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PHAL221 > Drug action > Flashcards

Drug action Flashcards

1
Q

types of receptors

A

enzymes, GPCRs, VGIC, LGIC, carriers, transporters

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2
Q

receptors as drug targets

A

1/3 of drugs target receptors
1000 receptor proteins
several binding sites, bind ligands and release unchanged

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3
Q

trends in indications

A

analgesics constant

diabetes drug increasing, plus alzheimers and obesity

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4
Q

trends in classes of target

A

growing in ligands and serine/RTKs
LGIC already found lots of targets
lots of GPCRs unexplored (100/400 non-olfactory) - orphan

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5
Q

orphan GPCRs

A

not matched to endogenous ligand

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6
Q

trends in molecule type

A

small molecules are more common moving more diverse - proteins, peptides, antibodies, etc

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7
Q

tends in mode of action

A

antagonists and agonists common moving to positive/negative allosteric modulator and biased drugs

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8
Q

allosteric modulator

A

bind elsewhere on receptor to change response to orthosteric ligand
can be more specific to one receptor subtype = more diverse

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9
Q

biased ligands

A

agonist -> unique conformation of receptor -> activate only certain signalling molecules
fewer side effects
eg opioid -> don’t activate arresting, only g protein

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10
Q

future of drug discovery

A

robust target validation (cause and causation)
better understanding of pharmacological targets
broad view of potential targets, molecule types, modes of action

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11
Q

allosteric agonist

A

bind allosterically and directly activate/inactivate the receptor

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12
Q

proteins

A

catalysts, receptors, scaffolding, transport, communication

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13
Q

proteins as drugs

A

cannot mimic with simple chemicals
less potential to interfere with normal biological processes
well tolerated, no immune response
replace deficient or abnormal protein, augment existing pathway

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14
Q

making protein biologics

A

PCR -> select vector -> recombinant vector -> organism -> selection and sequencing -> expression -> purify

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15
Q

production systems

A

bacteria, yeast, mammalian cells, transgenic animals

consider cost and PTMs

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16
Q

interferons

A

produced by any cell in response to virus infection

activates antiviral response and stops spread

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17
Q

recombinant interferons

A

produce in mammalian cells for glycosylation
coagulation to polyethylene glycol and glycoengineering to improve Vd, clearance and half life
inject into body for viral clearance/milder disease

18
Q

monoclonal antibodies

A

antibody made from cloning a unique white blood cell to substitute antibodies
interfere with growth factors, inflammatory cytokines, immune cells
deliver compounds and proteins

19
Q

interferons vs antibodies

A

antigens stimulate production of antibodies from B cells -> remove antigen
interferons are antiviral glycoproteins released by cells under viral attack -> viral resistance

20
Q

antibodies

A

proteins produced by immune cells in response to foreign antigens (microbes, human proteins or cells)
antigen detected by T cell -> activate B cells -> clone plasma cells -> secreted antibodies
bind to block antigens action

21
Q

making monoclonal antibodies

A

take B cells from animals and grow to find best via Fc domain (hybridoma)
use phage display (screening for best binding)
transgenic mice with human immune cells (screen B cells)
remove human B cells -> production of cell lines

22
Q

chimeric and humanised

A

chimeric - clone variable domain (-ximab)
humanised - take antigen recognition domain (-zumab)
or recombinant

23
Q

biologics examples

A

tumor necrosis factor - cytokine produced for tissue damage/infection -> cell death, inflammation etc.
anti-TNF (covid) monoclonal antibodies - humanised adalimumab (less immunogenic)

24
Q

biologics challenges

A

complex to make, difficult to deliver, have multiple effects and are expensive to use

25
Q

stem cells

A

can divide infinitely and differentiate to specialised cells

26
Q

pluripotent

A

can turn into all cell types (embryonic)

27
Q

multipotent

A

can specialise to only some cell types (adult)

28
Q

embryonic stem cells

A

early blastocyst stage of embryo
can be made from IVF (donated) -> made into cell lines -> somatic nuclear transfer
pluripotent

29
Q

adult stem cells

A

replenish cells and repair tissue damage

teeth, bone marrow, spinal cord, pancreas, blood vessels

30
Q

hematopoietic stem cells (HSC)

A

bone marrow stromal cells

differentiate into every type of blood cell

31
Q

mesenchymal stem cells (MSC)

A

bone marrow adherent cell layer + adipose + umbilical cord blood
-> fat, bone, cartilage, endothelial, muscle cells and immunomodulation

32
Q

ethics for embryonic stem cells

A

different for different cell types
destroy embryo
depends on when religion thinks life begins
many guidelines to follow - in NZ allowed for scientific and clinical research
some clinic offer unapproved products

33
Q

umbilical cord stem cells

A

obtained at birth
adult stem cells (MSC)
higher proliferation, immunological immaturity, less exposure to viruses/aging

34
Q

adipose derived stem cells

A

liposuction, cultured for isolation

35
Q

neuronal stem cells

A

bone marrow

CNS -> neurons, astrocytes, oligodendrocytes

36
Q

epidermal stem cells

A

hair follicle, hair regeneration and shedding, regrow epidermis

37
Q

induced pluripotent stem cells

A

normal adult cell -> stem cell
ESGs behaviour
delivered 3-4 transcription factors
concerns - genetic faults conserved, reduced longevity, cancer

38
Q

stem cell use

A

basic research, disease models, cell replacement therapy, cell regulatory therapies

39
Q

stem cell transplants

A 
bone marrow (relatives -> no immune reaction)
cord blood (frozen when born -> immune deficiency, blood disease)
skin grafts - biopsies from same patient = autologous -> skin cell colonies + structural support -> grafted
40
Q

arthritis stem cell therapy

A

rheumatoid (bone and cartilage wears) -> inject MSCs into joint -> T and B cell signalling/cytokine production, one dose = 6 months effectiveness
use extracellular vesicles and understand biology better, long range effects, costly
Osteoarthritis (break down cartilage and miniscus, ossification) > transplant byline and collagen cartilage, lasts 2 years

PHAL221 (5 decks)

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