Cholecystokinin-2 receptor targeted compounds and use thereof
The present disclosure provides, inter alia, novel compounds targeting cholecystokinin-2 receptor (CCK2R) expressed on the surface of cancer cells. Also provided are methods for imaging, diagnosing, and/or treating cancers using the same.
1 . A peptidomimetic conjugate having a structure selected from one of the following:
2 . The peptidomimetic conjugate according to claim 1 , wherein the peptidomimetic conjugate is capable of chelating a radionuclide.
3 . The peptidomimetic conjugate according to claim 2 , wherein the radionuclide is 203 Pb or 212 Pb.
4 . The peptidomimetic conjugate according to claim 2 , wherein the radionuclide is 61 Cu, 64 Cu, 67 Cu, or 68 Ga.
5 . A method for imaging or diagnosing a subject suffering from a cancer associated with expression of cholecystokinin-2 receptor (CCK2R), the method comprising administering the peptidomimetic conjugate of claim 1 to the subject, wherein the peptidomimetic conjugate is complexed with a radionuclide suitable for medical imaging use, and imaging the subject.
6 . A method for treating a subject suffering from a cancer associated with expression of CCK2R, the method comprising administering the peptidomimetic conjugate of claim 1 to the subject, wherein the peptidomimetic conjugate is complexed with a radionuclide suitable for therapeutic use, in a dosage sufficient to kill cancer cells.
7 . A method of diagnosing and treating a subject suffering from a cancer associated with expression of CCK2R, the method comprising:
diagnosing the subject by administering the peptidomimetic conjugate of claim 1 to the subject, wherein the peptidomimetic conjugate is complexed with a radionuclide suitable for medical imaging use, and imaging the subject to diagnose the subject as being afflicted with the cancer, and
treating the subject diagnosed as being afflicted by the cancer, by administering the peptidomimetic conjugate of claim 1 to the subject, wherein the peptidomimetic conjugate is complexed with a radionuclide suitable for therapeutic use, in a dosage sufficient to kill cancer cells.
8 . The method according to claim 5 , wherein the subject is imaged using single-photon emission computed tomography (SPECT) imaging or positron emission tomography (PET), optionally in combination with computed tomography (CT) imaging.
9 . The method according to claim 7 , wherein the cancer associated with expression of CCK2R is selected from thyroid cancer, lung cancer, tumors of the nervous system, ovarian cancer, gastrointestinal cancer, neuroendocrine tumors, neuroblastoma, endometrial cancer, insulinomas, prostate cancer, breast cancer, vipomas, bronchial carcinoids, ileal carcinoids, and sarcomas.