Oncology Med Chem Pharmacology

Question 0

-tinib

Answer 0

Small molecule
Enzyme kinase inhibitor
Modifies cellular signaling

Chemical synthesis
100% pure defined structure
Can take orally

Question 1

Targeted (signal based) therapies

HAG SINS TTZ

Answer 1

Herceptin
Avastin
Gleevec
Sutent 
Iressa 
Nexavar 
Sprycel 
Tarceva 
Tykerb 
Zactima

Question 2

-mab

Answer 2

Monoclonal antibody
Biologic

Works on receptor to modulate cell signaling

Living cells and cell lines
Heterogenous complex structure
Injected
Less stable and sensitive to denaturation

Question 3

Purines

Answer 3

Two rings fused

Guanine
Adenine purines

2GAPurines

Question 4

Pyrimidines

Answer 4

One ring

1CT pyramid

Cytosine
Thymine

Question 5

Guanine

GC3

Answer 5

Double bond O purine
3 Hbonds
ONN

Question 6

Adenine

Answer 6

3 nitrogen purine

2 Hbonds

Question 7

Cytosine

Answer 7

Double bond O Pyrimidine
3 Hbond
ONN

Question 8

Thymine

Answer 8

Two double bond O pyrimidine

2 Hbonds

Question 9

Go

Answer 9

Growth factors - EGF, VEGF

Oncogenes - ras

Question 10

Stop

Answer 10

Tumor suppressor genes

P53

Question 11

Purine biosynthesis

GGACT

Answer 11

Glycine
Glutamine
Aspartic acid
Cofactor THF
CO2

Question 12

6-MPRP

Mercapto-purine-ribose-phosphate

Answer 12

From 6-MP prodrug

Deplete PRPP stores
InosineMP mimic

Question 13

Methotrexate

Answer 13

Works and interferes wherever THF cofactors is active

Question 14

Purine antagonists

Answer 14

Fake nucleoside mimic

Competitively inhibit DNA polymerase

Vidarabine
Fludrabine
Cladribine

Question 15

Pentostatin

Answer 15

Adenosine Deaminase (ADA) inhibitor

Transition state analog mimic

Prevent breakdown of vidarabine and other nucleoside mimics

Adjunct therapy

Question 16

Xanthine oxidase inhibitor

Answer 16

Inhibit xanthine (from guanine and adenine) from oxidizing to Uric acid and causing gout

Question 17

Tumors with high EGFR expression

Answer 17

NSCLC - non-small cell lung cancer
Prostate
Gastric

Breast - HER2 human EGFR

Question 18

HER2

Answer 18

Human EGFR,

Active as homodimer

Herceptin (trastuzumab) flags for immune cell destruction and blocks downstream HER2 signaling by preventing dimerization of HER receptors

Question 19

Iressa and tarceva

Answer 19

EGFR kinase antagonists with common anikinoquinazoline skeleton

Affinity and compete for ATP-binding site

Tarceva has key water molecule interaction

Question 20

Gleevec

Answer 20

Bind and stabilize an inactive form

Question 21

Gleevec resistance mutation

Answer 21

Threonine 315 to isoleucine 315

ATP can displace gleevec easier

Question 22

Iressa resistance mutation

Answer 22

Threonine to methionine

Question 23

Nilotinib

Answer 23

Designed against amino acid resistance

Backup for gleevec resistant tumors

Question 24

Zolinza

Answer 24

HDAC inhibitor: Epigenetic target Acetyl makes lysine neutral and loosens histone grip on DNA: more transcription of p53 Lysine is normally positive without Acetyl and binds tightly to DNA

Question 25

Interchangeable biosimilar

Answer 25

FDA determined safe for substitution

Question 26

Glycine

Answer 26

Only amino acid with no chirality

Question 27

Mizoribine

Answer 27

IMP dehydrogenase inhibitor Blocks XMP/guanine nucleotide synthesis

Question 28

Mycophenolate

Answer 28

IMP dehydrogenase inhibitor and | GMP synthetase inhibitor

Question 29

ADA

Answer 29

Amine to double bond O Deactivated purine antagonists SCID = ADA deficiency & lymphocyte destruction

Question 30

Gout

Answer 30

Excess (AMP/GMP) purine catabolism Or deficient HGPRT salvage pathway (inosine gets deaminated and later forms Uric acid)

Question 31

Von gierks disease

Answer 31

Increase G6phosphatase Increase PRPP for purine biosynthesis Excess Uric acid production

Question 32

Purine metabolism disorders

Answer 32

Increases PRPP synthetase PRPP amido transferase Defective HGPRT Increase G6phosohatase

Question 33

Leech-Nyhan Syndrome

Answer 33

HGPRT deficiency

Question 34

Febuxostat

Answer 34

Selective XO inhibitor Non purine Less interactions and side effects than allopurinol

Question 35

Allopurinol

Answer 35

Nonselective XO inhibitor | Purine analog

Question 36

Rate limiting step of purine biosynthesis

Answer 36

PRPP to PRA Inhibited by 6MPRP