The present embodiments provide methods, compounds, and compositions useful for inhibiting KLK3 eRNA expression, which may be useful for treating, preventing, or ameliorating cancer, such as prostate cancer.

Provided are low glycosylated kallikrein I with no or a small amount of glycosylation at the NFS sequence and polyethylene glycol modified product and pharmaceutical applications. KLK1 with lower glycosylation at NFS is more active than KLK1 with higher glycosylation at NFS. A recombinant KLK1 mutant without N-glycosylation at the NFS sequence is also provided, containing only two N-glycosylation sites at NMS and NHT. Glycosylation of the recombinant KLK1 mutant is relatively more consistent, the molecular weight of the product is relatively more homogeneous, the yield is higher, the purification process is simpler, and the biological activity is higher, and the quality is more controllable.

Provided are preparations of tissue kallikrein-1 (KLK1) glycoforms having a defined number of oligosaccharide units per KLK1 molecule. Also provided are mixtures of such glycoforms, pharmaceutical compositions containing such glycoforms or mixtures thereof, methods of obtaining the rhKLK1 glycoforms, and therapeutic uses thereof.

Provided are preparations of tissue kallikrein-1 (KLK1) glycoforms having a defined number of oligosaccharide units per KLK1 molecule. Also provided are mixtures of such glycoforms, pharmaceutical compositions containing such glycoforms or mixtures thereof, methods of obtaining the rhKLK1 glycoforms, and therapeutic uses thereof.

The present invention relates to polyethylene glycol (PEG) modified protein drugs, and a PEGylated tissue kallikrein, a preparation method and use thereof are disclosed. The tissue kallikrein has a sequence as shown in SEQ ID No. 1 or SEQ ID No. 2, and the tissue kallikrein may be natural or recombinant. The PEG has a molecular weight of 20 to 40 kDa, and is conjugated to the N-terminal primary amino of the tissue kallikrein. In addition to the advantages of significantly extended half-life, significantly reduced immunogenicity and stable and uniform structure, the biological activity of the PEGylated KLK1 provided in the present invention is improved to a higher extent, which is more significant in the treatment of cerebral apoplexy and diabetic nephropathy in particular.

Provided are dosage forms of one or more tissue kallikrein-1 (KLK1) polypeptides which have a total KLK1 polypeptide dosage of about 0.1 g/kg to about 10.0 g/kg, including subcutaneous and intravenous dosage forms. Also provided are related devices and methods of use thereof, for example, for treating ischemic and hemorrhagic conditions.

Provided are methods and compositions for using tissue kallikrein-1 (KLK1) to treat or prevent pregnancy disorders such as fetal growth restriction (FGR) and preeclampsia.

Provided are pharmaceutical compositions, kits, and methods for the clinical use of tissue kallikrein-1 (KLK1) polypeptides in polyolefin-containing intravenous (IV) systems, including polyolefin IV bags.

Provided are dosage forms of one or more tissue kallikrein-1 (KLK1) polypeptides which have a total KLK1 polypeptide dosage of about 0.1 g/kg to about 10.0 g/kg, including subcutaneous and intravenous dosage forms. Also provided are related devices and methods of use thereof, for example, for treating ischemic and hemorrhagic conditions.

The present invention pertains to a multiple biomarker for cancer diagnosis and a use thereof and, specifically, to a composition for cancer diagnosis, comprising an agent for measuring the protein or mRNA expression levels of IGFI, KLK2, PKC, and TRPM8. The present inventors confirmed that rapid and accurate cancer diagnosis can be performed by detecting the unique marker combination of IGFI, KLK2, PKC, and TRPM8 of the present invention in serum samples from actual cancer patients and one or more cancers can be simultaneously detected. Thus, the combination of IGFI, KLK2, PKC, and TRPM8 is expected to allow for the rapid and accurate diagnosis of various cancers including prostate cancer.