Cancer Treatments and Pharmacology Flashcards - lect 19

Flashcards on Cancer Treatments and Pharmacology

Intercalators

Compounds with extended PI systems that can intercalate with DNA and are used in both antimicrobial and anticancer treatments.

Doxorubicin

An anticancer compound with an extended PI system, often formulated in a liposome due to poor oral availability, used to treat a wide spectrum of cancers.

Topoisomerase Inhibition

Inhibition of this process interferes with cell replication, distinguishing cancer cells from normal cells based on their rapid multiplication.

Dihydrofolate Reductase

Enzyme involved in the redox process within the folic acid pathway; inhibited by methotrexate.

Methotrexate

A compound that inhibits dihydrofolate reductase, an enzyme involved in the folic acid pathway, can actually be given orally, despite violating Lipinski's rules.

Target Enzyme

Enzymes convert DUMP to DTMP, targeted by five fluorosyl compounds.

Fluorine

A bioisostere for hydrogen that replaces hydrogen in uracil; gets incorporated into DNA, leading to cell death.

Raloxifene

Mimics estradiol, binds more strongly to the oestrogen receptor, and acts as a competitive inhibitor to stop cancer cell replication.

Percy Love Julian

Took plant oils and turned them into oestrogen and progesterone and paved the way for, as I said, a contraceptive pill and other innovations.

Physos

Used for treating glaucoma and as an antidote to systemic poisons; inhibits anti-cholesterolemin.

Microtubules

Protein-based structures that form spindles during cell replication; can be inhibited by natural compounds.

Vincristine

Natural compound from Madagascar that inhibits microtubule formation, raising ethical questions about patenting natural resources.

Kinases

Enzymes that add phosphate groups to hydroxy groups, activating or inactivating other enzymes involved in gene transcription.

Type One Kinase Inhibitors

Drugs that bind directly to the active site of kinases.

Optimization

Process of adding chlorine and fluorine to a lead compound to prevent metabolism, resulting in a longer-lasting drug.

Rigidification

Concept of locking a drug into its active confirmation to improve potency by restricting rotation about single bonds.

Allosteric Inhibition

Inhibition that occurs when a compound binds to a site other than the active site, affecting the protein's enzymatic ability.

Covalent RAS Inhibitors

Drugs that covalently bind to RAS to knock them out of the way, typically done by a conjugated addition.

Cribrion

The snippet of $170,000 per gram, Turned out to be creatine.

Antagonist

Blocks or interferes with the normal receptor or enzyme process.

Irreversible Antagonist

An antagonist binds covalently, they can't come off.

Reversible Antagonist

A drug that comes on and off a site.

Competitive Antagonist

They compete for the site.

Non Competitive antagonist

Go in for an allosteric site

EC50

The concentration where you get 50% of the maximal response.

Prazoxin

Acting at the alpha adrenergic receptor that competes with a natural agonist.

Partial Agonist

You can't overcome it because some of the time they're going have the partial agonist, so they're not going to be fully effective.

Chemical Antagonist

Change what your agonist is doing, for example, inactivating, a compound. So they're not acting on a receptor site but they're acting on your agonist, for example.

Physiological Antagonist

Might have compound which raises your blood pressure, your natural compound. You don't act on that or on those receptors, but you reduce the blood pressure through another mechanism.

Opioids

Morphine on the left, which, methadone is a second compound.