Table 1

Summary of the transporters responsible for the uptake of cytotoxic drugs.

Drug

Pool hits

Robot [μM]

Robot hits

Indirect effect

Verification hits

Competitor

Lipinski's

Rules [3]


Aminopterin

2

nrt1Δ, fen2Δ

ctr1Δ

nrt1Δ, ctr1Δ

NT

Fail


Amm. pyrrolidine thiocarbamate

20

pca1Δ

NT

NT

Pass


Artesunate

100

fen2Δ (2*σ)

cch1Δ, mid1Δ (2*σ)

NT

NT

Pass


Bay 11-7985

10

fui1Δ

NT

NT

Pass


Benzbromarone

None

28

fui1Δ

NT

NT

Fail


Canavanine

can1Δ

5

can1Δ

can1Δ

pass

Fail


Cantharidin

30

fen2Δ, snq2Δ (2.5*σ)

cch1Δ, mid1Δ, pho89Δ (2.5*σ)

fen2Δ pho89Δ (others NT)

NT

Pass


Cisplatin

50

fcy2Δ, lem3Δ, (fat1Δ, fps1Δ, hnm1Δ 2*σ)

fcy2Δ, (fat1Δ, fps1Δ, hnm1Δ NT)

NT

Pass


Clotrimazole

25

itr1Δ

ftr1Δ fet3Δ

NT

NT

Fail


3,4-Dichloroisocoumarin

8

None

Pass


Diphenyleneiodonium chloride

nrt1Δ

8

nrt1

nrt1Δ

pass

Pass


Fluconazole

100

itr1Δ fcy2Δ

ftr1Δ fet3Δ

NT

NT

Pass


5-Fluorocytosine

158

fcy2

fcy2Δ

NT

Pass


5-Fluorouracil

158

fcy2Δ

fen2Δ

fcy2Δ fen2

NT

Pass


Iodoacetamide

20

mal11Δ (2.5*σ)

Reproducible only on solid

NT

Pass


Ketoconazole

80

itr1Δ fat1Δ

NT

NT

Fail


Methotrexate

100

nrt1Δ

nrt1Δ

pass

Fail


Mitoxantrone

75

agp1

NT

NT

Fail


1,10-Phenanthroline

14

ctr1Δ

NT

NT

Pass


N-Phenylanthranilic Acid

100

None

Pass


Protoporphyrin

600

agp1Δ

NT

NT

Fail


Tamoxifen

730

None

Fail


Tetraethylthiuram disulfide

10

pdr5Δ (2*σ)

NT

NT

Fail


Tunicamycin

4

lem3Δ dnf2Δ qdr2Δ

pca1Δ pho89Δ

all confirmed

NT

Fail


Vanillylmandelic acid

647

None

Pass


ZM 39923

14

None

Fail


NT indicates liquid verification or competitor experiments were not tested.

Lanthaler et al. BMC Biology 2011 9:70   doi:10.1186/1741-7007-9-70

Open Data