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Table 5 Anticancer drugs and the hypertolerant phenotype of yeast strains heterozygous for the HP gene encoding their target protein

From: Copy-number variation of cancer-gene orthologs is sufficient to induce cancer-like symptoms in Saccharomyces cerevisiae

Drug

Concentration in solid medium (uM)

Concentration in liquid medium (uM)

Mode of action

Specific HP genetic target (yeast/human)

Hyper-tolerant yeast strains

Cancer in which CNV-reduction of the gene deleted

in the hypertolerant strain occurs

    

RAD54/RAD54L

  

Cycloheximide

0.36, 1.8

0.1

Inhibition of translation

RIM11/GSK3B

IRR1/irr1

-

Mitoxantrone

10, 25

-

TOPII inhibition

TOP2/TOP2A

-

-

     

NBP2/nbp2

 
     

GPD1/gpd1

Serous adenocarcinoma (NBP2)

Methotrexate

200

2, 100

Inhibition of nucleoside and purine synthesis

MET7/FPGS

RIM11/rim11

Renal cell carcinoma (GPD1)

Phleomycin

1, 2

0.1, 0.5

DNA strand break induction

-

MET7/met7

Serous adenocarcinoma

5-fluorouracil

200

2, 100

Inhibition of pyrimidine synthesis

-

IDP1/idp1

-

Tamoxifen

25

-

Estrogen receptor antagonist

-

-

-

     

NBP2/nbp2

 

Aminopterin

10

0.1,1, 5, 10, 50, 100

Inhibition of DNA, RNA & protein synthesis

-

TOP1/top1

Serous adenocarcinoma

SAHA/vorinostat

10, 20

-

Histone deacetylase inhibition

RPD3/HDAC2

-

-

Bay 11-7085

20, 40

-

NF-kB TF inhibitior; proapoptotic agent

-

-

-

Cantharidin

30, 60

6, 30

Inhibition of PP2A

TPD3

UBX4/ubx4

-

PD98059 (2'-amino-3'-methylflavone)

40, 80

4

MEK1 MAPK inhibition

PBS2/MAP2K1

NBP2/nbp2

Serous adenocarcinoma

     

HRK1/hrk1

 
     

MLH1/mlh1

 

Hydroxyurea

100000, 200000

100, 1000

Inhibition of DNA synthesis; DSB induction

RAD54/RAD54L

STP22/stp22

Renal cell carcinoma (MLH1)

Lithium chloride

 

-

Alternative RIM11 inhibitor

RIM11/GSK3B

-

 

Caffeine

1000, 5000

-

Alternative RAD54 inhibitor

RAD54/RAD54L

-

 

Methyl methanesulfonate

 

-

DNA methylation, causing DSB or stalled replication forks

-

-

 

DPI

10, 20

-

NAD(P)H oxidase inhibition

-

-

 

Tert-butyl hydroperoxide (TBHP)

 

-

Free-radical generation

-

-

 

Clotrimazole

2.5, 5, 7.5

-

Antifungal; increases cell wall permeability

-

-

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