Additional Agents Flashcards
which of the following drugs acts by binding to HER2?
a) trastuzumab
b) pertuzumab
c) margetuximab
d) T-DM1
e) all of the above
all of the above
which of the following drugs exerts antitumor effects by inhibiting the interaction between PD1 and PDL1?
a) cetuximab
b) ipilimumab
c) atezolizumab
d) all of the above
atezolizumab
what concept of immunity must ne overcome for immune system to successfullt eliminate cancer cells?
a) antibody-dependent cellular cytotoxicity
b) central tolerance
c) T-cell activity
d) B-cell activity
central tolerance
which is the function of cetuximab?
a) to block EGFR ligand binding
b) the same as panitumumab
c) bind VEGF
d) the same as pertuzumab
e) A and B
A and B
a) letrozole plus palbociclib
b) lapatinib plus capecitabine
c) trastuzumab
d) paclitaxole
e) irinotecan
letrozole plus palbociclib
phosphorylation isn’t the only posttranslational modification (PTM) that can affect protein function
- example: methylation
chromatin modifications are an emerging area
epigenetics and chromatin regulation
acetylation of histones can ___ the transcription of tumor suppressor genes
- deacetylation inhibitors - romidepsin, vorinostat, belinostat, panbinostat
methylation at histone 3, lysine 27 by EZH2 is increased (an mutates) in many cancers
- EZH2 inhibitors: Tazemetostat
increase
acetylation loosens up DNA
DNA methylation (cytosine)
switches gene ___
off
tightens up DNA
DNA methylation
- putting a methyl group on DNA will make it unrecognizable to transcription process
- we want to prevent methylation so that we can increase the transcription of___ genes
tumor suppressor
Azacitabine and Decitibine
- incorporates into DNA (and RNA for Azacitibine), and ___ binds ___ enzymes, preventing their function
___ cells and DNA ___ to be incorporated - DNMT inhibitors result in the reactivation of ___ genes
- indicated for the treatment of patients with ___ syndrome (MDS)
- covalently, DNMT
- cycling, synthesis
- tumor suppressor
- myelodysplastic
NOT ANTIMETABOLITES
targeting the proteasome
- the proteasome breaks down misfolded proteins and proteins get targeted for degradation by ___
- utilized in cell signaling and in normal protein turn over
- multiple myeloma cells make a lot of ___ ( ___ because they are B-cell cancer) so they are good targets for proteasome inhibition
- cancer cells have to degrade ___ “bad proteins” than normal cells
- ubiquitination
- proteins
- antibodies
- more
“-zomib”
bortezomib (Velcade), carfilzomib (Kyprolis), ixazomib (Ninlaro)
inhibitors of ___ activity
- disruption of intracellular protein homeostasis leads to cell death
indicated for the treatment of multiple ___ (B-cell malignancy). These cells naturally make a lot of proteins ( ___ )
- carfilzomib lacks ___ SE of bortezomib
- ixazomib is taken orally in a ___ form
proteasome
- myeloma
- antibodies
- neuropathy
- prodrug
including the unfolded protein response
thalidomide
interesting drug with stormy history
- anti- ___ activity
- binds to a ___ ligase protein cereblon (CRBN) and increases protein degradation of new substances (neosubstrates)
- leads to degradation of several proteins, including the transcription factor SALL4, which ___ development
toxicity
-potent ___ ? extraordinary precaustions taken to prevent pregnancy
- anti-angiogenic
- ubiquitin
- limb
- teratogen
inhibition of BCL-2
BCL-2 is an anti- ___ protein
anti-apoptotic
