Medicinal Chemistry Encyclopedia

 

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Flow Cytometry is a method to study cell proliferation. Following laser excitation cells treated with certain fluorescent dyes that bind specifically to DNA, fluoresce with an intensity proportional to their DNA content. Deconvolution of the intensity permits the estimation of the fraction of cells in stages G1, S and G2 + M.

 

Fragment-Based drug discovery Approaches to assemble molecular fragments to create more potent and selective molecules. Fragment-based approaches have also been classified according to the path taken after the low molecular weight ligand is identified. If the fragment is optimized by adding functionality that binds adjacent regions in the protein cavity, the approach is referred to as fragment evolution. Fragment linking occurs when two or more fragments are linked together to deliver a larger, higher affinity binding molecule. Fragment self-assembly is done when fragments of complementary functionality bind in proximity to each other, and are allowed to react in the presence of the target, creating a larger molecule of increased potency. Any of these approaches may require fragment optimization to improve the drug-like characteristics of the fragments, in addition to its potency.

 

Gangliosid is a sphingolipid whose polar head is comprised of a polysaccharide.

 

Gene an ordered string of DNA nucleotides inherited from parents. Each gene has a unique location on a particular chromosome and acts as the blueprint for producing a specific protein when needed by the body.

 

Gene Mapping refers to ascertaining the exact location of a specific DNA sequence on one of the 23 pairs of chromosomes that comprise our genome.

 

Gene Therapy After the exact location of a specific DNA sequence on one of the 23 pairs of chromosomes is known, the goal of Gene Therapy is to replace an individuals damaged or missing gene. The result is a partially or completely restoration of the intended function. Transferring new DNA or a complete gene in to the afflicted individual accomplishes this.

 

Genome is the complete set of chromosomal and extrachromosomal genes of an organism, a cell, an organelle or a virus; the complete DNA (deoxyribonucleic acid) component of an organism.

 

GMP is an abbreviation for Good Manufacturing Practices. Good Manufacturing Practices are regulations published by the Food and Drug Administration (FDA) to provide criteria for complying with provisions of the Federal Food, Drug, and Cosmetic Act (FD&C Act) requiring all human foods to be free from adulteration.  

 

GPCR is an abbreviation for G-Protein Coupled Receptors.

 

Granulocyte: a type of white blood cell filled with granules of compounds that digest microorganisms. Granulocytes are part of the innate immune system (see Immune System) and have broad-based activity. They do not respond only to specific antigens as do B-cells and T-cells. Basophils, eosinophils and neutrophils are all granulocytes.

 

Granulocytopenia: an abnormally low number of granulocytes in the blood, which increases risk of severe bacterial infection.

 

Growth Factor: one of many intercellular regulatory molecules that affect cell proliferation (rapid and repeated reproduction) and maturation in specific tissues.

 

Hansch analysis is the investigation of the quantitative relationship between the biological activity of a series of compounds and their physicochemical substituent or global parameters representing hydrophobic, electronic, steric and other effects using multiple regression correlation methodology.

 

Hapten is a low molecular weight molecule that contains an antigenic determinant but which is not itself antigenic unless combined with an antigenic carrier.

 

Hard drug is a nonmetabolizable compound, characterized either by high lipid solubility and accumulation in adipose tissues and organelles, or by high water solubility. In the lay press the term .Hard Drug. refers to a powerful drug of abuse such as cocaine or heroin.

 

Hepatitis A is a self-limiting virus-induced liver disease. Hepatitis A is acquired through ingesting fecally contaminated water or food or engaging in sexual practices involving anal contact. Injection drug users who share unclean needles also are at risk.

 

Hepatitis B is a virus-induced liver disease that usually lasts no more than six months, but becomes chronic and life threatening in ten percent of the cases. The highly contagious hepatitis B virus can be transmitted through sexual contact, contaminated syringes and blood transfusions.

 

Hepatitis C is another virus-induced liver disease. It appears to be more common among heterosexuals and injection drug users than hepatitis B.

 

Hepatomegaly refers to liver enlargement.

 

Hepatotoxicity refers to toxicity to the liver.

 

HERG The human ether-à-go-go-related gene (hERG) and KvLQT1 gene encode pore-forming proteins that are thought to represent the a-subunits of the human potassium channels. These subunit proteins can form hetero-oligomeric complexes with auxiliary b-subunits (i.e. MiRP and MinK gene products), which have been speculated to modulate the gating properties of the channel proteins. Inhibition of the delayed rectifier potassium channel appears to be the most common mechanism of QT interval prolongation by pharmaceuticals. The QT interval (time from the beginning of the QRS complex to the end of the T wave) of the electrocardiogram (ECG) is a measure of the duration of ventricular depolarization and repolarization. QT interval prolongation can be congenital or acquired (e.g., pharmaceutical-induced). When the QT interval is prolonged, there is an increased risk of ventricular tachyarrhythmia, including torsade de pointes, particularly when combined with other risk factors (e.g., hypokalemia, structural heart disease, bradycardia). Thus, much emphasis has been placed on the potential proarrhythmic effects of pharmaceuticals that are associated with QT interval prolongation.

 

Herpes Virus is a group of viruses that include herpes simplex type 1 (HSV-1), herpes simplex type 2 (HSV-2), cytomegalovirus (CMV), Epstein-Barr virus (EBV), varicella zoster virus (VZV) and human herpes virus type 6 (HHV-6). Herpes simplex virus 1 (HSV-1) can cause painful .cold sores. or .fever blisters. on the lips, in the mouth or around the eyes; herpes simplex virus 2 (HSV2) is usually transmitted sexually and generally causes lesions in the anus or the genital area. See names of individual viruses.

 

Heterocycle are ring systems containing atoms other than carbon. [TABLE OF RINGS]

 

Heteroreceptor is a receptor regulating the synthesis and/or the release of mediators other than its own ligand (See also Autoreceptor).

 

Hill Coefficient or Hill Plot is a means to infer cooperativity effects from binding data, i.e. if the binding to one receptor site facilitates the binding to subsequent receptor sites in the same population. The equation is deduced from the binding constant assuming the existence of multiple sites on the receptor.

 

Homologue is used to describe a compound belonging to a series of compounds differing from each other by a repeating unit, such as a methylene group, a peptide residue, etc.

 

Hormone is a substance produced by endocrine glands, released in very low concentration into the bloodstream, and which exerts regulatory effects on specific organs or tissues distant from the site of secretion.

 

Hydrogen Bond is a relatively weak bond of 20-30 kJ/mol formed by a shared proton hydrogen atom located between two electronegative atoms. The strength of the bond increases with an increase in the electronegativity or a decrease in the size of the participating atoms.

 

Hydrophilicity is the tendency of a molecule to be solvated by water.

 

Hydrophobicity is the association of non-polar groups or molecules in an aqueous environment which arises from the tendency of water to exclude non polar molecules. (See also Lipophilicity).

 

Hyperplasia: excessive growth of normal cells.

 

Hypertension: high blood pressure.