Med Chem Personally Made

What type of interactions do reversible inhibitors do?

Noncovalent

Is a reversible inhibitor in competition? If so, with what?

Yes. With Natural substrate

Does the reversible inhibitor undergo a reaction?

No

What does inhibition depend on in a reversible inhibitor?

The strength of inhibitor binding and concentration.

How can you reverse inhibition in a reversible inhibitor?

Increasing substrate concentration

What three things might a reversible inhibitor look like?

Substrate, Product, Cofactor

Where does the irreversible inhibitors bind?

The Active Site

What type of bond is formed in an irreversible inhibitor? What two things are bound?

Covalent. Drug and the enzyme.

Does increasing substrate concentration remove an irreversible inhibitor?

No

What will an irreversible inhibitors structure be similar to?

Substrate

What type of bonding does allosteric inhibitors do?

Noncovalent

What type of bonding does allosteric inhibitors do?

Noncovalent inhibitors

Allosteric inhibitors are not competitive, why is that?

The inhibitors performs induced fit therefore the enzyme changes shape. The substrate cannot bind.

What is unique about the shape of an allosteric inhibitor?

Not similar in structure to substrate.

What does a transition state inhibitor look like?

It mimics the transition state of an enzyme catalyzed reaction

Transition state inhibitors bind _____ than drugs that mimic the product or substrate.

stronger

What can’t you do to a transition state inhibitor?

Synthesize or isolate it

What are suicide substrates?

Agents that are converted to irreversible inhibitors by the enzyme catalyzed reaction

What do suicide substrates react with?

Target enzymes

Do suicide substrates bind reversible or irreversibly?

Irreversibly

What is an isozyme?

Different variant of the same enzyme

What are receptors activated by?

Chemical Messengers

What are two examples of chemical messengers?

Neurotransmitters and Hormones

What is signal transduction?

Chemical messages throughout the cell

Are messengers fast or slow?

Fast

What do agonists look like?

Natural messenger

What number is important with agonists?

Binding interactions

What is an antagonist?

Drug designed to block the natural messenger

How are antagonists different from agonists?

Antagonists have stronger binding reactions and do not activate receptor

How do agonists work?

They bind REVERSIBLY to binding side and produce same induced fit as natural messenger.

Do agonists activate the receptor?

Yes

What is an allosteric modulator?

Agents that enhance receptor activity by bunding to an allosteric binding site rather than the messenger binding site.

What type of bonding does reversible antagonists do?

Intermolecular / noncovalent

How does the receptor not activate with a reversible antagonist?

It’s a different induced fir than the normal messenger

What decides the level of reversible antagonism?

Strength of antagonist binding and concentration

Does increasing messenger concentration reverse reversible antagonists?

Yes

T or F: Antagonists use the same binding regions the natural messenger uses

False

How do irreversible antagonists bond?

Covalently

What are irreversible antagonists known for?

A label for receptors

How do allosteric antagonists bond?

Reversibly / noncovalently

Does increasing messenger concentration reverse antagonism in allosteric?

No

What is antagonists by the Umbrella effect?

Antagonist binds reversibly to a neighboring binding site, the antagonist overlaps the binding site for the messenger, its now blocked.

What is a partial agonist?

An agent that acts as an agonist but produce a weaker effect.

Why might partial agonists happen?

Not ideal IF, Agent beings to binding site as both antagonist and agonist, two different receptor subtypes