46 results about "Kinesin" patented technology

The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

The invention relates to novel prodrugs or conjugates of the general formula (Ia)

in which La, n, R and D have the definitions given in the description and which have a structural motif reduced to an asparagine derivative as cleavage site for tumour-associated proteases such as legumain, in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are released by legumain cleavage, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers. Reduction of the legumain-cleavable substrate peptide sequence to an asparagine derivative as structural motif, as a result of slowed legumain cleavage, achieves an increase in stability in the lysosomes of healthy organs while simultaneously maintaining the high anti-tumour effect.

Specific binder-drug conjugates (ADCs) of kinesin spindle protein inhibitors, effective metabolites of these ADCs, processes for preparing these ADCs, the use of these ADCs for the treatment and/or prevention of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases, are described.

The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.

The invention provides methods of treating a meiotic kinase-associated disease, preferably the meiotic kinase HSET, by administering an inhibitor of the meiotic kinase. Preferably, the disease is associated with the presence of supernumerary centrosomes, such as cancer. Methods of inhibiting the growth of a tumor cell by contacting the cell with an inhibitor of a meiotic kinase, preferably HSET, are also provided. Screening methods for identifying inhibitors of the meiotic kinase HSET are also provided. Methods of selecting subjects for treatment with an inhibitor of a meiotic kinase, such as HSET, are also provided.

As described herein, chromosomal missegregations, chromosomal micronuclei, cytosolic DNA, and combinations thereof are indicative of metastatic cancer. Methods and compositions are described herein that are useful for detection and treatment of patients with chromosomal instabilities such as chromosomal missegregations, chromosomal micronuclei, cytosolic DNA, and combinations thereof. For example,some of the methods and compositions include use of kinesin-13 proteins such as Kif2b, MCAK/Kif2c, or KIF13A. The methods and compositions can also include inhibitors of STING, ENPP1, cGAS, NF-kB transcription factor p52, NF-kB transcription factor RelB, or any combination thereof. Methods are also described for identifying compounds that are effective for treatment of cancer, including metastatic cancer.

An electric driven protein immobilizing module and method aims at immobilizing proteins rapidly and steadily on the surface of a selected support. The invention employs the characteristics of proteins/enzymes forming a slightly negative charge in a buffer solution. An external electric field is set up to drive the proteins/enzymes to be adsorbed onto the support. The invention improves upon conventional absorption or bonding methods that fix the protein in a non-directional approach which results in masking the protein active site and subsequently loss the protein activity. Thus activity of the protein/enzyme improved, while the time-consuming problem and enzymatic activity loss problem of incubation and vacuum absorption method may be avoided.

The invention belongs to the technical field of protein, and discloses an MdrP mutant gene, amino acid, and protein function and drug accumulation activity detection. According to the invention, CCCPis added to the Buffer containing cations (Na<+>, K<+>) to remove the transmembrane H<+> gradient, only transmembrane cation gradient is retained to drive protein translocation, or Monensin or Nigericin is added in the buffer to remove the cation gradient, and only the transmembrane H<+> gradient is retained to drive the protein translocation, and a relative quantitative comparison between different driving effects can be realized. The important function of highly conserving amino acid site of the MdrP protein can be clarified, and the MdrP protein can be proved as an H<+> and Na<+> driven drug efflux protein; N146 is the H<+> binding site, D223 and Q242 are Na<+>, H<+> competitive binding sites, or can be a favorable theoretical support for understanding the MFS family of drug resistanceproteins.

The invention discloses a polysubstituted 2-aminopyridine compound and application thereof in preparation of anti-tumor drugs. The polysubstituted 2-aminopyridine compound is characterized by having the general formula as shown in the figure (I) in the specification, wherein R1 and R2 are each independently selected from substituted phenyl, substituent of the R1 and the R2 is selected from C1-C3 alkyl, C1-C3 alkoxy and halogen, R3 is selected from hydrogen, C1-C3 alkoxy, benzyl or substituted benzyl, substituent of the R3 is selected from C1-C3 alkyl, C1-C3 alkoxy and halogen, and R4 and R5 are each independently selected from hydrogen, C1-C3 alkyl and C1-C3 alkoxy. The polysubstituted 2-aminopyridine compound has a remarkable anti-tumor metastasis effect and acts on brand-new tumor metastasis kinesin WSB-1 (WD-40 repeat-containing SOCS Box protein) under the hypoxia condition, so that the tumor metastasis process is directly inhibited, and the compound has great significance in the anti-tumor metastasis drugs with a novel development action mechanism and high specificity.

The invention belongs to the field of molecular biology, and particularly relates to a sarcoma radiotherapy resistance-related diagnostic marker and application. According to application of IF18B as asarcoma biomarker, the IF18B is highly expressed in sarcoma tissue, and tumor cell radiotherapy sensitivity can be improved by inhibiting kinesin family member 18B (KIF18B) expression. According to asarcoma detection product, the sarcoma detection product includes a reagent for detecting KIF18B expression, and is a product used for sarcoma diagnosis, radiotherapy means therapeutic effect evaluation and prognosis judgment. According to the diagnostic marker, genes significantly differential in carcinoma and para-carcinoma tissues in all sarcoma subtypes are widely screened, and are intersected with differentially expressed genes (DEGs) in carcinoma and para-carcinoma tissues of soft tissue sarcoma in a The Cancer Genome Atlas (TCGA) database, and it is the first time to discover that thegenes can be used as targets in all subtypes of sarcomas so as to improve huge differences of treatment schemes for patients with different subtypes of sarcomas at present; and the radiotherapy resistance-related gene KIF18B is obtained by further screening, which proves that the radiotherapy sensitivity of sarcoma cells can be enhanced by inhibiting the KIF18B, and the KIF18B can be used as a specific target for sarcoma radiotherapy. According to the diagnostic marker, by taking the KIF18 as the biomarker and with a targeting therapy, a new thought is provided for sarcoma treatment, and detection indexes are also provided for radiotherapy means therapeutic effect evaluation and prognosis judgment, and the diagnostic marker has important clinical application value.

The invention belongs to the technical field of medicines, and specifically relates to the application of a compound in the preparation of anti-cardiovascular and cerebrovascular disease drugs; the compound of the invention can inhibit the activity and aggregation of platelets, more effectively inhibit the formation of thrombus, and has no effect on normal physiological activity. Influence, better overcome the shortcomings of KIF; thus it can resist cardiovascular and cerebrovascular diseases, and has a good clinical application prospect.