Anti-HER2 polypeptides derivatives as new diagnostic molecular probes
The present invention provides new polypeptide derivatives binding to Human Epidermal Growth Factor Receptor 2 (HER2) and their conjugates thereof, and to their use as a diagnostic agent, particularly for early detection, patient stratification and treatment monitoring of forms of cancer characterized by over-expression of HER2.
1 . A polypeptide that specifically binds to Human Epidermal Growth Factor Receptor 2 (HER2), comprising the amino acid sequence of SEQ ID NO: 1.
2 . The polypeptide according to claim 1 , consisting of the amino acid sequence of SEQ ID NO: 1.
3 . The polypeptide according to claim 1 , comprising the amino acid sequence of SEQ ID NO: 2.
4 . The polypeptide according to claim 3 , consisting of the amino acid sequence of SEQ ID NO: 2.
5 . The polypeptide according to claim 1 , which is linked to an imaging agent.
6 . The polypeptide according to claim 5 , wherein the imaging agent is selected from the group consisting of a fluorophore moiety, a magnetic or paramagnetic moiety, a radiolabeling isotope, an affinity label, an X-ray responsive moiety, an ultrasound responsive moiety, and a photoacoustic responsive imaging moiety.
7 . The polypeptide according to claim 6 , wherein the fluorophore moiety is a cyanine dye.
8 . The polypeptide according to claim 6 , wherein the radiolabeling isotope is selected from 18 F, 124 I, 11 C, 64 Cu, 68 Ga, 89 Zr, 44 Sc, 99m Tc, indium, gallium, yttrium, bismuth, radioactinides and radiolanthanides.
9 . The polypeptide according to claim 6 , wherein the affinity label is biotin.
10 . A diagnostic or imaging composition comprising the polypeptide as defined in claim 5 with pharmaceutically acceptable carriers, excipients, diluents and/or additives.
11 . A method of imaging comprising:
administering the composition according to claim 10 to a subject; and
imaging the subject with a diagnostic device.
12 . The method according to claim 11 , wherein said imaging is performed using an imaging technique selected from magnetic resonance, positron-emission tomography (PET), computed tomography (CT), ultrasounds (US), photoacoustic imaging (PAI), near-infrared fluorescence imaging (NIRF) and single photon emission computed tomography (SPECT).
13 . A conjugate comprising a polypeptide consisting of the amino acid sequence of SEQ ID NO: 1, wherein the polypeptide is linked to an imaging agent.
14 . The conjugate according to claim 13 , wherein the imaging agent is selected from the group consisting of a fluorophore moiety, a magnetic or paramagnetic moiety, a radiolabeling isotope, an affinity label, an X-ray responsive moiety, an ultrasound responsive moiety, and a photoacoustic responsive imaging moiety.
15 . The conjugate according to claim 14 , wherein the fluorophore moiety is a cyanine dye.
16 . The conjugate according to claim 14 , wherein the radiolabeling isotope is selected from 18 F, 124 I, 11 C, 64 Cu, 68 Ga, 89 Zr, 44 Sc, 99m Tc, indium, gallium, yttrium, bismuth, radioactinides and radiolanthanides.
17 . The conjugate according to claim 14 , wherein the affinity label is biotin.
18 . A diagnostic or imaging composition comprising the conjugate as defined in claim 13 with pharmaceutically acceptable carriers, excipients, diluents and/or additives.
19 . A method of imaging comprising:
administering the composition according to claim 18 to a subject; and
imaging the subject with a diagnostic device.
20 . The method according to claim 19 , wherein said imaging is performed using an imaging technique selected from magnetic resonance, positron-emission tomography (PET), computed tomography (CT), ultrasounds (US), photoacoustic imaging (PAI), near-infrared fluorescence imaging (NIRF) and single photon emission computed tomography (SPECT).