tech
HIVART_9 - I-Tech

... Get advice from experienced clinicians Consider resistance testing if available Premature changing in ARV can limit future options ...
Novel Therapies and New Targets of Treatment for Familial
Novel Therapies and New Targets of Treatment for Familial

... FAHA, FNLA Associate Professor of Medicine Washington University School of Medicine May 16, 2010 ...
Mebendazole
Mebendazole

... CO H N ...
A Map to Learn your Way around Antibioticland
A Map to Learn your Way around Antibioticland

... “You have to run towards where the ball is going to be.” Yogi Berra ...
Acute Coronary Syndrome Therapeutic Intervention
Acute Coronary Syndrome Therapeutic Intervention

... 2. In order to activate the plasminogen into its active form; Plasmin, human kidneys secrete an enzyme called Urokinase. Urokinase will cleave the Plasminogen to Plasmin through proteolytic mechanism 3. Nevertheless, activated plasmin is vulnerable to be deactivated by plasma AntiPlasmin which can r ...
Test Set - Focus Synthesis LLC
Test Set - Focus Synthesis LLC

... Affinity (PLogIC50) is significantly higher in a diverse Test Set of 80 ligands ...
DISCOVERY OF NOVEL IKK-Β INHIBITOR BY STRUCTURAL MODIFICATIONS OF
DISCOVERY OF NOVEL IKK-Β INHIBITOR BY STRUCTURAL MODIFICATIONS OF

... Objective: Diabetes Mellitus (Type II) is one of the predominant diseases which has seen rise globally. Kappa-B kinase beta (IKK-β) - a protein subunit of IKappa-B kinase, is an emerging target for treatment of non-insulin dependent diabetes mellitus (NIDDM). Chlorpropamide(diabinese) and nateglinid ...
Urinary Antiseptics
Urinary Antiseptics

... Taken orally excreted unchanged in urine where these drugs are bactericidal for some Gm –ive bacteria when pH is less than 5.5 ...
Efficacy of Antiviral Drugs against Feline Immunodeficiency Virus
Efficacy of Antiviral Drugs against Feline Immunodeficiency Virus

... sodium salt), a sulfated naphthylamine and trypan red derivative, is one of the oldest known antimicrobial agents. It has been used as an antitrypanosomal agent and for the treatment of some tumors, such as prostate cancer [58]. It also has an inhibitory effect on the RT activity of retroviruses and ...
Are all angiotensin-converting enzyme inhibitors
Are all angiotensin-converting enzyme inhibitors

... definition of the term “class effect.” Although members of a drug class share main actions, they may have clinically important differences in terms of efficacy and safety. There are many such examples in the literature. This article reviews the class effect concept as it applies to the angiotensin-c ...
informational handout - Western Connecticut State University
informational handout - Western Connecticut State University

... activity by binding to bacterial ribosomes and preventing the initiation of protein synthesis. They've been used against a wide variety of bacterial infections caused by Gram-positive and Gram-negative bacteria. Streptomycin has been used extensively as a primary drug in the treatment of tuberculosi ...
CLINICAL PHARMACOLOGY OF DRUGS AFFECTING THE
CLINICAL PHARMACOLOGY OF DRUGS AFFECTING THE

... metabolized to trichloroacetic acid, which is toxic and may accumulate); mechanism of action is not known ...
Effect of protein binding on PK/PD
Effect of protein binding on PK/PD

... With two sites per albumin molecule, the drug-binding capacity of plasma albumin would therefore be about 1.2 mmol/L. ...
23  REVIEW ARTICLE
23 REVIEW ARTICLE

... The structure of quinolone pharmacophore was shown in Fig. 3 The figure shows the core molecule and the positions at which key changes are engineered. Some of these molecular substitutions should not be altered as they would interface with or reduce markedly the basic mode of action of the drug. The ...
Docking and Drug Design
Docking and Drug Design

... • Ligands that bind to a specific protein • Either increase its activity (an agonist) ­­or­­ decrease/block its activity (an antagonist) • Many problems… solubility, stability, selectivity • Most drugs are not very selective… side effects • Rational drug design… exploit structure of the protein and  ...
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Discovery and development of integrase inhibitors

The first human immunodeficiency virus (HIV) case was reported in the United States in the early 1980s. Many drugs have been discovered to treat the disease but mutations in the virus and resistance to the drugs make development difficult. Integrase is a viral enzyme that integrates retroviral DNA into the host cell genome. Integrase inhibitors are a new class of drugs used in the treatment of HIV. The first integrase inhibitor, raltegravir, was approved in 2007 and other drugs were in clinical trials in 2011.
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