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Drug Discovery1
Exam 1
26
Other
Undergraduate 4
02/12/2013

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Term
drug (2)
Definition
s chemical substance used in the treatment, cure, prevention, or diagnosis of disease or used to otherwise enhance physical or mental well-being
Term
druggable target (2)
Definition
a biological molecule such as a protein that is known to or is predicted to bind with high affinity to a drug.
Term
undruggable target (2)
Definition
no molecules can be identified that modulate a target of interest OR
-a potent and selective inhibitor is found against the target, but it has no effect on the disease for which it was intended
Term
mechanism of action (2)
Definition
the specific biochemical interaction through which a drug substance produces its pharmacological effect
Term
exon (3)
Definition
a sequence of DNA that codes information for protein synthesis that is transcribed to messenger RNA
Term
regulatory regions (3)
Definition
a segment of the DNA molecule which is capable of increasing or decreasing the transcription of specific genes
Term
SNPs - single nucleotide polymorphism (3)
Definition
a DNA sequence variation occurring when a single nucleotide differ between individuals
Term
oncogene (4)
Definition
a gene that causes normal cells to become cancerous either because the gene is mutated or because the gene is (over)-expressed at the wrong time in developement
Term
chromosomal translocation (4)
Definition
an abnormality caused by rearrangement of parts between chromosomes. a gene fusion may be created when the translocation joins two otherwise separated genes, the occurrence of which is common in cancer
Term
kinase (4)
Definition
an enzyme that catalyzes the transfer of a phosphate group from ATP to an accepter, usually another kinase
Term
kinome (5)
Definition
currently over 500 protein/lipid kinases that exist within the human genome
Term
kinase domains (5)
Definition
the N-terminal regulatory domain and the highly conserved C-terminal catalytic lobe common to all kinases
Term
Type I Kinase inhibitor (5)
Definition
binds to the ATP Binding site of the enzyme in its active form
Term
Type II Kinase inhibitor (5)
Definition
binds to the inactive form of the enzyme
Term
pleiotropy (6)
Definition
a drug's actions, usually unanticipated, other than those for which the agent was specifically developed. May include adverse side effects, but often used to denote beneficial effects
Term
enzyme (7)
Definition
protein molecules that manipulate other molecules (substrates). uses active site to bind target molecules and transform them into products through a series of steps (enzymatic mechanism)
Term
substrate (7)
Definition
the molecule upon which the enzyme acts in the chemical transformation of product formation
Term
kinetics (7)
Definition
the reaction rate of a chemical reaction that is catalyzed by an enzyme
Term
Vmax (7)
Definition
the maximum catalytic rate achieved at saturation
Term
Km (7)
Definition
the concentration of substrate that results in half the Vmax
Term
absorbance (7)
Definition
fraction of incident radiation (photon) absorbed by a molecule over a range of frequencies
Term
fluorescence (7)
Definition
the emission of light by a substance that has absorbed light or other energy
Term
stokes shift (7)
Definition
the difference in wavelength between the absorption and emission peaks
Term
Fluorescence Resonance Energy Transfer (FRET)
Definition
the fluorescence of an acceptor molecule is measured upon excitation by the fluorescence of a donor molecule
Term
HTRF Donor (7)
Definition
a molecule with a long-lived fluorescence signal (1-2 milliseconds)
Term
HTRF Acceptor (7)
Definition
a molecule with an absorption excitation spectrum that coincides with the emission spectrum of the TRF Donot
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