Chemical genetics for therapeutic target mining

Expert Opinion on Therapeutic Targets

Volumn 8, Issue 6, 2004, Pages 653-661

  Shim, Joong Sup ^a   Kwon, Ho Jeong ^a  

^a Sejong University   (South Korea)

Author keywords

Angiogenesis; Chemical genetics; Functional genomics; Target identification

Indexed keywords

AMINOPEPTIDASE; ANGIOGENESIS INHIBITOR; BETULIC ACID; CALCINEURIN; CURCUMIN; DOXORUBICIN; DYCLONINE; EPOXOMICIN; FK 506 BINDING PROTEIN; FUMAGILLIN; GLUCOSE; HEAT SHOCK PROTEIN 90; HOMOISOFLAVONE DERIVATIVE; I KAPPA B KINASE; INDISULAM; LACTACYSTIN; MICROSOMAL AMINOPEPTIDASE; MITOGEN ACTIVATED PROTEIN KINASE 1; PARTHENOLIDE; PHOSPHATASE; RADICICOL; RAPAMYCIN; SEMAXANIB; SIRTUIN; TACROLIMUS; THALIDOMIDE; THERMOZYMOCIDIN; UNINDEXED DRUG; URSOLIC ACID; VASCULOTROPIN;

ANGIOGENESIS; CHEMICAL GENETICS; CLINICAL TRIAL; COLON CANCER; DNA MICROARRAY; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVITY; GENE FUNCTION; GENETIC MANIPULATION; GENOMICS; HUMAN; MUTAGENESIS; NONHUMAN; PROTEIN FUNCTION; PROTEIN TARGETING; REVIEW;

ANGIOGENESIS INHIBITORS; ANTIGENS, CD13; CHROMATOGRAPHY, AFFINITY; CLINICAL TRIALS, PHASE I; COLONIC NEOPLASMS; COMBINATORIAL CHEMISTRY TECHNIQUES; CURCUMIN; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; MODELS, CHEMICAL; MOLECULAR STRUCTURE; OLIGONUCLEOTIDE ARRAY SEQUENCE ANALYSIS; PEPTIDE LIBRARY; PHENOTYPE; PROTEIN BINDING; PROTEINS;

EID: 11144294717     PISSN: 14728222     EISSN: None     Source Type: Journal    
DOI: 10.1517/14728222.8.6.653     Document Type: Review

References (59)

1. TAKAHASHI JS, PINTO LH, VITATERNA MH: Forward and reverse genetic approaches to behavior in the mouse. Science (1994) 264 1724-1733.
2. STARK GR, GUDKOV AV: Forward genetics in mammalian cells: functional approaches to gene discovery. Hum. Mol. Genet. (1999) 8:1925-1938.
3. BROADIE K: Forward and reverse genetic approaches to synaptogenesis. Curr. Opin. Neurobiol. (1998) 8:128-138.
4. BOSHER JM, LABOUESSE M: RNA interference: genetic wand and genetic watchdog. Nat. Cell Biol. (2000) 2:E31-E36.
5. LANDEL CP, CHEN SZ, EVANS GA: Reverse genetics using transgenic mice. Ann. Rev. Physiol. (1990) 52:841-851.
6. MITCHISON TJ: Towards a pharmacological genetics. Chem. Biol. (1994) 1:3-6.
7. SCHREIBER SL: Chemical genetics resulting from a passion for synthetic organic chemistry. Bioorg. Med. Chem. (1998) 6 1127-1152.
8. CREWS CM, SPLITTGERBER U: Chemical genetics: exploring and controlling cellular processes with chemical probes. Trends Biochem. Sci. (1999) 24:317-320.
9. STOCKWELL BR: Chemical genetics: ligand-based discovery of gene function. Nat. Rev. Genet. (2000) 1:116-125.
10. KWON HJ: Chemical genomics-based target identification and validation of anti-angiogenic agents. Curr. Med. Chem. (2003) 10 717-736.
11. LOKEY RS: Forward chemical genetics: progress and obstacles on the path to a new Pharmacopeia. Curr. Opin. Chem. Biol. (2003) 7:91-96.
12. GIAEVER G, FLAHERTY P, KUMM J et al.: Chemogenomic profiling: identifying the functional interactions of small molecules in yeast. Proc. Natl. Acad. Sci. USA (2004) 101:793-798.
13. STOCKWELL BR, HAGGARTY SJ, SCHREIBER SL: High-throughput screening of small molecules in miniaturized mammalian cell-based assays involving post-translational modifications. Chem. Biol. (1999) 6 71-83.
14. PETERSON RT, LINK BA, DOWLING JE et al.: Small molecule developmental screens reveal the logic and timing of vertebrate development. Proc. Natl. Acad. Sci. USA (2000) 97 12965-12969.
15. ZHAO Y, DAI X, BLACKWELL HE et al.: SIR1, an upstream component in auxin signaling identified by chemical genetics. Science (2003) 301:1107-1110.
16. SCHREIBER SL: Target-oriented and diversity-oriented organic synthesis in drug discovery. Science (2000) 287:1964-1969.
17. HARDING MW, GALAT A, UEHLING DE et al.: A receptor for the immunosuppressant FK506 is a cis-trans peptidyl-prolyl isomerase. Nature (1989) 341:758-760.
18. LIU J, FARMER JD Jr, LANE WS et al.: Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell (1991) 66:807-815.
19. SIN N, MENG L, WANG MQ et al.: The anti-angiogenic agent fumagillin covalently binds and inhibits the methionine aminopeptidase, MetAP-2. Proc. Natl. Acad. Sci. USA (1997) 94 6099-6103.
20. ODA Y, OWA T, SATO T et al.: Quantitative chemical proteomics for identifying candidate drug targets. Anal. Chem. (2003) 75:2159-2165.
21. SCHE PP, MCKENZIE KM, WHITE JD et al. Display cloning: functional identification of natural product receptors using cDNA-phage display. Chem. Biol. (1999) 6:707-716.
22. HEITMAN J, MOVVA NR, HALL MN: Targets for cell cycle arrest by the immunosuppressant rapamycin in yeast. Science (1991) 253 905-909.
23. MARTON MJ, DERISI JL, BENNETT HA et al.: Drug target validation and identification of secondary drug target effects using DNA microarrays. Nat. Med. (1998) 4:1293-1301.
24. GIAEVER G, CHU AM, NI L et al.: Functional profiling of the Saccharomyces cerevisiae genome. Nature (2002) 418 387-391.
25. SEBOLT-LEOPOLD JS, DUDLEY DT, HERRERA R et al.: Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. Nat. Med. (1999) 5:810-816.
26. KURUVILLA FG, SHAMJI AF, STERNSON SM et al.: Dissecting glucose signalling with diversity-oriented synthesis and small-molecule microarrays. Nature (2002) 416:653-657.
27. HORROCKS C, HALSE R, SUZUKI R: Human cell systems for drug discovery. Curr. Opin. Drug Discov. Devel. (2003) 6:570-575.
28. LANGER T, ROVAT EM: Chemical feature-based pharmacophores and virtual library screening for discovery of new leads. Curr. Opin. Drug Discov. Devel. (2003) 6:370-376.
29. FOLKMAN J: What is the role of endothelial cells in angiogenesis? Lab. Invest. (1984) 51:601-604.
30. FOLKMAN J, KLAGSBRUN M: Angiogenic factors. Science (1987) 235:442-447.
31. FOLKMAN J: Fundamental concepts of the angiogenic process. Curr. Mol. Med. (2003) 3:643-651.
32. FOLKMAN J: Tumor angiogenesis. Adv. Cancer Res. (1974) 19:331-358.
33. MOSES MA, LANGER R: A metalloproteinase inhibitor as an inhibitor of neovascularization. J. Cell Biochem. (1991) 47 230-235.
34. MILLAUER B, WIZIGMANN-VOOS S, SCHNURCH H: High affinity VEGF binding and developmental expression suggest Flk-1 as a major regulator of vasculogenesis and angiogenesis. Cell (1993) 72:835-846.
35. KRUGER A, SOELTL R, SOPOV I et al.: Hydroxamate-type matrix metalloproteinase inhibitor batimastat promotes liver metastasis. Cancer Res. (2001) 61:1272-1275.
36. GILES FJ, COOPER MA, SILVERMAN L et al.: Phase II study of SU5416 - a small-molecule, vascular endothelial growth factor tyrosine-kinase receptor inhibitor in patients with refractory myeloproliferative diseases. Cancer (2003) 97:1920-1928.
37. LOOK AT, ASHMUN RA, SHAPIRO LH et al.: Human myeloid plasma membrane glycoprotein CD13 (gp150) is identical to aminopeptidase N. J. Clin. Investig. (1989) 83:1299-1307.
38. DANIELSEN EM, HANSEN GH, NIELS-CHRISTIANSEN LL: Localization and biosynthesis of aminopeptidase N in pig fetal small intestine. Gastroenterology (1995) 109:1039-1050.
39. FUJII H, NAKAJIMA M, SAIKI I et al.: Human melanoma invasion and metastasis enhancement by high expression of aminopeptidase N/CD13. Clin. Exp. Metastasis (1995) 13:337-344.
40. SAIKI I, FUJII H, YONEDA J et al.: Role of aminopeptidase N (CD13) in tumor-cell invasion and extracellular matrix degradation. Int. J. Cancer (1993) 54:137-143.
41. MENRAD A, SPEICHER D, WACKER J et al.: Biochemical and functional characterization of aminopeptidase N expressed by human melanoma cells. Cancer Res. (1993) 53:1450-1455.
42. PASQUALINI R, KOIVUNEN E, KAIN R et al.: Aminopeptidase N is a receptor for tumor-homing peptides and a target for inhibiting angiogenesis. Cancer Res. (2000) 60:722-727.
43. BHAGWAT SV, LAHDENRANTA J, GIORDANO R et al.: CD13/APN is activated by angiogenic signals and is essential for capillary tube formation. Blood (2001) 97:652-659.
44. SHIM JS, KIM JH, CHO HY et al.: Irreversible inhibition of CD 13/aminopeptidase N by the antiangiogenic agent curcumin. Chem. Biol. (2003) 10:695-704.
45. KELLOFF GJ, CROWELL JA, HAWK ET et al.: Strategy and planning for chemopreventive drug development: clinical development plans II. J. Cell Biochem. (1996) 26(Suppl.):54-71.
46. THALOOR D, SINGH AK, SIDHU GS et al.: Inhibition of angiogenic differentiation of human umbilical vein endothelial cells by curcumin. Cell Growth Differ. (1998) 9:305-312.
47. MOHAN R, SIVAK J, ASHTON P et al.: Curcuminoids inhibit the angiogenic response stimulated by fibroblast growth factor-2, including expression of matrix metalloproteinase gelatinase B. J. Biol. Chem. (2000) 275:10405-10412.
48. ARBISER JL, KLAUBER N, ROHAN R et al.: Curcumin is an in vivo inhibitor of angiogenesis. Mol. Med. (1998) 4 376-383.
49. SHIM JS, KIM DH, JUNG HJ et al.: Hydrazinocurcumin, a novel synthetic curcumin derivative, is a potent inhibitor of endothelial cell proliferation. Bioorg. Med. Chem. (2002) 10:2439-2444.
50. SHARMA SV, AGATSUMA T, NAKANO H: Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol. Oncogene (1998) 16:2639-2645.
51. FENTEANY G, STANDAERT RF, LANE WS et al.: Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin. Science (1995) 268:726-731.
52. NISHI K, YOSHIDA M, FUJIWARA D et al.: Leptomycin B targets a regulatory cascade of crm1, a fission yeast nuclear protein, involved in control of higher order chromosome structure and gene expression. J. Biol. Chem. (1994) 269:6320-6324.
53. TAUNTON J, HASSIG CA, SCHREIBER SL: A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p. Science (1996) 272:408-411.
54. MENG L, KWOK BH, SIN N et al.: Eponemycin exerts its antitumor effect through the inhibition of proteasome function. Cancer Res. (1999) 59:2798-2801.
55. CHEN JK, LANE WS, SCHREIBER SL: The identification of myriocin-binding proteins. Chem. Biol. (1999) 6:221-235.
56. KWOK BH, KOH B, NDUBUISI MI et al.: The anti-inflammatory natural product parthenolide from the medicinal herb Feverfew directly binds to and inhibits IkappaB kinase. Chem. Biol. (2001) 8:759-766.
57. JIN Y, YU J, YU YG: Identification of hNopp140 as a binding partner for doxorubicin with a phage display cloning method. Chem. Biol. (2002) 9:157-162.
58. HUGHES TR, MARTON MJ, JONES AR et al.: Functional discovery via a compendium of expression profiles. Cell (2000) 102:109-126.
59. BUTTE AJ, TAMAYO P, SLONIM D: Discovering functional relationships between RNA expression and chemotherapeutic susceptibility using relevance networks. Proc. Natl. Acad. Sci. USA (2000) 97 12182-12186.