Abstract: The present invention provides a selective CXCR4 binding peptide conjugate (“PC”), and a method for using and producing the same. In particular, the selective CXCR4 binding peptide conjugate of the invention comprises a peptide portion that selectively binds to CXCR4 and a medically useful compound, such as an imaging agent, a diagnostic agent, or a therapeutically or pharmaceutically active compound. In one particular embodiment, the selective CXCR4 binding peptide conjugate (“PC”) is of the formula: or a pharmaceutically acceptable salt thereof, wherein a, b, AA1, AA2, Ar1, X1, and AA3 are those defined herein. The peptide conjugate of the invention can be used in a variety of medical applications including, but not limited to, a targeted drug delivery or imaging a patient or diagnosing a patient for a disease or a clinical condition associated with overexpression and/or upregulation of CXCR4, such as cancers, HIV infection, and immune disorders.

Abstract: The present invention provides method treating a subject suffering from a clinical condition associated with CXCR4 activity, said method comprising administering to a subject in need of such a treatment a therapeutically effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein a is 0 or 1; AA1 along with the sulfur atom that is attached thereto is 3-mercaptopropionic acid, optionally substituted cysteine, or optionally substituted homocysteine; AA2 along with the sulfur atom that is attached thereto is cysteine or homocysteine; Ar1 is an optionally substituted aryl; X1 is Arg, Dap, Dab, Orn, Lys, Dap(iPr), Dab(iPr), Orn(iPr), or Lys(iPr); X2 is Arg, Dap, Dab, Orn, Lys, Dap(iPr), Dab(iPr), Orn(iPr), Lys(iPr), a D-isomer thereof, or absent; X3 is Gly or absent; X4 is Phe, 2Nal, 1Nal, or absent; X5 is Gly or absent; R2 is —OR4 or —NHR5; R4 is H or alkyl; and R5 is H, alkyl, optionally substituted aryl, optionally substituted aralkyl.

Abstract: The present invention provides a compound that can be used for targeted drug delivery, imaging a patient, or diagnosing a subject for a clinical condition which is believed to be associated with overexpression and/or upregulation of CXCR4. In particular, the present invention provides a high affinity CXCR4 selective binding ligand peptide conjugate (PC) of the Formula: P-(L-A)n (I) or a pharmaceutically acceptable salt thereof, and a method for using and producing the same. The high affinity CXCR4 selective binding ligand peptide conjugate (PC) of the invention is useful in diagnosing, treating or imaging a patient. In compound of Formula (I), n is an integer from 1 to the sum of (the total number of amino acid resides in P and the total number of side-chain functional group in the amino acid residue of P); each A is independently a diagnostic agent, a therapeutic agent, or an imaging agent; L is a linker or absent; and P is a high affinity CXCR4 selective binding peptidyl ligand.

Abstract: The present invention provides compounds that are antagonists of CXCR4 and methods for using the same for treatment of a clinical condition associated with CXCR4 activation. In particular, compounds of the invention include cyclic peptides. Compounds of the invention can be used to treat a variety of clinical conditions, including but not limited to, cancers, pulmonary fibrosis, HIV infection, rheumatoid arthritis, and other immune disorders. In addition, compounds of the invention can also be used in stem cell therapy.

Abstract: The present invention provides compounds that are antagonists of CXCR4 and methods for using the same for treatment of a clinical condition associated with CXCR4 activation. In particular, compounds of the invention include cyclic peptides. Compounds of the invention can be used to treat a variety of clinical conditions, including but not limited to, cancers, pulmonary fibrosis, HIV infection, rheumatoid arthritis, and other immune disorders. In addition, compounds of the invention can also be used in stem cell therapy.