Lecture 9

Question 0

Theranostics

Answer 0

Patients with positive imaging results can be treated with therapeutic agent. Patients with negative results will not be treated with targeted agent

Question 1

Phenotypic screening

Answer 1

Speeds up physiochemical property optimization.

Provide leads for conditions that don’t have known targets

Question 2

Reverse pharmacology

Answer 2

ID of the biomolecular targets of efficacious agents with unknown mechanisms of action

Question 3

Bypass genetics

Answer 3

Exposes a protein to a small molecule and absurd Suffex.

Identifies both a target and hit Compound at the same time

Question 4

Tubulin

Answer 4

Inhibiting microtubule polymerization so it’s a target for anticancer drugs like paclitaxel
Geldanamycin, brefeldin A, isogranulatimide: ID by phenotypic effects

Question 5

Proteomics

Answer 5

Provides a protein profile of cell, tissue or bodily fluids that can be used to compare between healthy and disease states.
Provides a comparative analysis of protein profiles and healthy and diseased states

Question 6

See an 15N shift

Answer 6

Overexpressed protein.
Purified protein.
Determine 3-D structure.
If structure determined screen 1000 compound a day

Question 7

ID a potent and selective inhibitor

Answer 7

Screen for the first ligand. 
Optimize the first ligand. 
Screen for the second ligand. 
Optimize the second ligand. 
Link the two Luganda

Question 8

Chelation therapeutics

Answer 8

Used for toxic accumulations of metals

Question 9

Inorganic chemo therapeutics

Answer 9

Consolation: acts by coordination of platinum atom to guanine forming a covalent bond

Question 10

Imaging agents

Answer 10

Designed to provide more information about internal organs or processes
Designed around metal elements that act as receptors and organic ligands that act as delivery vehicles
Examples: PET, MRI, SPECT, x-rays

Question 11

18FDG PET Imaging agent

Answer 11

Non-toxic.

Taken up by the cell with high glucose turnovers

Question 12

Gadolinium MRI Contrast Agents

Answer 12

Works due to the water molecule rapidly exchanging with nearby physiological water molecules.
Strong paramagnetic altering the MRI properties causing detectable changes.

Question 13

99mTC SPECT Radiotracer

Answer 13

Half-life allows for a relatively large synthesis, formant formulation, and application window.
Detects gamma emissions.
Excreted through urine, needs frequent urination to ensure no damage to bladder.
Do not use in pregnancy or lactation

Question 14

Barium meal crazy contrast agent

Answer 14

Used for esophagus, stomach and intestines.
Monitor progress of the barium through the digestive system to identify a blockage or other problem.
Non-toxic.
Uses oil

Question 15

Octahedral metal

Answer 15

Six different substitutes forming 30 different stereoisomers

Question 16

Ruthenium II

Answer 16

Possesses hexavalent coordination sphere.
Kinetically inert coordinated bonds.
Purely structural and not reactive

Question 17

Boron

Answer 17

Tri and tetravalent.
Conform additional covalent bonds with active site residuals.
Non-toxic.
Boron neutron capture therapy important treatment option for brain tumors.
Bortezomib relapsed multiple myeloma treatment.
First in class as a chemotherapy.
Acts as protease inhibitor forming covalent bonds in active site with high specificity and potency

Question 18

Magnetic nano particles

Answer 18

Can’t be manipulated by a magnetic field.
Mainly composed of Fe2O3.
Heat when exposed to an alternative magnetic field so they are used in an experimental process known as magnetic hypothermia to combat cancer