Classical Target Drug Receptors

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Classical Target Drug Receptors

Nuclear

Might contain or have a non-genomic target interacting directly with cytosolic proteins

subfamilies

Class III

small includes receptors for

Vit. D receptor

Thyroid hormones

form obligate heterodimers with RXR

Hybrid class

Class II

include receptors for

xenobiotic

Cyt. P3A for metabolization of drugs

cholesterol

fatty acids

form heterodimers with RXR (retinoid x receptor)

found in nucleus

Class I

primary receptors to steroid hormones

estrogen, progesterone, and androgen

mineralocorticoids

glucocorticoids

form homodimers

found in cytoplasm

response time: hours to days

function

modulates transcription

directly interact with DNA

monomeric

no transmembrane domain

thus separate receptor and DNA binding domains

found in cytoplasm or nucleus of cell

do not reside in membrane

Kinase-Linked

Kinase Receptors

Cytokine Receptors

associated with cytosolic tyrosine kinases (JAK)

no intrinsic kinase activity

Serine/Threonine Kinase

TFG receptor

RTK

TLRs

bacterial infection mediate response

growth factor receptors (EGF and NGF)

End Result: activation or inhibition of nuclear transcription factors by:

suppression or activation of target genes

Ligands

hormones

types

bacterial lipopolysaccharides

insulin

cytokines

growth factors

Function in controlling:

immune response

apoptosis

cell cycle progression

tissue repair

inflammation

response time: hours

1

GPCR

desensitization

Receptor internalization

endocytosis

downregulation of receptor

phosphorylation

Protein Kinase A and C

nonspecific kinases

threorine and serine

GPCR Subfamilies

Subtopic

metabotropic Glu Receptor/Ca Sensor

small groups

GABAb receptors

Secretin/glucagon

intermediate EC tail

peptide hormones

calcitonin

Rhodopsin

short EXC tail on N-terminal

ligands bind to helices of EXC hoops

largest group

purines

neuropeptides

amine neurotransmitters

protanoids and cannabinoids

GPCR ligands

Act on different types of receptors

5-HT

ACh

Opioids

Dopamine

fast response: seconds

composition

7

C-terminal

N-terminal

Ligand-Gated

other biological ligands

respond to intracellular binding signals

atp recepots

calcium binding receptors

arachadonic acid sensitive receptors

selective channels

Cation selective pores

anion selective pores

Receptors

GABA

mediate chloride transport

Receptos

5-HT3 receptors

drug target of psychoactive drugs

fast response: milliseconds

Composition

transmembrane domain

4

cytoplasmic domain

extracellular domain

membrane bound