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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.
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