Abstract: The present invention provides a method of regulating the expression of the urokinase type plasminogen activator (“uPA”) gene in a mammalian cell comprising the steps of: identifying a target nucleotide sequence in a gene of interest, obtaining a methylated antisense oligonucleotide sequence complementary to the target sequence, said oligonucleotide sequence having 5 methylated cytosine in place of unmethylated cytosine in the region complementary to the CpG region in the target nucleotide sequence, and exposing the cell to copies of the oligonucleotide sequence under suitable conditions, such that the oligonucleotide sequence enters the nucleus and interacts with the target sequence to promote methylation of the target nucleotide sequence.

Abstract: The present invention relates to the use of uPAR-binding molecule-drug conjugates capable of specifically binding a urokinase plasminogen activator receptor (uPAR) as therapeutic and diagnostic reagents for the treatment and monitoring of metastases. The present invention provides methods of treatment of metastases, comprising administering to a subject a uPAR-binding molecule-chemotherapeutic conjugate that is capable of binding to and internalizing into uPAR-expressing cells. The present invention further provides pharmaceutical compositions and kits comprising such conjugates. The present invention further provides methods and compositions relating to combination therapy for cancer involving or mediated by uPAR-expressing cells using uPAR-binding molecule-drug conjugates of the invention.

Abstract: The present invention discloses the use of PSP-94, PCK3145 and other derivatives and biologically active analogues for treating a patient having a condition such as metastasis, metastatic cancer, a condition associated with elevated levels of parathyroid hormone-related protein (PTHrP), PTHrP-induced osteolysis and/or hypercalcemia of malignancy. These compounds were found to be effective treatment modalities for bone metastasis caused by prostate cancer. Furthermore, decrease in cellular and plasma PTHrP levels as well as plasma calcium levels observed by treatment with such compound can serve as useful biochemical markers for monitoring the efficacy of these anti-metastatic compounds.

Abstract: The present invention relates to the use of molecules capable of specifically binding a urokinase plasminogen activator receptor (uPAR) as diagnostic reagents for the detection of metastases in vivo. Such metastases can include, but are not limited to, micrometastases.

Abstract: The present invention provides a method of regulating the expression of the urokinase type plasminogen activator (“uPA”) gene in a mammalian cell comprising the steps of: identifying a target nucleotide sequence in a gene of interest, obtaining a methylated antisense oligonucleotide sequence complementary to the target sequence, said oligonucleotide sequence having 5 methylated cytosine in place of unmethylated cytosine in the region complementary to the CpG region in the target nucleotide sequence, and exposing the cell to copies of the oligonucleotide sequence under suitable conditions, such that the oligonucleotide sequence enters the nucleus and interacts with the target sequence to promote methylation of the target nucleotide sequence.

Abstract: The present invention relates to the use of molecules capable of specifically binding a urokinase plasminogen activator receptor (uPAR) as diagnostic reagents for the detection of metastases in vivo. Such metastases can include, but are not limited to, micrometastases.