Albany Medical College

Clf Medical Technology Acceleration Program, Inc.

Ordway Research Institute, Inc.

Herbert I Jacobson

Thomas T Andersen

James A Bennett

Fassil B Mesfin

Alberto Bryan

Leroy Joseph

George C Shields

Karl N Kirschner

The invention relates to compounds that are analogs of a cyclic peptide, cyclo[EKTOVNOGN], AFPep, that has anti-estrotrophic activity. The analogs of the invention include peptides and peptidomimetics that inhibit estrogen receptor-dependent cell proliferation. The compounds of the invention are useful for treating cell proliferative disorders or physiological conditions characterized by undesirable or unwanted estrogen induced cell proliferation, including breast cancer.

Alpha-fetoprotein 'ring and tail' peptides

The invention relates to compounds that are analogs of a cyclic peptide, cyclo[EKTOVNOGN] (SEQ ID NO: 13), AFPep, that has anti-estrotrophic activity. The analogs of the invention include peptides and peptidomimetics that inhibit estrogen receptor-dependent cell proliferation. The compounds of the invention are useful for treating cell proliferative disorders or physiological conditions characterized by undesirable or unwanted estrogen induced cell proliferation, including breast cancer.

The invention relates to compounds that include peptides that inhibit estrogen receptor dependent cell proliferation. The compounds of the invention are useful for treating cell proliferative disorders or physiological conditions characterized by undesirable or unwanted estrogen induced cell proliferation, including breast cancer.

Alpha-fetoprotein peptides

Therapeutic compounds which are cell proliferation modulators, preferably inhibitors. These modulators contain amino acid structures that are arranged as a hydrophilic analog of an alpha-fetoprotein. The modulator may be a peptide itself, e.g., an octapeptide like that of SEQ ID NO: 5; a peptidomimetic; or may be in the form of a pharmaceutically acceptable scaffold, such as a polycyclic hydrocarbon to which is attached the necessary amino acid structures for biological and/or chemical activity. The modulators of the invention are distinguished in one aspect over previous compounds in that they are orally active, and therefore do not have to be injected into the patient. The compositions and methods are useful for reducing estrogen-dependent and estrogen-independent growth of cells, and treating or preventing cancer, such as breast cancer, brain cancer, head-and-neck cancer, thyroid cancer, lung cancer, colon cancer, ovarian cancer, prostate cancer, cervical cancer, and skin cancer. The treatment or prevention methods can include the use of tamoxifen therapy in combination with the peptide therapy.

Alpha-fetoprotein peptides and uses thereof

The invention relates to compounds that include peptide and peptidomimetics that inhibit estrogen receptor dependent cell proliferation. The compounds of the invention are useful for treating cell proliferative disorders or physiological conditions characterized by undesirable or unwanted estrogen induced cell proliferation, including breast cancer.

The invention provides diagnostic procedures wherein the presence or absence of a cell-proliferating disorder, e.g., a breast cancer, may be determined. The imaging agents of the invention include alpha-fetoprotein hydrophilic analogs which have been determined to target cancers, e.g., breast cancer, and are also anti-cell proliferating in nature. These modulators contain amino acid structures which are arranged as a hydrophilic analog of an alpha-fetoprotein. The modulator may be a peptide; a peptidomimetic; or may be in the form of a pharmaceutically acceptable scaffold, such as a polycyclic hydrocarbon to which is attached the necessary amino acid structures. The imaging agents of the invention further comprise an imaging moiety that allows for the imaging of the area targeted by the imaging agent.

Alpha-fetoprotein peptides and uses for imaging

The subject invention addresses the need for methods of treatment and prevention of breast cancer, and other cancers, by providing a peptide of eight to twenty amino acids in length which comprises a hydrophilic analog of an alpha-fetoprotein peptide having SEQ ID NO:6: EMTPVNPG. The peptides may be linear, but are preferably cyclic. The peptides may be provided as dimers or other multimers. A composition comprising the peptide, an antibody that specifically binds to the peptide, a method of reducing estrogen-stimulated growth of cells using the peptide, as well as a method of treating or preventing cancer, such as breast cancer, are also provided. The treatment or prevention method can include the use of tamoxifen therapy in combination with the peptide therapy.

Therapeutic compounds which are cell proliferation modulators, preferably inhibitors. These modulators contain amino acid structures that are arranged as a hydrophilic analog of an alpha-fetoprotein. The modulator may be a peptide itself, e.g., an octapeptide like that of SEQ ID NO: 5; a peptidomimetic; or may be in the form of a pharmaceutically acceptable scaffold, such as a polycyclic hydrocarbon to which is attached the necessary amino acid structures for biological and/or chemical activity. The modulators of the invention are distinguished in one aspect over previous compounds in that they are orally active, and therefore do not have to be injected into the patient. The compositions and methods are useful for reducing estrogen-stimulated growth of cells, and treating or preventing cancer, such as breast cancer. The treatment or prevention methods can include the use of tamoxifen therapy in combination with the peptide therapy.

The subject invention addresses the need for methods of treatment and prevention of breast cancer, and other cancers, by providing a peptide of eight to twenty amino acids in length which comprises a hydrophilic analog of an alpha-fetoprotein peptide having SEQ ID NO: 6: EMTPVNPG. The peptides may be linear, but are preferably cyclic. The peptides may be provided as dimers or other multimers. A composition comprising the peptide, an antibody that specifically binds to the peptide, a method of reducing estrogen-stimulated growth of cells using the peptide, as well as a method of treating or preventing cancer, such as breast cancer, are also provided. The treatment or prevention method can include the use of tamoxifen therapy in combination with the peptide therapy.

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Albany, NY, United States of America

Herbert I Jacobson