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12 4 1999 11 Journal of Iso topes V o l. 12 N o. 4 N ov. 1999 (EGF) (, 610041), 90%, 54%,, (EGF) (EGFR ) R 817 O 575 + 111,, CT M R I,,,,, (EGFR ) [ 1 3 ] EGFR [ 3, ], (EGF ) EGFR 1 EGF EGF, B runner [ 4 53 ], 1959 W alerfield (N GF),, [ 5, ] EGF (m EGF) 6 045 D, 416, 1125 s, 3, 1975, m EGF, (hegf), m EGF,, hegf m EGF 53 37, 3 EGF 6310 310 Λg 5210 315 Λg, ; EGF 6 17 80 29 272 2 4 ΛggL [ 6 ] 2 EGFR [ 7 EGFR 1 186 ], :, 33,, : 1999206222 : 1999210210

4 : (EGF) 223, EGF EGFR EGF EGFR, K d 0116 0177 nm o lgl [ 6, 8, 9 ] EGF, (T K) A T P, EGF,,, Ca 2+, C,, 3 EGFR, 90% EGFR, 54% [ 10 EGFR ], ( ) EGFR [ 1 3, 8, 9, 11 21 ] EGFR T K, (R T K), T K,, EGFR 992 1 068 1 173 C2Χ, EGFR 1 068 GRB 2, ras,, EGFR C2Χ GRB 2, EGF, EGFR, (T GF2Α), EGF, EGFR, 4 EGFR [ 8, 9 EGFR ] CT M R 1, Yo sh ida [ 3 ] EGFR EGF 21 (RCC) EGFR 16 EGFR, 11 EGFR, (P < 0. 000 1) RCC EGFR, 4 EGFR, EGFR, H arney [ 1 ] EGFR 425 EGFR 425 14 10, 1, 3 6, 4, 1, 425, 5 7 5, EGFR, EGFR 1997 Capala [ 15 ] 99 T c m EGF, EGFR 131 I 99 T c m EGF, C6EGFR, 131 I 131 I2EGF 30 m in,, 99 T c m 99 T c m 2EGF 6 h EGF, C6EGFR F ischer ; 4, 99 T c m 2 131 I2EGF Χ 131 I 99 T c m, 12 h 50% ;, 6 h, 20% 99 T c m EGF,, EGF EGFR EGFR

224 12 [ 8, 12, 22 ], EGFR : EGFR ( ) ; EGFR, ;,, 5 EGFR T K, T K,, R T K, R T K, R T K : EGFR, EGF R T K, EGFR,, Schm idt [ 23 ] EGFR EGFR EFGR 1992 B rady [ 18 ] 125 I EGFR 425, 1993 T akahash i [ 24 ] 131 I 425 F (ab ) 2 EGFR 555 M Bq 131 I 425 F (ab ) 2 U 287M G 131 I,, HAM A, ;,,, EGF EGFR, EGFR 6 1997 P irinen [ 22 ] 198 EGF, S EGF (P = 0. 007) (P = 0. 003) (P = 0. 003), EGF EGF, EGF EGFR, EGF, 131 I, :, Β, ; 99 T c m SPECT, 186 R e 90 Y, 99 T c m 186 R e 90 Y EGFR EGF, EGF EGF SH EGF 3,, EGFR ;,, D T PA EGF D T PA 2EGF, D T PA 99 T c m 186 R e 90 Y,, EGFR 99 T c m 2D T PA 2EGF 186 R e2 90 Y2D T PA 2EGF, EGFR 1 H arney JV, L iebert M,W edem eyer G, et al. T he Exp ression of Ep iderm al Grow th Facto r R ecep to r on H um an B ladder Cancer: Po tential U se in R adio imm uno scintigraphy. J U ro l, 1991, 146 (1): 227. 2 Kobaysh il T, Honke K, Gasa S, et al. R egulation of A ctivity L evels of Glyo lip id Sulfo transferases by

4 : (EGF) 225 T ransfo rm ing Grow th Facto r A lpha in R enal Cell Carcinom a Cell. Cancer R es, 1993, 53 (23): 5 638. 3 Yo sh ida K, Ho soya Y, Sum i S, et al. Studies of T he Exp ression of Ep iderm al Grow th Facto r R ecep to r in H um an R enal Cell Carcinom a: A Comparison of Inm unoh istochem icalm ethod V ersus L igand B inding A s2 say. O nco logy, 1997, 54 (3): 220. 4 F isher DA, L ak shm anan J. M etabo lism and Effects of Ep iderm al Grow th Facto r and R elated Grow th Facto r in M amm alṡ Endocr R ev, 1990, 11 (2): 418. 5 W alerfield M D. Pep tide R egulato ry Facto r: Ep iderm al Grow th Facto r and R elated M o leculeṡ L ancet, 1989, 1 (6): 1 243. 6.., 1994, 10 (2): 106. 7 Carpenter G, Cohen S. Ep iderm ic Grow th Facto ṙ J B io l Chem, 1990, 265(34): 7 709. 8 Santini J, Fo rm ento JL, F rancoualm, et al. Characterization, Q uantification and Po tential C linicalv alue of the Ep iderm al Grow th Facto r R ecep to r in H ead and N eck Squanous Cell Carcinom aṡ H ead N eck, 1991, 13 (2): 132. 9 L agrange JL, F rancoualm, Fo rm ento JL, et al. D emonstration and Characterization of EGF R ecep to rs in Cancer of the U terine Cervix. Bu ll Cancer Paris, 1993, 80 (3): 219. 10 A rtagaveytia N, L e Penven S, Faletle N, et al. Ep iderm al Grow th Facto r and T ransfo rm ing H row th Facto r A lpha M rnal Exp ression in H um an B reast Cancer B iop sies; A nalysis in R elation to Setradio l, P rogesterone and EGF R ecep to r Contenṫ J Stero id B iochem M o l B io l, 1997, 60 (3 4): 221. 11 M objtahedi H, H ick ish T, N ico lson M, et al. Phase 1 T rial and L ocalisation of the A nti2egfr M ono2 clonal A ntibody ICR 62 in H ead and N eck o r L ung Canceṙ B r J Cancer, 1996, 73 (2): 228. 12 Szepeshazi K, Schally AV, H almo s G, et al. Effect of a Cyto toxic A nalog of L H 2RH (T 298) on the Grow th of E strogen2dependent M XT M ouse M amm ary Cancers: Co rrelations Betw een Grow th Charac2 teristics and EGF R ecep to r Content of T umo rṡ B reast Cancer R es T reat, 1996, 40 (2): 129. 13 Goh ring U J, ScharlA, A h r A. V alue of Imm unoh istochem icald eterm ination of R ecep to rs, T issue P ro2 teases, T umo r Supp resso r P ro teins and P ro liferation M arkers as P rogno stic Indicato rs in P rim ary B reast Carcinom a. Gebu rtsh ife F rauenheilkd, 1996, 56 (4): 177. 14 A dach i K, H erlyn D. Enhancem ent of Ep iderm al Grow th Facto r R ecep to r (EGF2R ) Exp ression on Gliom a Cells by Cytok ineṡ N ippon Ika D aigaku Zassh i, 1991, 58 (5): 537. 15 Capala J, Barth R F, BaileyM Q, et al. R adio labeling of Ep iderm al Grow th Facto rw ith 99 T c m and in V i2 vo L ocalization Fo llow ing In tracereb ral In jection In to N o rm al and Gliom a2bearing R atṡ B iocon jug Chem, 1997, 8 (3): 289. 16 Straglio tto G, V ega F, Stasieck i P, et al. M ultip le Infusions of A nti2ep iderm al Grow th Facto r R ecep to r (EGFR ) M onoclonala ntibody (EM D 55900) in PatientsW ith R ecurrentm alignant Gliom aṡ Eur J Can2 cer, 1996, 32A (4): 636. 17 H uang S, T rujillo JM, Chak rabarty S. P ro liferation of H um an Co lon Cancer Cells: Ro le of Ep iderm al Grow th Facto r and T ransfo rm ing Grow th Facto r A lpha. Int J Cancer, 1992, 52 (6): 978. 18 B rady LW, M iyamo to C, W oo DV, et al. M alignant A strocytom as T reated W ith Iodine2125 L abeled M onoclonal A ntibody 425 A gainst Ep iderm al Grow th Facto r R ecep to r: A Phase g T rial. Int J R adiat O nco l B io l Phys, 1992, 22 (1): 225. 19 N ess GO, H augen DR, V arhaug JE, et al. Cytop lasm ic L ocalization of EGF R ecep to r N Pap illary T hy2 ro id Carcinom as: A ssociation W ith the 150 Kda R ecep to r Fo rm. Int J Cancer, 1996, 65 (2): 161. 20 Yash iro M, Chung YS, N ish im ura S, et al. E stablishm ent of Tw o N ew Scirrhous Gastric Cancer Cell L ines: A nalysis of Facto rs A ssociated W ith D issem inated M etastasiṡ B r J Cancer, 1995, 72 (5): 1 200. 21.., 1994, 16 (5): 395. 22 P irinen R, L ipponen P, A altom aa S, et al. P rogno stic V alue of Ep iderm al Grow th Facto r Exp ression in B reast Canceṙ J Cancer R es C lin O nco l, 1997, 127 (1): 63. 23 Schm idt M, V akalopoulou E, Schneider DW, et al. Construction and Functional Characterization of SCFV (14E1) 2A N ovel H igh ly Po tent A ntibody2toxin Specific fo r the EGF R ecep to ṙ B r J Cancer, 1997, 75 (11): 1 575. 24 T akahash i H, N akazaw a S, H erlyn D. Experim ental R adio imm uno therapy of a Xenografted H um an Gliom a U sing 131 I L abeled M ononclonal A ntibody to Ep iderm al Grow th Facto r R ecp to ṙ N euro l M ed Ch ir Tokyo, 1993, 33 (9): 610.

226 12 EP ID ERM AL GROW TH FACTOR AND IM AGINE D IAGNOSIS AND THERAPY OF TUMOUR W ITH RAD IONUCL ID ES L i Yunchun T an T ianzh i (D ep artm ent of N uclear M ed icine, T he F irst U niversity H osp ital of W est Ch ina U niversity of M ed ical S ciences, Cheng d u 610041) Abstract It has a direct p ropo rtin co rrelation betw een the ep iderm al grow th facto r re2 cep to r levels of tum ou r and tum ou r differen tiation degree, tum ou r sizes, stage, m o to tic in2 dex o r cancer recu rrence. Ep iderm a l g row th facto r recep to r is detected in 90% of the tu2 m ou rs, in w h ich, 54% of ep iderm al grow th facto r recep to r of m alignan t tum ou rs can link w ith ex ternal genou s ligand. T herefo re, radionuclinde labelled ep iderm al grow th facto r w ill b ring abou t the im aging diagno sis and therapy of m alignan t tum ou rṡ T he research p resen t situation and clin ical sign ificance of radionuclinde labelled ep iderm al grow th facto r fo r recep2 to r im aging diagno sis and therapy of tum ou r are em phatically elabo rated in the papeṙ Key words Ep iderm al grow th facto r (EGF) tum ou r ep iderm al grow th facto r recep2 to r (EGFR ) im aging diagno sis therapy ( ), ( ) 20,,,