8 results about "Cathepsin K" patented technology

The present invention relates to a cathepsin K inhibitor comprising or consisting of Formula (I) (X1)(X2)(X3)(X4)(Y)(X5)(X6)(X7) Formula (I), wherein (X1) is the amino acid K; (X2) is an amino acid selected from R and W, and is preferably R; (X3) is an amino acid selected from R and W, and is preferably R; (X4) is the amino acid L; (X5) is an amino acid selected from Y, V and W, and is preferably V or Y, and is most preferably V; (X6) is an amino acid selected from I, M, L, W and R, and is preferably I, L or W; and is most preferably I; (X7) is an amino acid selected from H, W, A T, R; and is preferably H or R, and is most preferably R; and (Y) is a Michael acceptor. The present invention also relates to a cathepsin L inhibitor comprising or consisting of Formula (II) (X1)(X2)(X3)(X4)(Y)(X5)(X6)(X7) Formula (II), wherein (X1) is the amino acid K; (X2) is the amino acid R; (X3) is an amino acid selected from R, L and M, and is preferably L; (X4) is an amino acid selected from L, W, F and Y, and is preferably W; (X5) is an amino acid selected from V, H and R, and is preferably V; (X6) is an amino acid selected from M, L, I, W and R, and is preferably L; (X7) is an amino acid selected from W, A T, R; and is preferably W; and (Y) is a Michael acceptor.

The invention relates to the technical field of biological medicines, and discloses a pharmaceutical composition, a preparation method and application thereof, and a medicine for promoting wound healing. The pharmaceutical composition comprises a cathepsin K inhibitor and an exosome. Through combined use of the cathepsin K inhibitor and the exosome, especially the exosome derived from mesenchymal stem cells, the defects of an existing diabetes wound treatment method are overcome, collagen degradation is reduced, and collagen deposition is promoted; angiogenesis is enhanced, and wound blood supply is improved; the cell survival rate is improved; energy metabolism is recovered, and cell functions are enhanced. Moreover, the purposes of repairing and healing wounds more efficiently can be achieved on the premise that the dosage is smaller, the production cost is reduced, and the treatment feasibility and clinical popularization value are improved.

The invention provides a cathepsin K (CTSK) responsive polypeptide derivative and application thereof. The CTSK responsive polypeptide derivative provided by the invention has the following structure: Ar-L1-dipeptide linker-hydrophobic membrane permeation sequence-CTSK response sequence-bone targeting sequence, and can be self-assembled to form bone targeting nanoparticles. According to the CTSK responsive polypeptide derivative and the bone targeting nanoparticles obtained from the CTSK responsive polypeptide derivative disclosed by the invention, the combination of osteoclast and apoptotic body mediated bone regeneration is specifically eliminated by utilizing self-assembly triggered by CTSK, so that bone balance is recovered, and physiological bone remodeling is not destroyed.

The invention relates to the technical field of biological medicines, in particular to application of cathepsin K (CTSK) or a coding gene thereof serving as a target to preparation of an ARDS diagnosis product or treatment product or preparation of an ARDS related pulmonary fibrosis diagnosis product or treatment product. The invention discloses that the CTSK level in serum or pulmonary alveolar lavage fluid can be used for accurately evaluating whether ARDS or ARDS-related pulmonary fibrosis occurs or not and the degree of pulmonary alveolar-capillary membrane injury; aRDS caused by different factors can be used as a biomarker; compared with existing evaluation indexes, the CTSK has higher response speed and higher sensitivity to ARDS or ARDS-related pulmonary fibrosis, is beneficial to early diagnosis and prognosis evaluation of acute lung injury, and has good market transformation prospects.

The instant disclosure describes an injectable composition comprising a Cathepsin K blocking amount of a polydisperse preparation of collagen macropeptides with an average molecular weight between about 10 and about 100 kDa and an acceptable sterile injection vehicle. Methods of treating arthritis and methods of manufacturing injectable composition are also disclosed.

The invention discloses a macrophage targeting probe, a preparation method and application, the probe is based on blood platelets coupled with a CD41 antibody, and the surfaces of the blood platelets are further modified with phospholipid compounds coupled with a cathepsin substrate peptide fragment-fluorophore structure. The probe has the advantages of good macrophage targeting property, low immunogenicity and capability of crossing a biological membrane barrier. Meanwhile, the cathepsin substrate peptide fragment-fluorophore structure in the probe can generate fluorescence only after being cut by cathepsin K in the macrophage, real-time fluorescence tracking imaging of the functional state and position of the macrophage can be effectively achieved, and then early diagnosis of diseases and guidance of disease treatment are achieved.

The present invention relates to a cathepsin K inhibitor having the structure as shown in formula (0) and / or formula (II), wherein cyanopyrimidine or a keto group as an electrophilic group is a key group to exert a good inhibitory effect on cathepsin K. Further provided are a preparation method therefor and use thereof. The provided cathepsin K inhibitor has a relatively high inhibitory effect and selectivity, and is expected to be used for treating diseases including thyroid diseases, cardiovascular diseases, bone diseases and gum diseases.

Provided herein are methods of diagnosing, monitoring and treating a disease or disorder using cathepsin K as a biomarker. The disease or disorder may be an inflammatory disease, an autoimmune disease, or sepsis. Also, provided herein are compositions for treating the disease or disorder diagnosed by the described methods.