Transmembrane Receptor Enzymes

Question 1

what aer the three types of transmembrane receptor enzymes

Answer 1

receptor tyrosine kinase
receptor serine/threonine kinase
receptor guanylyl cyclase

Question 2

what are the types of receptor tyrosine kinases

Answer 2

insulin receptor
human epidermal growth factor receptor(HER)
platelet derived growth factor receptor(PDGF)
vascular endotheilai growth factor receptor (VEGF)

Question 3

what are the different types of receptor serine/threonin kinase

Answer 3

transforming growth factor B (TGF-B) receptor
activin and inhibin receptor
bone morphogenic protein(BMP) receptors

Question 4

what are the type of reecptor guanylyl cyclase

Answer 4

atrial natriuretic peptide(ANP) receptor
GC-A
GCB
GCC receptors

Question 5

what is the mechanism of receptor tyrosine kinase?

Answer 5

from inactive monomers, they become inactive dimers and cross phsophorylate and casue the active dimer
they can also become acitve dimers straight away, adn once they ligand bind, they result in the ligand bound active dimer, that result in the sigalling

Question 6

which domain allow for auto phosphorylation of the tyrosine kinase receptors

Answer 6

Src homology 2 domain

Question 7

how many ways can phosphorylation occure

Answer 7

auto phosphorylation and substrate phsophrylation

Question 8

what are the pathways that lead to cellular proliferation response ? from which receptor does it occure

Answer 8

EGFR Tyrosine kinase activation
- Mitogen activated protein Kinase Pathway
- Phospholipase Cy pathway
- Phosphatidylinositol 3 kinase athway

Question 9

Describe the Receptor Tyrosine Kinsae: PLCy pathway

Answer 9

When the PLCY is activaed by phosphorylation,
it converts PIP2 into DG and IP3

dag which is converted into PKC

IP3 causes CA2+ to increase

Question 10

describe the receptor tyrosoine kinase:PI3K pathway

Answer 10

PI3 kInsae result in convertions of PIP2 into PIP3

PIP3 result in attraction of peckstrin homology with the phosphatidylinositol depdendeent kindase 1

Activation of Akt (Protein Kinase B )

promote cell survival and inhibit apoptosis by phosphorylating and inactivating pro-apoptotic proteins such as Bad and caspase-9.

Question 11

describe the MAPK signaling pathway

Answer 11

GDP to GTP at Ras

result on Raf creation
Mak
Map kinase

Question 12

list the epidermal growth factor receptor inhibitor that causes inhibition of cancer

Answer 12

HER1 inhibitors

drug name : Geftinib, erlotinib
biologics: cetuximab, panitumumab

Question 13

list the epidermal growth factor receptor inhibitor that causes inhibition of breast cancer

Answer 13

HER2

small molecules: Lapatinib
biologics: Trastuzumab

Question 14

Platelt derived Growth Factor Receptor Inhibitor

Answer 14

Imatinib for cancer

Question 15

Vacsular Endothelial Growth Factor(VEGF) Receptor Inhibitor for Cancer

Answer 15

Sunitinib, Sorafenib
biologica: Bevacizumab

Question 16

Vacsular Endothelial Growth Factor(VEGF) Receptor Inhibitor for Muscle Degeneration

Answer 16

Oligonucleotide drug: Pegaptanib binds and blocks VEGF actions via intravitreal injections

Question 17

what are some functions the Receptor Serin/Threonine kindase : Transforming Growth Factor B Receptor are related to?

Answer 17

Growth Arrest
Cancer
Promote Apoptosis
Fibrosis
Angiogenesis
Immunomodulation
Atherosclerosis
Inflammation

• this thus makes it diffficult to design an inhibitor without causing any side effects

Question 18

receptors of Receptor Serine/ Theronin Kinase(TGFB) when the ligand binds

Answer 18

They will already be in a dimer and once the receptor binds, they become heterotetramer(dimer bind with dimer)
cross phosphorylation would happen adn then the MH2 AND MH1 Rsmad would be attracted

Question 19

what is SMAD

Answer 19

It has a mad homology1 and mad homology 2
- mad holomolgy 1 bind ot DNA while mad homology 2 bings for receptor kinase interactions and causes trasncriptional activation

Question 20

For bone morphology protein what are the R smads

Answer 20

1,5,8

Question 21

for TGF-B what are the R smad

Answer 21

2,3

Question 22

what are cosmads

Answer 22

they are smad4 that combine with Rsmad to move into the nucleus and regulate gene expression

Question 23

inhibitory smad

Answer 23

6, 7
interact with Rsmad and ensure they cannot bind tot eh DNA, thus no gene trasncription process

Question 24

Drug development for TGF B receptor signaling- Anti-TFG-B mAb

Answer 24

Fresolimumab

Question 25

Drug development for TGF B receptor signaling- TBRI Kinase inhibitor

Answer 25

Vactosertib

Question 26

Drug development for TGF B receptor signaling- Recombinant Human Bone Morphogenic Protein

Answer 26

rhBMP-2- for spinal deformity rhBMP-7- for bone nonuniors

Question 27

Drug development for TGF B receptor signaling- Activin Receptor Ligand Traps

Answer 27

Activin Receptor Type IIB-Fc Fusion Protein Luspatercept- Anemia in B thalassemia

Question 28

Drug development for TGF B receptor signaling- Activit Receptoy type IIA-Fc Fusion protien

Answer 28

Sotatercept- Pulmanory Arterial hypertension(PAH)

Question 29

What happens when TGF-B binds to the TBRII and TBRI recpetors

Answer 29

smad2or 3 will be released after the cross phosphorylation of the heterotetramer the smad2/3 binds with the COSMAD to modulate the geen expression

Question 30

Receptor Guanylyl Cyclase(GC) what are they and their ligands

Answer 30

there are NPR-A (GCA)- Atrial NP(ANP) and Brain NP(BNP) NPR-B CNP from endothelial and renal cells NPR-C clearance receptor for anp, bnp, cnp GCC- Uroguanylin and Guanylin GCA, GCB, GCC- are mainly in the CVS, skeletal system adn GI tract GCD AND GCG- absent in the human GCE AND GCF- in the retinal photoreceptors

Question 31

how many domains do the Natruretic peptide receptor have

Answer 31

ligand binding domin kinse homology domain hinge region Guanylyl cyclase domain

Question 32

drugs for the Natriuretic Peptide Receptors

Answer 32

ANP: Carperitide, for short term acute decompensated CHF BNP: Mesiritide: for short terms acute decompensated CHF CNP: cenderititde for natiuresis, diuresis and cardiac fibrosis

Question 33

function of PCGA

Answer 33

Natrurietic aterial vasodialtion renin and aldosterone suppressing anti apoptotic anti hypertrohic lusitropic lipolytic

Question 34

function of PGCB

Answer 34

anti fibrotic anti inflammatory vascular regenerating

Question 35

GCC receptor agonist

Answer 35

linaclotid and plecanatide for chronic idiopathic constipation and IBD predominant constipation and GI tumorigenesis