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SAR
or Quantitative Structure-Activity Relationships are
mathematical relationships linking chemical structure and pharmacological
activity in a quantitative manner for a series of compounds. Methods,
which can be used in QSAR, include various regression and pattern
recognition techniques.
Randomization:
the process by which patients in a clinical trial are randomly
assigned to different treatments Randomization minimizes the differences
among groups by equally distributing people with particular characteristics
among all the trial arms.
Randomized Trial:
a trial in which the participants are randomly assigned
to receive one of the treatments under study or a placebo. See
Randomization
Receptor
is a molecule or a polymeric structure in or on a cell that specifically
recognizes and binds a compound acting as a molecular messenger
(neurotransmitter, hormone, lymphokine, lectin, drug, etc.).
Receptor mapping
is the technique used to describe the geometric and/or electronic
features of a binding site when insufficient structural data for
this receptor or enzyme are available. Generally the active site
cavity is defined by comparing the superposition of active to that
of inactive molecules.
Recombinant DNA
(deoxyribonucleic acid)
molecules with different origins that have been joined to form a
new chimeric chain. It also refers to compounds (proteins) produced
by laboratory or industrial cultures of genetically engineered Iiving
cells. The cells. genes have been altered to give the capability
of producing large quantities of the desired compound for use as
a medical treatment.
Rectum: the
terminus of the large intestine including the anus.
Refractory: severe
disease that is resistant to treatment.
Remission: a
period when the signs of a disease have been eliminated through
treatment or the immune response. A disease may be in remission
without a complete cure having been effected.
Renal: of
or relating to the kidneys.
Resistance: reduction
in the sensitivity to a particular drug, common for antimicrobial,
antiviral or anticancer drugs. Resistance can arise by production
of enzyme that destroy the drug, changes in the permeability of
the cell membrane or bacterial wall; aleration of the structure
of the target for the drug, altered metabolic pathways, by pass
of the target of the drug. Resistance detected by searching a pathogen.
genetic makeup for mutations thought to confer lower susceptibility
is called genotypic resistance. Resistance found by successfully
growing laboratory cultures of the pathogen in the presence of a
drug is called phenotype resistance.
Retina: the
multilayered, light-sensitive membrane lining the inner eyeball
that sends visual images to the brain via the optic nerve.
Retinal Detachment:
a condition in which a portion of the retina becomes separated
from the inner wall of the eye. Retinal detachment can result from
retinal disease such as CMV retinitis (see). The condition
can rapidly lead to vision loss, but is treatable by adding silicone
to the eye.s vitreous humor (see) to increase the pressure
on the retina.
Retinitis: inflammation
of the retina, usually caused by infections such as CMV. If left
untreated, it can lead to blindness.
Retrovirus: a
type of virus that, when not infecting a cell, stores its genetic
information on a single-stranded RNA molecule instead of the more
usual double-stranded DNA. HIV is an example of a retrovirus. After
a retrovirus penetrates a cell, it constructs a DNA version of its
genes using a special enzyme, reverse transcriptase. This
DNA then becomes part of the cell.s genetic material.
Ribozyme is
a recombinant RNA/enzyme combination designed to fit onto
and cleave specific viral or cancerous genetic sequences from a
cell.s DNA.
Rule-of-five
is a rule that establishes that poor absorption or permeation of
drugs are more likely when there are 5 or more hydrogen bond donors,
10 or more hydrogen bond acceptors, logP is over 5 and the molecular
weight is over 500.
Salvage Therapy:
the final possible treatment for people who are nonresponsive
to or cannot tolerate other available treatments for a particular
condition.
Sarcoma: a
malignant tumor of the skin and soft tissue.
Scatchard equation
or Scatchard plot is a method to extract binding data.
Rearranging into a linear form the equilibrium constant and expressing
it in terms of the fraction of sites occupied by the drug. The slope
of the equation provides the reciprocal of the binding constant,
while the intercept of the abscissa is the number of binding sites.
Second messenger
is an intracellular metabolite or ion increasing or decreasing as
a response to the stimulation of receptors by agonists, considered
as the .first messenger.. This generic term usually does not prejudge
the rank order of intracellular biochemical events.
Septicemia: a
serious condition caused by large numbers of bacteria in the blood.
This condition can be fatal. Symptoms are a sudden drop in blood
pressure and changes in heart rate and temperature.
Serum is
the clear portion of the blood from which cellular components
have been removed
Single nucleotide
polymorphisms SNPs (pronounced .snips.) are
minute genetic variations that occur throughout human DNA.
Their value as genetic markers resides in their simplicity, frequency,
and relatively even distribution throughout the genome. Of the roughly
3-billion nucleotide pairs (i.e., the .letters.) that make up the
genetic code, it is estimated that a SNP.a single letter variation
in the code from one person to the next.occurs every thousand or
so nucleotide pairs.
Sinusitis is
an inflammation of the nasal cavity and sinuses.
Site-specific
delivery is an approach to target a drug to a specific
tissue, using prodrugs or antibody recognition systems.
Sphingolipid
is a complex lipid found in membranes of nerve and brain
tissue which contains three components, a sphingosine (long chain
amino alcohol) or one of its derivatives, a fatty acid and a polar
head group.
Spleen: a
large lymphatic organ in the upper left of the abdominal cavity
with several functions: 1) trapping of foreign matter in the blood,
2) destruction of degraded red blood cells and foreign matter by
macrophages, 3) formation of new lymphocytes and antibody production,
and 4) storage of excess red blood cells.
Soft drug
is a compound that is degraded in vivo to predictable non-toxic
and inactive metabolites, after having achieved its therapeutic
role.
Southern Blot
or DNA blot transfer is a series of techniques that allow the visualization
of specific DNA fragments. In the case where the procedure is carried
out on RNA, the technique is named a Northern Blot.
Stem Cell: the
precursor of all blood cells, which lives in the bone marrow. Clones
of stem cells may become any one of the repertoires of immune cells
depending upon what cytokines and hormones they are exposed to.
Steroids
are compounds based on the steran skeleton, a fully hydrogenated
cyclopentane phenantrene. Steroids are classified according to their
substitution patterns in Sterols, bile acids, estrogens, gestagens,
androgens, corticoids, cardenolids, sapogenins and steroid alkaloids.
[See figure]
Stomatitis: inflammation
of the mucous membranes in the mouth.
Structure-activity
relationship (SAR) is the relationship between chemical
structure and pharmacological activity for a series of compounds.
Structure-based
design (SAR) is a drug design strategy based on the 3D
structure of the target obtained by X-ray or NMR.
Structure-property
correlations refers to all statistical mathematical methods
used to correlate any structural property to any other property
(intrinsic, chemical or biological), using statistical regression
and pattern recognition techniques.
Subcutaneous:
injected directly under the skin.
Superoxide Dismutase
is one of the major cellular antioxidant
enzymes. It removes surplus peroxide, an oxidizing free radical
(see). Superoxide dismutase comes in two forms, one containing zinc
and the other containing manganese.
Surrogate Marker
A measurement of a drug.s biologic activity that substitutes for
a clinical endpoint such as death or pain relief.
Suicide Substrate
or Kcat substrate is an irreversible enzyme inhibitor that
binds covalently.
Symptomatology:
the collected symptoms of a particular disease.
Synergy: the
interaction of two or more treatments such that their combined effect
is greater than the sum of the individual effects observed when
each treatment is administered alone.
Systemic
means relating to or affecting the whole body. A systemic therapy
is one that the entire body is exposed to, rather than just the
target tissues affected by a disease.
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