Genome-wide characterisation of the binding repertoire of small molecule drugs

Makowski, Lee; Rodi, Diane J

doi:10.1186/1479-7364-1-1-41

Human Genomics

Table 1 A sample list of drugs on the market for which multiple protein/macromolecule targets have been identified or implied [1] in the literature

From: Genome-wide characterisation of the binding repertoire of small molecule drugs

Drug	Target	Physiological effect	Experimentally confirmed?
Taxol™	β-Tubulin	Mitotic block	Yes[2]
	Bcl-2	Apoptosis	Yes[3]
	P-glycoprotein	Drug resistance	Yes[4, 5]
	CD18	LPS-like activity	Yes[6]
	Topoisomerase II	Mitotic block?	Yes[7]
	Hsp90	?	Yes[8]
Aspirin	COX	Anti-inflammatory activity	Yes[9]
	IKKKβ	Anti-inflammatory activity	Yes[10]
	Carbonic anhydrase	Anti-inflammatory activity	Yes[11]
	Antithrombin III	Anticoagulant activity	Yes[12]
	LCHAD	Beta-oxidation inhibition	Yes[13]
	Fatty acid-binding protein	Peroxisome proliferator activity	Implied[14]
Gentamicin	16S ribosomal RNA	Antibiotic activity	Yes[15]
	α9 nAChR	Side effects on organ of Corti	Yes[16, 17]
	Glutamate dehydrogenase	Nephrotoxicity	Yes[18]
	Steroidogenic enzymes?	Sperm count decline	Implied[19]
Ibuprofen	Prostaglandin H(2) synthase-I	Anti-inflammatory activity	Yes[20]
	Steroid sulfotransferase	Toxicity	Yes[21]
	?	PMN migration inhibition	Implied[22]
Saquinavir	HIV protease	Anti-HIV activity	Yes[23]
	PPARγ	Fat metabolism effects	Yes[24]
Neomycin B	16S ribosomal RNA	Antibiotic activity	Yes[25]
	Multiple ribozymes	?	Yes[26, 27]
	α9 nAChR	Side effects on organ of Corti	Yes[16]
	Inositol phospholipids	Inhibition of phospholipase C	Yes[28]
	RRE RNA from HIV	Anti-HIV activity	Yes[29]
	Glutamate dehydrogenase	Nephrotoxicity	Yes[18]
Penicillin	β-Lactamase	Antibiotic activity	Yes[30]
	GSH S-transferase	?	Yes[31]
	?	IFN-γ modulation	Implied[32]
Genistein	Tyrosine protein kinase	Multiple cellular effects	Yes[33–35]
	Topoisomerase I and II	Multiple cellular effects	Yes[36, 37]
	Oestrogen receptor β	Partial agonist activity	Yes[38, 39]
Fluoroquinolones	GyrA gene product	Antibiotic activity	Yes[40]
	ParC (topoisomerase IV) gene product	Antibiotic activity	Yes[41, 42]
CGP64222	HIV TAR RNA	Anti-HIV activity	Yes[43]
	CXCR4 coreceptor	Anti-HIV activity	Yes[44]
Flavopiridol	Cyclin-dependent kinase	Anti-cancer activity	Yes[45]
	Duplex DNA	Anti-cancer activity	Yes[46]
Coumarins	DNA gyrase	Antibiotic activity	Yes[47]
	hel gene product(s)	Antibiotic activity	Possible[48]

Note: [1] 'Implied' means that there is no direct data to substantiate the direct binding of that drug to that particular target, merely indirect evidence.
LCHAD: long chain 3-hydroxyacyl-CoA-dehydrogenase; nAChR: neuronal nicotinic acetylcholine receptor; COX: cyclooxygenase; PPAR: peroxisome proliferator-activated receptor; RRE: Rev response element; GSH: glutathione S-transferase; TAR: transactivation response; LPS: lipopolysaccharide; PMN: polymorpho-nuclear leukocyte.

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ISSN: 1479-7364

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