NOTHING IS REAL! EXAM 1 REVIEW Flashcards
Antigens are recognized with high affinity by antibodies because
the sequences of three hypervariable loops are selected in an immune response to exquisitely complement the 3D shape of the antigen.
kcat is what type of parameter?
Kinetic rate constant independent of enzyme or substrate concentration
Change in Km
noncompetitive (mixed)
Change in Km and Vmax
uncompetitive
change Vmax
competitive
The assigned reading “Therapeutic monoclonal antibodies,” describes several types of engineered antibody molecules that have been developed for therapeutics. Which of the names below DOES refer to a type of therapeutic monoclonal antibody?
Fab, BiTE, scFv
Twelve domains compose an IgG molecule. Of these domains,
all have two or more cysteine residues.
Ig chains
4: 2 heavy 2 light
Ig fold (Domain)
-sandwich of 2 antiparallel B-sheets
-disulfide bond linkage
-hydrophobic residues
-connected to each other by loops = flexible
Substrate enzyme interactions
-hydrophobic to hydrophobic
-H bonding
-coloumbic
KI
-dissociation constant
-analogous to KD
-low=more affinity
Cheng-Prusoff
relationship btw Ki and IC50
The development of an allosteric drug is attractive because
it is possible to consider ACTIVATING an enzyme target in treating a disease.
Darunavir
interacts with polypeptide backbone and catalytic asp residues from each subunit of HIV protease
The basis for selectivity of certain NSAIDS, such as celecoxib, for COX-2 over COX-1 is
the spatial complementarity between the inhibitor and COX-1 is poor
HIV protease
-homodimer
-heme group
-aspartic
Aspirin vs everything else on COX
acetylates SERINE residue near active site to block access
Mech-based inhibitors
-2-thioxanthines on MPO
TX2 on MPO
covalently bonded to heme via thioether bond
NSAIDs
block prostaglandin
COX-2 vs COX-1
small Valine residue
steric hinderance
Allosteric inhibitor kinetics
typically mixed
Allosteric inhibition
increase Km
Cytochrome inhibitor
-increase bioavailability/plasma levels of drug
-drug more potent