摘要:
The present invention relates to 18 F-labeled compounds suitable for positron emission tomography (PET) imaging. The invention further relates to the use of these compounds for carrying out PET scans, imaging the indoleamine 2,3-dioxygenase, pathway, predicting the responsiveness of a subject with a solid tumor to therapies including immunotherapy such as PD-1/PD-L1 inhibition, and determining whether a solid tumor in a subject contains tumor-infiltrating immune cells.
摘要:
In one aspect, the present invention provides a method of inhibiting proliferation of a multiple myeloma cell, the method comprising contacting the cell with BRD9647, thereby inhibiting proliferation of the cell. In another aspect, the present invention provides a method of treating multiple myeloma in a pre-selected subject, the method comprising administering an effective amount of BRD9647 to the subject, wherein the subject is pre-selected by detecting a mutation in an AZIN1 polynucleotide or polypeptide relative to a reference in a biological sample obtained from the subject. In another aspect, the present invention provides a method of modulating benzoylation of an agent in a cell, the method comprising contacting the cell with BRD9647, thereby modulating benzoylation of an agent in the cell.
摘要:
Provided herein are compositions and methods for generating polypeptides using non-natural amino acids (nnAAs) and genetic machinery, wherein the modified polypeptides, such as therapeutic polypeptides, bind to albumin, such as serum albumin. Methods of substituting a non-natural amino acid in a first polypeptide to obtain a modified polypeptide, the nnAA in some instances comprising an albumin targeting group, are disclosed, as are methods for making populations of such modified polypeptides. A therapeutic polypeptide, interleukin-1 receptor antagonist (IL-1RA) is exemplified using the disclosed methods.
摘要:
Radiofluorinated carboximidamides are disclosed as selective IDO enzyme radioligands and generate specific binding in accordance with IDO expression in vitro. MicroPET experiments indicate [ 18 F]IDO49 specifically accumulate in IDO-expressing tumors which confirmed by Western blot and IHC analysis supported. Using Hela tumor bearing models with IFN-γ treatment confirmed that [ 18 F]IDO49 accumulation in the IFN- γ treatment tumor mouse. These results can have implications that [ 18 F]IDO49 has substantial potential as an imaging agent that targets IDO in tumors.
摘要:
The present invention provides compounds of Formula (I) or Formula (II), pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
摘要:
The present invention relates to novel tracer substances useful in the analysis for semi-volatile organic contaminants (SVCs) such as PCBs (polychlorinated biphenyls). The invention also describes methods for establishing multilayered sealant barriers towards SVCs, which barriers contain said tracer substances, and methods for assessing the integrity of such barriers.
摘要:
Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.