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THE QUARTERLY JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Rivista di Medicina Nucleare e Imaging Molecolare


A Journal on Nuclear Medicine and Molecular Imaging
Affiliated to the Society of Radiopharmaceutical Sciences and to the International Research Group of Immunoscintigraphy
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The Quarterly Journal of Nuclear Medicine 2003 December;47(4):321-36

Copyright © 2009 EDIZIONI MINERVA MEDICA

lingua: Inglese

Radiolabelled peptides and low molecular weight proteins in metabolic diseases

Aprile C.

“S. Maugeri” Foundation Occupational Health and Rehabilitation Clinic IRCCS, Nuclear Medicine Unit, Pavia, Italy


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During the ­last ­decade ­there has ­been a tre­men­dous ­effort to devel­op ­labelled pep­tides for diag­no­sis and ther­a­py. The ­main ­goal has ­been to devel­op ­tumor imag­ing/ther­a­peu­tic ­agents, as ­well as pep­tides direct­ed to the ­study of throm­bo­sis and infec­tion. Relatively few ­efforts ­have ­been ­made to devel­op pep­tides direct­ed to the ­study of meta­bol­ic dis­eas­es. Ideally, a pep­tide suit­able for the ­study of metab­olism ­should be con­struct­ed keep­ing in ­mind the fol­low­ing char­ac­ter­is­tics: a) pre­served affin­ity con­stant, b) pre­served or ­improved spec­i­fic­ity for its bind­ing ­site, c) ­increased bio­log­i­cal ­half-­life in com­par­i­son ­with the par­ent pep­tide, d) label­ling ­with a γ or posi­tron emit­ter ­whose phys­i­cal ­half-­life ­fits ­with the bio­log­i­cal ­half-­life, e) ­strong bind­ing of the ­nuclide to the mole­cule so ­that it can­not be ­released ­after inter­nal­iza­tion. In ­this ­paper ­some of the pep­tides or low molec­u­lar ­weight pro­teins ­along ­with ­some ana­logues ­which ­have ­been ­employed in experi­men­tal stud­ies and in ­humans are ­reviewed, ­with ­major empha­sis on amy­loid seek­ers, insu­lin and lep­tin. Many of ­these radio­phar­ma­ceu­ti­cals ­have ­been ­labelled ­with ­iodine iso­topes, how­ev­er ­their in ­vivo appli­ca­tion suf­fer of ­severe lim­i­tra­tions due to rap­id ­release of ­iodine ­after inter­nal­iza­tion. On the oth­er ­hand, new per­spec­tives are ­opened by new radio­flu­o­ri­na­tion tech­niques, ­which ­offer the ­unique advan­tage to quan­ti­fy ­organ ­uptake and kinet­ics, param­e­ters ­which are of par­a­mount impor­tance in meta­bol­ic stud­ies.

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