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Medchem > Medchem > Flashcards

Medchem Flashcards

1
Q

Bevacizumab

A

Targets VEGF and can be used to prevent angiogenesis
Selectively binds VEGF and can stop it from binding to its receptors, reducing microvascular growth of tumour blood vessels and limiting blood supply to tumours
Neutralises VEGFA

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2
Q

Afilbercept

A

Human recombinant fusion protein with antiangiogenic effects - functions as a decoy receptor to bind to VEGF
Reduces production of VEGF

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3
Q

Ramucirumab

A

Binds VEGFRs, inhibiting angiogenesis pathways

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4
Q

Ipilimumab

A

Anti-cancer antibody that targets CTLA-4
Results in T-cell proliferation and cytokine release, resulting in an amplified immune response

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5
Q

Pembrolizumab

A

Binds to PD-1 on the surface of activated T-cells, blocking its binding by ligands, which results in the activation of T-cell-mediated immune responses against tumor cells.

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6
Q

Nivolumab

A

Binds to PD-1 on the surface of activated T-cells, blocking its binding by ligands, which results in the activation of T-cell-mediated immune responses against tumor cells.

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7
Q

Durvalumab

A

New PDL-1 inhibitor. Binding results in the release the inhibition of immune responses, without inducing antibody-dependent cell-mediated cytotoxicity.

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8
Q

Herceptin

A

EGFR inhibitor. Prevents HER2-mediated signalling

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9
Q

Cetuximab

A

Inhibits growth and survival of EGFR-positive tumours. It promotes antibody-dependent cellular cytotoxicity (ADCC) against certain human tumour types

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10
Q

Sorafenib

A

Has multi-kinase inhibitory action. Inhibits the RAF/MEK/ERK pathway and reduces angiogenesis by inhibiting EGFR.

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11
Q

Dasatinib

A

Blocks the ATP binding site of Src

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12
Q

Sotorasib

A

Binds to the cys residue in mutated Ras, locking it in its inactive form.

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13
Q

Gefitinib (Iressa)

A

First gen. EGFR inhibitor

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14
Q

Erlotinib

A

First gen. EGFR inhibitor

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15
Q

Lapatinib

A

2nd gen. EGFR inhibitor

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16
Q

Afatinib

A

2nd gen EGFR inhibitor

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17
Q

Rocilentinib

A

3rd gen EGFR inhibitor, can target T790M mutation

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18
Q

Osimertinib

A

3rd gen EGFR inhibitor, can target T790M mutation

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19
Q

Advexin

A

Adenovirus that delivers normal P53 to the cells, outcompeting mutated P53

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20
Q

Pifithrin

A

Suppresses normal P53 in normal tissue, reducing the effects of chemo

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21
Q

PRIMA-1

A

suppresses mutant P53 expression

22
Q

Imatinib (Glivec)

A

Targets BCR-Abl translocation, by inhibiting Abl tyrosine kinase

23
Q

Idasanutlin (AR)

A

MDM2 inhibitor, preventing MDM2 from inhibiting P53

24
Q

TERT-vaccines

A

Stimulate the immune system to target cells expressing TERT, the gene encoding telomerase, that maintains the length of telomeres, and is thus found in cancer cells.

25
Q

Methotrexate

A

Dihydrofolate analogue, binds to DHFR. Folate antagonist

26
Q

5-FU

A

Pyrimidine antagonist
fluorine atom ends up on dUMP (fdUMP), which binds to TS and 5,10-CH2-T to form a ternary complex
the F atom is too electronegative for the complex to break apart, so TS is trapped and the folate cycle cannot continue

27
Q

6-MP

A

Purine antagonist

It is converted into an active metabolite (by HGPRT?), thio-IMP, which is further metabolised into thio-GMP and thio-dGTP, which are incorporated into DNA, resulting in impaired DNA replication.

28
Q

Gemcitabine

A

Sugar modified nucleoside
Gemcitabine (F2dC) is readily converted into triphosphate F2dCTP
This inhibits DNA polymerases as an analogue of dCTP

F2dC –> (dCk) F2dCMP –> (UMP kinase) F2dCDP –> (NDP kinase) F2CTP
depletion of dCTP as a result of F2dCDP results in activation of dCk. Activation of dCk increases formation of F2dCMP (self-potentiation of Gemcitabine)

29
Q

Cytarabine

A

Inhibits DNA polymerases as an analogue of dCTP

30
Q

Taxane ligands - Paclitaxel

A

MSA.
Binds near the ML surface on the B-subunit, on the inside of the MT
Fits between small gaps and induces a conformational change, disrupting MT dynamics

31
Q

Vinca alkaloids

A

MDA
Binding site is at the +end surface of B-tubulin - forms a wedge, interfering with the incorporation of new heterodimers
+end remains curved and MT wall cannot form

32
Q

Colchicine

A

binding site is located between the alpha and beta subunits
binding stabilises the heterodimer in the curved formation
binds to soluble pool and is incorporated
destabilises MT at high concentrations

33
Q

Carfilzomib (AR)

A

Proteasomal inhibitor
could attenuate paclitaxel resistance through activation of hypoxia-inducible factor 1

34
Q

Nitrogen mustards

A

Alkylator
Target guanine N7 and exo-cyclic NH2, as well as Adenine N7 and N3
Chlorine atoms are lost, and the DNA becomes covalently bound to the drug

35
Q

Estramustine

A

Alkylator
A nitrogen mustard tagged with an oestrogen molecule, used to target oestrogen-dependent cells.
Can also be used in prostate cancer because the estradiol slows the body’s testosterone production, which the prostate cancer needs to grow

36
Q

Temozolomide

A

Alkylator (DNA methylator)
Transporter of a methyldiazonium ion, which is attaches to the DNA and methylates it.
T is broken down by water hydrolysis in order to release the methyldiazonium ion.

37
Q

CPIs (Adozelesin, Bizelesin)

A

DNA minor groove binder (covalent) - anti-tumour antibiotics
Their stereochemistry in the isopropyl ring is essential, as only one isomer is reactive
Bizelesin forms inter-strand DNA duplex crosslinks, while Adozelesin forms mono-alkylation duplex adducts

38
Q

PBDs

A

DNA minor groove binder (covalent) - anti tumour antibiotics
Form a reversible amime bond between the eco-cyclic NH2 of guanine and the C2 position on the PBD

39
Q

Distamycin and Netropsin

A

DNA minor-groove binders (non-covalent)

40
Q

Mitomycin C

A

DNA minor-groove binder (covalent)
Reduction of the molecule occurs, releasing a molecule of methanol - the now-reduced mitocene interacts with the DNA
DNA alpha attack occurs, and a second molecule of DNA then reacts with the drug.
2 tags on DNA formed
HYPOXIA-selective drug

41
Q

Patrin/O-6-benzylguanine

A

MGMT inhibitors - pseudosubstrates that deplete MGMT levels, which normally removes adducts from alkylators
Can therefore be used in combination with Temozolomide to treat high grade glioma

42
Q

Olaparib

A

Inhibits PARP1, 2 and 3
Binds to active site of PARP and prevents it from carrying out its function

43
Q

Rucaparib

A

Inhibits PARP1 and 2
Binds to the active site of PARP and preventing it from carrying out its function

44
Q

Nitromidazole

A

Has radiosensitising properties so can be used in hypoxic tumours
Reduces glutathione concentration and inhibits glutathione S-transferase
This causes tumours to become more sensitive to ionising radiation
A pro-drug that is activated by low oxygen levels

45
Q

Imetelstat (AR)

A

Inhibits telomerase activity
A synthetic oligonucleotide that targets the RNA component of telomerase
Promising against NSCLC, but need more trials

46
Q

Bleomycin

A

Cytotoxic glycopeptide antibiotics
Initiate ssDNA cleavage at pyrimidines 3’ to a guanine, generating blunt/staggered ends, depending on the residue
B is reactivated + reorganised after cleavage of the first strand of DNA - linker is key for this
Bond rotation between the two thiazole tails makes the drug available for interaction with the second DNA strand

47
Q

Cisplatin

A

Intercalator
Activated by water - it attacks the N7 of guanine
Bends the DNA and makes it difficult to recognise for repair mechanisms

48
Q

Carboplatin

A

Second generation platinum agent (intercalator)
Activated by water - it attacks the N7 of guanine
Bends the DNA and makes it difficult to recognise for repair mechanisms
Has a ligand that slows the release of the platinum moiety, leading to prolonged DNA binding and greater cytotoxicity.

49
Q

Oxaliplatin

A

Second generation platinum agent (intercalator)
Activated by water - it attacks the N7 of guanine
Bends the DNA and makes it difficult to recognise for repair mechanisms
Has a diaminocyclohexane ligand that enhances the reactivity of the drug, forming more inter strand cross links.

50
Q

Doxorubicin

A

Intercalation that targets TOP2
Stabilises the top2 complex, producing a cleavable complex that results in DNA strand breakage

51
Q

NK314 (AR)

A

A new intercalator that targets TOP2a, a specific isoform.
There is no therapeutic benefit in targeting TOP2b, as side effects such as cardiotoxicity and secondary malignancy can occur

Medchem (1 decks)

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