50 results about "Kinesin" patented technology

The present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.

Provided herein are certain compounds of Formula I: that can be used to treat diseases of proliferating cells. The compounds are KSP kinesin inhibitors, particularly inhibitors of human KSP.

The present application relates to novel antibody 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 prevention of diseases, in particular hyperproliferative and / or angiogenic disorders such as, for example, cancer diseases. Such treatments can be carried out 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.

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.

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 discloses a relative transferring function of kinesin family member KIF1B, a landmark application thereof in predicting tumor patient prognosis and an application method thereof, belonging to the technical field of tumor molecular biology. The invention discloses a relative transferring function of kinesin family member KIF1B, a landmark application of KIF1B expression level in predicting tumor patient prognosis and a detection and application method based on the KIF1B expression level in predicting tumor patient prognosis. In the method, real-time quantitative RT-PCR is carried out to detect the method for KIF1B mRNA expression level; quantitative PCR amplification comprises relative quantitative PCR amplification and absolute quantitative PCR amplification; the KIF1B expression level detection can also adopt a molecular hybridization method to detect the KIF1B mRNA expression level; an immunostaining method and / or immunoblotting method can be adopted to detect the KIF1B protein expression level; a critical value for prognosis judgment is determined according to the KIF1B gene or protein expression level in the primary cancer tissues of recurrent and metastatic positive cases and recurrent and metastatic negative cases of tumor patients; and the patient the critical value of whom is higher than the threshold value has favorable prognosis, and the patient the critical value of whom is lower than the threshold value has poor prognosis.

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.

The invention relates to site specific homogeneous binder drug conjugates of kinesin spindle protein inhibitors, to active metabolites of these conjugates, to processes for preparing these conjugates, to the use of these conjugates for the treatment and / or prophylaxis of diseases and to the use of these conjugates for preparing medicaments for treatment and / or prevention of diseases, in particular hyperproliferative and / or angiogenic disorders such as, for example, cancer diseases. Such treatments can be carried out 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.

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 belongs to the field of biopharmacy and relates to a small hairpin RNA (Ribonucleic Acid) recombination oncolytic adenovirus carrying a target human kinesin (mitotic phase phosphoprotein 1) gene and a preparation method of the recombination oncolytic adenovirus. The invention provides a brand-new liver cancer drug target, namely mitotic phase phosphoprotein 1 which has a broad spectrum that the traditional gene therapy target p53 gene does not have; the invention further provides the preparation method of the small hairpin RNA recombination oncolytic adenovirus for expressing the mitotic phase phosphoprotein 1; and at the same time, the invention provides an application of the recombination oncolytic adenovirus in preparing a cancer treatment drug.

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.

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.