A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned Drug
Several studies investigated the use of <sup>99m</sup>Tc-labelled Aprotinin as an amyloid seeker some years ago. In vitro tests showed high binding affinity for several types of amyloid fibrils accompanied by an excellent specificity. Initial human studies demonstrated good accuracy in d...
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| Format: | Article |
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MDPI AG
2022-06-01
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| Series: | Biomedicines |
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| Online Access: | https://www.mdpi.com/2227-9059/10/6/1377 |
| _version_ | 1797489698287910912 |
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| author | Carlo Aprile Lorenzo Lodola |
| author_facet | Carlo Aprile Lorenzo Lodola |
| author_sort | Carlo Aprile |
| collection | DOAJ |
| description | Several studies investigated the use of <sup>99m</sup>Tc-labelled Aprotinin as an amyloid seeker some years ago. In vitro tests showed high binding affinity for several types of amyloid fibrils accompanied by an excellent specificity. Initial human studies demonstrated good accuracy in detecting cardiac involvement. Scintigraphy results were confirmed in a group of 28 endomyocardial biopsies. Unfortunately, clinical studies were halted because of a temporary suspension of the vector protein (Trasylol) and public health concerns over prion contamination of the bovine origin compound. To obviate these limitations, efforts have been made to label a recombinant Aprotinin with 99mTc, which exhibits the same affinity for h-insulin fibrils. With the aim of developing a PET tracer, the same recombinant protein was labeled with Gallium. The introduction of a bifunctional chelator did not affect fibril affinity. Finally, a synthetic peptidic fragment, the cyclic 30-51 SS, was synthetized. After direct technetium labeling, an impressive increase in affinity was demonstrated. This peptide appears to be a potential candidate for Gallium labeling through a bifunctional chelator for PET imaging. |
| first_indexed | 2024-03-10T00:21:20Z |
| format | Article |
| id | doaj.art-ecdc6c787b59434096d8799b6a87167d |
| institution | Directory Open Access Journal |
| issn | 2227-9059 |
| language | English |
| last_indexed | 2024-03-10T00:21:20Z |
| publishDate | 2022-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Biomedicines |
| spelling | doaj.art-ecdc6c787b59434096d8799b6a87167d2023-11-23T15:43:47ZengMDPI AGBiomedicines2227-90592022-06-01106137710.3390/biomedicines10061377A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned DrugCarlo Aprile0Lorenzo Lodola1IRCCS Fondazione Policlinico San Matteo, Nuclear Medicine Unit, I-27100 Pavia, ItalyIRCCS Fondazione Policlinico San Matteo, Nuclear Medicine Unit, I-27100 Pavia, ItalySeveral studies investigated the use of <sup>99m</sup>Tc-labelled Aprotinin as an amyloid seeker some years ago. In vitro tests showed high binding affinity for several types of amyloid fibrils accompanied by an excellent specificity. Initial human studies demonstrated good accuracy in detecting cardiac involvement. Scintigraphy results were confirmed in a group of 28 endomyocardial biopsies. Unfortunately, clinical studies were halted because of a temporary suspension of the vector protein (Trasylol) and public health concerns over prion contamination of the bovine origin compound. To obviate these limitations, efforts have been made to label a recombinant Aprotinin with 99mTc, which exhibits the same affinity for h-insulin fibrils. With the aim of developing a PET tracer, the same recombinant protein was labeled with Gallium. The introduction of a bifunctional chelator did not affect fibril affinity. Finally, a synthetic peptidic fragment, the cyclic 30-51 SS, was synthetized. After direct technetium labeling, an impressive increase in affinity was demonstrated. This peptide appears to be a potential candidate for Gallium labeling through a bifunctional chelator for PET imaging.https://www.mdpi.com/2227-9059/10/6/1377cardiac amyloidosistechnetium aprotininrecombinant aprotinin30-51 SS cyclic peptide: synthetic insulin fibrilsradioactive GalliumPET |
| spellingShingle | Carlo Aprile Lorenzo Lodola A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned Drug Biomedicines cardiac amyloidosis technetium aprotinin recombinant aprotinin 30-51 SS cyclic peptide: synthetic insulin fibrils radioactive Gallium PET |
| title | A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned Drug |
| title_full | A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned Drug |
| title_fullStr | A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned Drug |
| title_full_unstemmed | A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned Drug |
| title_short | A Narrative Review of <sup>99m</sup>Tc-Aprotinin in the Diagnosis of Cardiac Amyloidosis and a New Life for an Unfairly Abandoned Drug |
| title_sort | narrative review of sup 99m sup tc aprotinin in the diagnosis of cardiac amyloidosis and a new life for an unfairly abandoned drug |
| topic | cardiac amyloidosis technetium aprotinin recombinant aprotinin 30-51 SS cyclic peptide: synthetic insulin fibrils radioactive Gallium PET |
| url | https://www.mdpi.com/2227-9059/10/6/1377 |
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