Endo, Topnotch Flashcards
Etymology of “hormone”
Hormaein meaning to arouse
Hormone classes (3)
1) Steroid
2) Protein
3) Tyrosine derivatives
Hormones that induce production of new protein from DNA
Steroid
Hormones that modify existing proteins
Protein hormones
Tyrosine-derived hormones (4)
1) NE
2) Epinephrine
3) T3
4) T4
T/F Thyroid hormones are lipid-soluble
T
G protein subunits
α, β, γ
G protein-coupled receptors are activated by
GTP
GTP is activated by
Guanine nucleotide exchange factors (GEFs)
GTP is inhibited by (2)
1) GTPase-accelerating proteins (GAPs)
2) RGS proteins (regulator of G protein signaling)
G protein subunit bound to GDP
α
Sequence of events upon binding of hormone to extracellular portion of G protein-coupled receptor
1) GDP > GTP
2) α-subunit dissociates from trimeric complex to associate with other signaling proteins
3) Signaling process terminated with removal of bound hormone
4) α-subunit inactivates itself
5) GTP > GDP
6) α-subunit combines with β- and γ-subunit
Signaling proteins associated with α-subunit alter activity of (2nd messengers)
1) Ion channels
2) Adenylyl cyclase
3) Phospholipase C
Activity of adenylyl cyclase
ATP > cAMP > activation of protein kinase A > downstream phosphorylation
Activity of phospholipase C
PIP2 (membrane phospholipid) > IP3 + DAG
Activity of IP3
Mobilizes Ca from mitochondria and ER > smooth muscle contraction or cell secretion
Activity of DAG
Activates PKC > phosphorylation of downstream proteins
2nd messenger that is the precursor of PGs and other local hormones
DAG
2nd messenger associated with αs- and αi-subunit
Adenylyl cyclase > cAMP > PKA
Activities of cAMP
1) Activation of PKA
2) Directly regulate ion channels
Enzyme for degradation of cAMP
Phosphodiesterase
αt-associated G protein is aka
Transducin
Activity of αt-subunit
Activates cGMP PDE > decreases cGMP > closes cGMP-dependent ion channels
α-subunit associated with phospholipase C
αq-subunit
Catalytic or enzyme-linked receptors (4)
1) Guanylyl cyclase
2) Serine/threonine kinase
3) Tyrosine kinase
4) Tyrosine-associated kinase
Downstream activity of receptor guanylyl cyclase
GTP > cGMP > protein kinase G > downstream phosphorylation
Ligands that bind to receptor guanylyl cyclase (2)
1) ANP
2) NO
3) EDRF
Receptor serine/threonine kinase: Subunit to which ligand binds
Type 1
Receptor serine/threonine kinase: Subunit that is phosphorylated with ligand binding
Type 2
Downstream activity of receptor serine/threonine kinase
Ligand binds to type 1 subunit > phosphorylation of serine/threonine residues on type 2 subunit > downstream activation of effectors
Ligand that binds to receptor serine/threonine kinase
TGF-β
Ligands that use receptor tyrosine kinase (5)
1) NGF
2) EGF
3) PDGF
4) IGF-1
5) Insulin
6) PRL
No intrinsic tyrosine kinase activity but associate with proteins that have tyrosine kinase activity
Tyrosine-associated kinase receptor
Receptor families associated with tyrosine-associated kinase receptor (2)
1) Src family
2) Janus family (JAK)
Hormones that have tyrosine-associated kinase receptor, JAK
1) EPO
2) GH
Hormone whose receptor has 2 beta chains attached together by sulphide bonds
Insulin
cAMP vs IP3/DAG: ADH V2
cAMP
cAMP vs IP3/DAG: ADH V1
IP3/DAG
cAMP vs IP3/DAG: ATII on epithelial cells
cAMP
cAMP vs IP3/DAG: ATII on vascular smooth muscles
IP3/DAG
cAMP vs IP3/DAG: Catecholamines beta1 and beta2
cAMP
cAMP vs IP3/DAG: ACTH
cAMP
cAMP vs IP3/DAG: LH, FSH, TSH
cAMP
cAMP vs IP3/DAG: Catecholamines alpha1
IP3/DAG
cAMP vs IP3/DAG: GnRH
IP3/DAG
cAMP vs IP3/DAG: HCG
cAMP
cAMP vs IP3/DAG: MSH
cAMP
cAMP vs IP3/DAG: CRH
cAMP
cAMP vs IP3/DAG: Calcitonin
cAMP
cAMP vs IP3/DAG: TRH
IP3/DAG
cAMP vs IP3/DAG: Calcitonin, PTH
cAMP
cAMP vs IP3/DAG: GHRH
IP3/DAG
cAMP vs IP3/DAG: Secretin
cAMP
cAMP vs IP3/DAG: Somatostatin
cAMP
cAMP vs IP3/DAG: Glucagon
cAMP
cAMP vs IP3/DAG: Oxytocin
IP3/DAG
Steroid hormones
1) Aldosterone
2) Cortisol
3) Progesterone
4) Estrogen
5) Testosterone
6) Vitamin D
7) Thyroid hormone
Unbound vs bound: Active form of steroid hormone
Free
Main site of inactivation of steroid hormones
Liver
Mechanism for removal of steroid hormones
Kidneys
2 categories of synergistic effects of hormones
1) Additive
2) Complementary
Additive vs complementary: Epi and NE on the heart
Additive
Additive vs complementary: FSH and testosterone on spermatogenesis
Complementary
Synergistic vs permissive: Cortisol and epi & NE on blood vessels
Permissive
Synergistic vs permissive: T3 and epi on lipolysis
Permissive
Permissive vs antagonistic: Estrogen and prolactin on breasts during pregnancy
Antagonistic
Negative vs positive feedback: More common
Negative
Negative vs positive feedback: Exploding
Positive
Long loops of negative feedback (players)
1) Hormone-anterior pituitary
2) Hormone-hypothalamus
Short loop of negative feedback
Anterior pituitary-hypothalamus
Positive feedback, examples (3)
1) Estrogen-induced LH and FSH surge
2) Oxytocin during labor
3) Oxytocin during lactation
Examples of hormone down-regulation
1) Progesterone down regulates its own receptors and estrogen receptors on the uterus
2) T3 downregulates TRH receptors