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drug discovery > 3🅱️ > Flashcards

3🅱️ Flashcards

1
Q

new trends // targets

A

targeting protein protein interactions that were considered undruggable

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2
Q

lipinskis rule is whattt

A

a rule of thumb!!
also a rule of 5 🤞🏼

getting violated by many newish drugs that are large complex natural products

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3
Q

why the 5 lipinskis rules

A

drug discovery companies limit themselves to these rules as small molecules that violate these rules tend to be too toxic in general

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4
Q

name the 5 lipinski rules

A
  • no more than 5 H bond donors in a molecule
  • no more that 10 H bond acceptors in the molecule (O + Ns in total)
  • molecular mass less than 500amu
  • octanol // water partition coefficient (Clog P) that does not exceed 5)
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5
Q

molecules that obey lipinskis rule are said to be

A

‘druglike’

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6
Q

name some biologics

A

proteins
hormones
antibodies
vaccines
gene therapy (vaccines)

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7
Q

recombinant proteins

A

insulin hormone

controls glucose absorption from blood

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8
Q

what leads to autoimmune diseases

A

over activity of the immune system can lead to autoimmune disorders

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9
Q

name some autoimmune disorders

A
  • rheumatoid arthritis
  • psoriasis
  • asthma
  • hay fever
  • crohn’s disease
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10
Q

what triggers an immune response

A

an antigen

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11
Q

killer cells in an immune response

A

a phagocyte

non specific

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12
Q

what is inflammation caused by

A

release of cytokines
from macrophages
in order to reduce damage from trauma

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13
Q

what is a cytokine

A

small signalling proteins secreted by certain cells of the immune + nervous system

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14
Q

what do cytokines activate

A

an immune response + inflammation

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15
Q

cytokine timeline ig

A

recognised by specific receptors on cell surfaces

the cytokine - receptor recognition system is targeted to suppress inflammatory diseases.

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16
Q

acute phase reaction

A

cytokine production by macrophages
inflammation

17
Q

structure of an antibody

A
  • variable region / portion
  • constant region / portion
  • light chain (outer + shorter)
  • heavy chain (inner + longer)
  • disulphide bond between heavy and light chain.
18
Q

polyclonal

A

different antibodies being produced by different b cells//leukocytes during an immune response to produce a large variety of binding regions // variable regions.

19
Q

antibody that comes from one b cell only

A

monoclonal antibody!!
same variable portion

20
Q

why are polyclonal antibodies not rlly good at inhibiting specific disease

A

they have different variable regions
therefore different effects

they therefore have unpredictable + inefficient pharmacological effects

21
Q

what are problems with monoclonal antibody production

A
  • cells undergo apoptosis + die after 50 divisions : need a cell that grows indefinitely
  • need to grow many IC in order to find effective antibodies
  • variable region must be human to target human cells.
  • constant region should be part animal,, variable region should be part human. this is bc human immune system recognised the heavy chain + led to an immune effect (part human part animal). ANTIBODY SHOULD BE CHIMERAS (part human and part animal)
22
Q

chimeras

A

antibody is split
- variable region + human
- constant region + animal

bc constant regions,, if human can be recognised by the human immune system + trigger an immune response

23
Q

monoclonal antibody production

A
  • mouse immunised by antigen + it’s spleen produces plasma cells that secrete specific antibodies
  • myeloma cells that can’t product antibodies are selected
  • plasma cells from spleen and myeloma cells fuse -> hybridomas.
  • infused cells die
  • cell transferred to a medium
  • hybridomas (plasma X myeloma) are bulk grown (it selected)
24
Q

how many of the top 10 best selling drugs are small molecules

A

only 2 of the top 10!! m

eliquis
biktarvy

25
Q

problems with monoclonal antibodies

A
  • they’re proteins,, they cannot lass the digestive system (must be injected)
  • expensive to produce (small molecules would be cheaper to produce)
26
Q

what is the current drug market dominated by

A

dominated by expensive biologics for first world health conditions.

cancer + diabetes

drug discovery (18 decks)

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