Abstract: The synthesis and use of radiolabeled derivatives of poly-(ADP-ribose) (PARP) inhibitors in positron emission tomography (PET) imaging methods are disclosed. A novel non-radioactive analogue of the PARP inhibitor Talazoparib (TZ) provides a branch point for the syntheses of various radiolabeled Talazoparib derivatives. Aspects of the disclosure include such radiolabeled derivatives and TZ analogues, along with methods of use for diagnosis, treatment, imaging, and theranosis of cancer.

Abstract: Combination therapies for the treatment of cancers are provided. In some embodiments, a flagellin derivative such as CBLB502 is administered in combination with an immune checkpoint therapy (e.g., an anti-PD 1 antibody and an anti-CTLA4 antibody) to treat a cancer in a mammalian subject. In some embodiments, the combination therapy is administered intratumorally or peritumorally.

Abstract: Provided herein are agents, such as antibodies, antibody-drug conjugates, or chimeric antigen receptors, that target B7-H3. Methods of treating cancer are provided, comprising administering to a patient in need thereof an effective amount of an B7-H3-targeting agent. The patient may be selected for treatment if the cancer expresses an increased level of B7-H3.

Abstract: The present disclosure provides radiolabeled compounds of the formula: (I) and (II), as well as precursor compounds of the formula: (VII) wherein the variables are defined herein. The present disclosure also provides radiopharmaceutical compositions comprising the radiolabeled compounds disclosed herein as well as precursor compositions comprising the precursor compounds disclosed herein. The present disclosure further provides methods of imaging using the radiolabeled compounds and/or radiopharmaceutical compositions of the present disclosure as well as kits for the preparation of the radiolabeled compounds and radiopharmaceutical compositions disclosed herein.

Abstract: Zaprinast has been discovered to have activity against glutaminase 1, an important metabolic enzyme in selected cancers, for example, glutamine-dependent cancer types. Thus, glutamine-dependent cancer types, such as IDH1/2 gain-of-function mutant cancers or GLI1 overexpressing cancers, may be particularly sensitive to Zaprinast analogues.

Abstract: Methods of imaging distribution of myeloperoxidase activity in a subject are disclosed. These methods include the use of bioluminescent substrates, including luminol and wavelength-shifted analogues of luminol. Bioluminescent myeloperoxidase substrates that emit light at longer wavelengths compared to luminol are shown to be useful for imaging myeloperoxidase activity in vivo. The disclosed methods can be used for imaging sites of inflammation and other pathological conditions associated with abnormal levels of MPO activity in vivo. Methods of synthesis of luminol analogues are also disclosed.

Abstract: Methods of imaging distribution of myeloperoxidase activity in a subject are disclosed. These methods include the use of bioluminescent substrates, including luminol and wavelength-shifted analogues of luminol. Bioluminescent myeloperoxidase substrates that emit light at longer wavelengths compared to luminol are shown to be useful for imaging myeloperoxidase activity in vivo. The disclosed methods can be used for imaging sites of inflammation and other pathological conditions associated with abnormal levels of MPO activity in vivo. Methods of synthesis of luminol analogues are also disclosed.