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52 results about "Sarcoma" patented technology

A rare type of cancer that grow in connective tissue like bones, nerves, muscles, tendons, cartilage and blood vessels of the arms and legs.

Pelvic soft osteosarcoma MRI segmentation method based on edge-guided multi-scale fusion

The invention discloses a pelvic soft osteosarcoma MRI (Magnetic Resonance Imaging) segmentation method based on edge-guided multi-scale fusion. The method comprises the following steps: firstly, acquiring an MRI image of a patient with soft osteosarcoma of pelvis, and preprocessing the image; and then, constructing a pelvic soft osteosarcoma MRI segmentation network model, namely an EMU-Net segmentation network, based on edge-guided multi-scale fusion. And training the network by using the preprocessed training data, inputting a pelvic soft osteosarcoma MRI image to be segmented into the trained network, outputting a corresponding segmentation probability graph, and obtaining a final tumor segmentation mask by setting a threshold value. The method not only effectively overcomes the clinical segmentation bottleneck, but also realizes full-automatic and high-efficiency precise segmentation by means of an end-to-end deep learning architecture, and has remarkable advantages in the aspects of precision and robustness.
Owner:HANGZHOU DIANZI UNIV

Sarcoma fusion gene nanopore sequencing primer set and application thereof

The application relates to a sarcoma fusion gene nanopore sequencing primer set and application thereof, wherein the primer set comprises five pairs of specific primers (Primer 1-5) with fixed sequences, each primer follows the design principle of 18-25 bp in length, 40%-60% in GC content and strict matching of a target sequence at a 3' end, and the length of an amplification product is 300-800 bp, which is suitable for nanopore sequencing. Through qPCR verification, the primer set has single-peak melting curves, close-to-100% amplification efficiency, strong specificity and excellent amplification performance.
Owner:SHANGHAI SIXTH PEOPLES HOSPITAL

FBXO21 MEDIATED P85a UBIQUITYLATION AS A THERAPEUTIC TARGET IN CANCER

PCT designated stageWO2026072967A1Organic chemistryAntineoplastic agentsGastrointestinal cancerChronic myeloproliferative disorders
The present disclosure is concerned with compounds and compositions for use in the prevention and treatment of cancer associated with FBOX21 mediated p85a ubiquitination such as, for example, cancer (e.g., sarcoma, a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, a glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinoma, renal cancer, lung cancer, colon cancer, cervical cancer, and plasma cell neoplasm (myeloma)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Owner:UNIV OF UTAH RES FOUND +1

Sarcoma evaluation sections, methods of making and use thereof

The application discloses a kind of for carcinosarcoma evaluation section and its preparation method and application, belong to pathological technical field.The preparation method includes the following steps: reticular fiber staining: silver staining method is carried out to the reticular fiber in section tissue and is dyed;Immunohistochemical staining: AE1 / AE3 protein in section tissue is marked and dyed by immunohistochemical staining method.The section obtained by the preparation method can present two kinds of staining on a tissue section, improve the expression effect of cancer, sarcoma, carcinosarcoma, reduce the identification difficulty, and be beneficial to tumor accurate typing.
Owner:GUANGZHOU KINGMED DIAGNOSTICS GRP CO LTD +1

Culture medium, method and kit for constructing and / or culturing sarcoma organs

The invention relates to a culture medium for constructing and / or culturing a sarcoma-like organ, a method for constructing and / or culturing the sarcoma-like organ by using the culture medium, a sarcoma tissue dissociation digestive juice and a kit for constructing and / or culturing the sarcoma-like organ. The culture medium disclosed by the invention not only can construct and obtain high-quality sarcoma organs at a relatively high success rate, but also can support long-term stable culture of the sarcoma organs. The sarcoma tissue dissociation digestive juice not only can efficiently dissociate sarcoma tissues, but also can retain living tumor cells to the maximum extent, so that the construction success rate of sarcoma organs is further improved. Therefore, according to the sarcoma organ culture medium and the culture system thereof, high-quality sarcoma organs can be stably obtained, key technical support is provided for pathological mechanism research, drug sensitivity detection, personalized treatment scheme formulation and the like of sarcoma diseases, and the culture medium and the culture system have clear and important clinical transformation value and industrialization potential.
Owner:PEKING UNIVERSITY THIRD HOSPITAL (THE THIRD CLINICAL MEDICAL SCHOOL OF PEKING UNIVERSITY)

Medicinal folium artemisiae argyi composition for preventing and treating atherosclerosis combined skin suppurative bacterial infection

The invention discloses a medicinal moxa composition for preventing and treating atherosclerosis and suppurative bacterial infection co-disease. The medicinal moxa composition comprises coptis chinensis, radix rehmanniae, polygala tenuifolia, juncus effuses and moxa. The medicinal folium artemisiae argyi composition disclosed by the invention can be used for effectively preventing and treating atherosclerosis and skin suppurative bacterial infection co-diseases through a multi-target synergistic effect. The medicinal moxa composition has the core effects of clearing away heart-fire, inducing diuresis for treating stranguria and promoting blood circulation to remove meridian obstruction, and forms a complete treatment system which uses cold and warm as well as treats both symptoms and root causes by purging fire for removing toxin through coptis chinensis, clearing heat and cooling blood through radix rehmanniae, soothing nerves and promoting intelligence through polygala, inducing diuresis and conducting heat downward movement through juncus effuses and combining moxa floss for warming and dredging meridians, eliminating cold to stop pain, resisting bacteria and diminishing inflammation. By inhibiting inflammatory factors, regulating epithelial cell proliferation and reaction to oxidative stress, regulating fluid shear force, atherosclerosis and Kaposi sarcoma-related herpesvirus infection-related pathways and other mechanisms, the medicinal folium artemisiae argyi composition realizes synergistic prevention and treatment of atherosclerosis and skin infection, and provides a basis for co-disease treatment.
Owner:CHONGQING ACAD OF CHINESE MATERIA MEDICA

1,5-Naphthyridine derivatives as KRAS oncoprotein inhibitors

PendingJP2026503866AOrganic active ingredientsOrganic chemistryDiseaseRat sarcoma virus
The present invention is directed to inhibitors of Kirsten rat sarcoma virus (KRAS) oncoprotein, and more particularly to inhibitors of certain formula I: The present invention is directed to 1,5-naphthyridine derivatives of formula I, as well as compositions comprising the compounds of formula I and methods of using the compounds of formula I for the treatment or prevention of diseases, disorders, or medical conditions mediated by KRAS, particularly KRAS G12C or KRAS G12D oncoprotein.
Owner:BETA PHARMA INC

Application of epimedin A as unique active ingredient in preparation of medicine for preventing and / or improving sarcopenia

PendingCN121891388AOrganic active ingredientsMuscular disorderLiver and kidneyTruncal muscle weakness
The invention relates to application of traditional Chinese medicine herba epimedii, especially an aqueous extract of herba epimedii and epimedin A in prevention and / or improvement of sarcopenia. Compared with a blank control group and a negative control group, the body lengths of the herba epimedii aqueous extract with the concentration of 1 mg / mL, the total flavonoids with the concentration of 0.026 mg / mL, the epimedium A with the concentration of 50 [mu] M, the epimedium B with the concentration of 200 [mu] M, the epimedium C with the concentration of 100 [mu] M, the icariin with the concentration of 200 [mu] M and the icaritin with the concentration of 100 [mu] M are increased by 21.40%, 23.09%, 26.69%, 24.91%, 29.22%, 33.15% and 28.35% respectively. The icariin administration concentration is improved, and the growth promoting effect concentration dependence is obviously enhanced. The body length of the caenorhabditis elegans is increased by 24.19% and even exceeds that of a positive control group. Epimedin A of 50 mu M can effectively increase the body length of caenorhabditis elegans, and other Epimedin A needs higher concentration; 50 [mu] M has the best effect of protecting and relieving the muscular structure. The invention provides a thought for developing medicines for improving dyskinesia and muscle volume reduction, prolonging life, improving muscle fiber atrophy, treating muscle strength decline, tonifying liver and kidney and strengthening muscles and bones, and the medicine is high in safety.
Owner:GANSU UNIV OF CHINESE MEDICINE

Use of cinobufotalin in the preparation of a drug for treating osteoarthritic diseases

This invention belongs to the field of biomedical technology, specifically relating to the application of bufalin in the preparation of drugs for treating osteoarthritis. The structure of bufalin is shown in the following formula. Research results of this invention show that bufalin can significantly inhibit the inflammatory response and matrix degradation of chondrocytes, protecting the extracellular matrix of chondrocytes, thereby effectively delaying or reversing the pathological progression of osteoarthritis. This invention uses the SW1353 human chondrosarcoma cell line and SD rat primary chondrocytes as in vitro experimental models. The two cell models mutually validated each other, fully demonstrating the protective effect of bufalin on chondrocytes and its potential application value in the treatment of osteoarthritis.
Owner:XINXIANG MEDICAL UNIV

Combination therapy for treatment of cancer

PCT designated stageWO2026112410A1Organic active ingredientsAntineoplastic agentsOestrogen receptorOncology
Disclosed are novel compounds for use in treating a proliferative disorder such as a cancer. Further disclosed are compositions comprising the novel compounds. Methods of using the disclosed compounds and compositions are further described. The methods include administering one or more of the disclosed compounds for treatment of various proliferative disorders, including an HRAS-driven cancer, a KRAS-driven cancer, a NRAS-driven cancer, Ewing sarcoma, B-cell acute lymphoblastic leukemia, leukemia, lung cancer, non-small cell lung cancer (NSCLC), solid tumor, breast cancer, triple-negative breast cancer (TNBC), hormone-resistant triple negative breast cancer. Further described are combination therapies in which a novel compound is administered in combination with one or more of a MEK inhibitor, a KRAS G12C inhibitor, or a Selective Estrogen Receptor Degrader (SERD) to an individual in need thereof.
Owner:CHILDRENS HOSPITAL MEDICAL CENT CINCINNATI

TYR peptide compositions and methods for use

The present disclosure, relates, in general to analogs of proline-rich polypeptide 1 (PRP-1) designated tyrosine peptides (TYR peptide) that are useful to treat cancer, such as sarcomas, carcinomas and leukemias or liquid cancers.
Owner:UNIV OF MIAMI

Method for capturing, identifying and culturing sarcoma circulating tumor cells in vitro

The invention discloses a method for capturing, identifying and culturing circulating tumor cells of sarcoma in vitro. The method comprises a step of filtering a peripheral blood sample of a sarcoma patient by using a flexible microfiltration membrane, and cells obtained by filtration can be directly subjected to multiplication culture on the filtration membrane. Immunomagnetic beads of a monoclonal antibody combination group coupled with the anti-human leukocyte surface antigen CD45 can be used for negative enrichment and then multiplication culture is carried out in a cell culture bottle, and the captured or cultured cells can be subjected to subtype identification, characterization and counting by adopting an iFISH technology. It is found for the first time that the flexible microfiltration membrane can be used for capturing and culturing the sarcoma circulating tumor cells, and the flexible microfiltration membrane has no toxic effect on the sarcoma circulating tumor cells. The invention not only provides an effective means for real-time monitoring of relapse and metastasis processes of sarcoma patients and chemotherapy drug resistance monitoring, but also can perform drug sensitivity experimental verification on CTC after multiplication culture, and provides a powerful weapon for accurate diagnosis and treatment of sarcoma.
Owner:PEOPLES HOSPITAL PEKING UNIV

CDK2 inhibitor for the treatment of KRAS mutant cancer

PCT designated stageWO2026064479A1Amine active ingredientsHeterocyclic compound active ingredientsAcquired resistanceCyclin-dependent kinase 2
Combinations, compositions and uses of a cyclin dependent kinase 2 (CDK2) inhibitor INX-315, or a pharmaceutically acceptable salt thereof described herein, in combination with a CDK4 / 6 inhibitor for the treatment of disorders characterized by mutation of Kirsten rat sarcoma (KRAS), including but not limited to the treatment of tumors and cancers. In addition, the invention includes a method to delay acquired resistance to a RAS inhibitors in a KRAS mutant cancer, comprising administering the CDK2 inhibitor INX-315 optionally in combination or alternation with a KRAS inhibitor.
Owner:INCYCLIX BIO LLC

Application of HDAC7 as target spot in diagnosis and treatment of rhabdomyosarcoma

The invention relates to the technical field of biological medicines, in particular to application of HDAC7 as a target spot in diagnosis and treatment of rhabdomyosarcoma. The invention reveals for the first time that circular RNA (F-circP3F) sourced from an oncogenic fusion gene PAX3-FOXO1 is directly combined with and inhibits histone deacetylase HDAC7 to play a role through a novel mechanism, and HDAC7 can be used for early diagnosis, prognosis evaluation and curative effect monitoring of rhabdomyosarcoma as a core link of the regulation mechanism. And the method is a treatment intervention target with great potential.
Owner:SHIHEZI UNIVERSITY

Plasmid standard substance for quantitatively detecting Kaposi sarcoma-related herpes virus and construction method of plasmid standard substance

The invention relates to the technical field of gene detection, and discloses a plasmid standard substance for quantitatively detecting Kaposi sarcoma-related herpes virus and a construction method thereof. A primer capable of amplifying a KSHV ORF26 target fragment containing BamH I / Xba I double restriction enzyme cutting sites is designed, and the target fragment is connected to a carrier pBluescript SK (+), so that a plasmid standard substance capable of being used for quantitatively detecting the KSHV is obtained. The plasmid standard substance can be used for rapidly and quantitatively detecting the KSHV, the detection method is convenient and rapid, the operability is high, the sensitivity is high, KSHV genes are rapidly recognized and the virus load is obtained under the conditions that the sample virus load is low and the sample is improperly stored, and a foundation is laid for early discovery and prevention of diseases. Important data can be provided for epidemiological virus traceability, pathogenicity conditions and clinical treatment.
Owner:FUDAN UNIVERSITY

Method for classification of cancer

The present disclosure pertains to an in vitro method for the diagnostic classification of cancer based on the biological state of specific genomic sites. The disclosure provides a method that allows for a classification of a tumour sample obtained from a patient by analysing a multitude, preferably genome wide, collection of gene sites, combining the biological state of the analysed gene sites into a biological state pattern and comparing with pre-determined biological state patterns pertaining to different cancer types or tumour species. The disclosure is in particular useful for classifying cancer e.g. of the central nervous system, such as brain tumour samples and tumours of the spinal cord, since these are characterized by a large variety of distinct tumour species which have different prognostic values and require a developed treatment regime for each species in the clinical context. However, other cancers could similarly profit from the disclosure, for example sarcomas.
Owner:DEUTES KREBSFORSCHUNGSZENT STIFTUNG DES OFFENTLICHEN RECHTS +1

Application of detection reagent in malignant differentiation detection of Carbosi sarcoma

The invention discloses application of a detection reagent in malignant differentiation detection of Carbosi sarcoma, and belongs to the technical field of biological medicine. Aiming at the problem of insufficient specificity of a malignant differentiation marker of Carbosi sarcoma in the prior art, the invention provides application of a detection reagent in detection of the malignant differentiation of Carbosi sarcoma, and the detection reagent can simultaneously detect two biomarkers, namely CXCL12 and VWF, and is used for identifying endothelial cell malignant differentiation subgroups in tissue focuses of Carbosi sarcoma. By detecting the expression of CXCL12 and VWF in a tested sample, the endothelial cell malignant differentiation subgroup can be stably identified, and meanwhile, the expression level of CXCL12 can be used as an indicator of disease progression: the higher the expression level of CXCL12 is, the higher the lesion progression degree is, the higher the risk is, and the expression level is also positively correlated with the counting of peripheral blood lymphocytes. According to the invention, high-specificity recognition and standardized reading of the endothelial cell malignant differentiation subgroups are realized.
Owner:PEOPLES HOSPITAL OF XINJIANG UYGUR AUTONOMOUS REGION

Pharmacological re-activation of mutant pvhl

PCT designated stageWO2026107377A1Organic chemistryAntineoplastic agentsChronic myeloproliferative disordersProstate cancer
The present disclosure relates to compounds, pharmaceutical compositions, and methods of using the compounds and compositions to restore activity of von Hippel Lindau tumor suppressor protein (pVHL). Such compounds and compositions can be useful in, for example, the treatment of cancer (e.g.. a sarcoma, a carcinoma, a head-and-neck cancer, hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, a glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinoma, small cell lung carcinoma, renal cancer, lung cancer, colon cancer, cervical cancer, and plasma cell neoplasm (myeloma)) and von Hippel-Lindau disease (VHLD). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Owner:KARANICOLAS JOHN +2

Microcrystalline polymorphs of LMP400 and uses thereof

PCT designated stageWO2026029971A1Organic active ingredientsOrganic chemistryGastrointestinal cancerChronic myeloproliferative disorders
Disclosed herein are crystalline polymorphs of indotecan (LMP400) that can be used in the treatment of cancers associated with dysregulation of Topl and / or MYC activity, such as, for example, a sarcoma, (e.g., Ewing's sarcoma), a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, non-small cell lung carcinoma, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, a melanoma, a. glioma, leukemia, a lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, and plasma cell neoplasm (myeloma). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Owner:GIBSON ONCOLOGY LLC

A cyclic polypeptide molecular probe targeting neuropilin-1, preparation method and application thereof

PendingCN122277655ARealize imaging diagnosisHigh biosecurityAutoimmune conditionAutoimmune disease
This invention relates to a cyclic polypeptide molecular probe targeting neurocilia protein-1 (NRP-1), its preparation method, and its applications. The cyclic polypeptide molecular probe comprises the structure shown in Formula I or Formula II, where R1 is the structure shown in Formula III or Formula IV; and R2 is a radiolabeled nuclide or a radiolabeled nuclide including a bifunctional chelating group. The technical solution of this invention exhibits excellent targeting specificity and high sensitivity for NRP-1 protein, enabling visualization of NRP-1-highly expressing tumors (such as fibrosarcoma, lung cancer, pancreatic cancer, or breast cancer) and NRP-1-positive lesions (such as metabolic diseases, sclerotic lesions, or autoimmune diseases) on positron emission tomography (PET). It shows great promise in the early diagnosis of NRP-1-highly expressing malignant tumors and in guiding clinical NRP-1 monoclonal antibody treatment regimens.
Owner:FUDAN UNIV SHANGHAI CANCER CENT

Microcrystalline polymorphs of LMP744 and uses thereof

PCT designated stageWO2026029972A1Organic chemistryAntineoplastic agentsGastrointestinal cancerChronic myeloproliferative disorders
Disclosed herein are crystalline polymorphs of LMP744 that can be used in the treatment of cancers associated with dysregulation of Top1 and / or MYC activity, such as, for example, a sarcoma, (e.g., Ewing's sarcoma), a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, non-small cell lung carcinoma, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, a melanoma, a glioma, leukemia, a lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, and plasma cell neoplasm (myeloma). This abstract is intended as a scanning tool for purposes of searching m the particular art and is not intended to be limiting of the present invention.
Owner:GIBSON ONCOLOGY LLC

A novel micropeptide MP36 and application thereof

PendingCN122138975AMicrobiological testing/measurementFermentationOncologyPeptide expression
A novel micropeptide, MP36, and its applications are provided. This MP36 micropeptide can be used to prepare reagents or drugs for the detection, prevention, or treatment of tumors, including one or more of lung cancer, breast cancer, colon cancer, glioma, bladder cancer, gastric cancer, head and neck cancer, and sarcoma. In tumors, the MP36 micropeptide can inhibit tumor cell growth and / or metastasis by specifically inhibiting MP36 expression via small interfering RNA; or by overexpressing MP36 to inhibit tumor cell growth and / or metastasis; or by conjugating a membrane-penetrating peptide to inhibit tumor growth and / or metastasis. It has significant value for new drug development and tumor detection.
Owner:NANJING ANJI BIOLOGICAL TECH CO LTD

Dcaf1 ligands and uses thereof

PendingCN122341585ATransplant rejectionPyrrole
This disclosure provides small molecule pyrrole-3-carboxamide compounds, compositions thereof, and methods of using them to modulate DCAF1 and treat a variety of diseases, disorders or conditions associated with DCAF1, such as neurological disorders like Alzheimer's disease, Parkinson's disease or Huntington's disease, transplant rejection, AIDS-related Kaposi's sarcoma, and particularly cancer.
Owner:KEMERA THERAPEUTICS

Goose head sarcoma intelligent rating method and system

The invention discloses a goose head sarcoma intelligent rating method and system, and the method comprises the steps: collecting a goose pose image of a target goose individual, inputting the goose pose image into a pre-trained goose pose detection model, outputting a pose category and a corresponding confidence coefficient, and screening a specific pose image; inputting the specific pose image into a pre-constructed goose head sarcoma detection and segmentation model, and outputting a head region and a sarcoma region; calculating a quantitative index value of goose head sarcoma features according to the head area and the sarcoma area; and inputting the quantitative index value into a pre-constructed intelligent goose head sarcoma rating model, and outputting the score and grade of the head sarcoma of the target goose individual. According to the embodiment of the invention, automatic identification, quantitative analysis and comprehensive rating of goose head sarcoma features can be realized, and efficient and standardized evaluation of sarcoma appearance features is further realized.
Owner:SHANGHAI ACAD OF AGRI SCI +1

An engineered glutamine depletion bacteria and application of a pharmaceutical composition thereof

PendingCN122256214AOrganic active ingredientsBacteriaTumour metabolismTumor targeting
This invention discloses the application of a glutamine-depleting engineered bacterium and its pharmaceutical composition. The engineered bacteria use attenuated bacteria with tumor-targeting capabilities as vector strains. The genome or plasmid of the vector strain integrates a therapeutic gene encoding glutaminase. This method achieves deep and continuous depletion of glutamine in the tumor, avoiding drug resistance caused by tumor metabolic compensation. The inhibition rate against c-Myc-overexpressing soft tissue sarcomas is significantly higher than that of small molecule inhibitors. Enzyme production is only carried out locally in the tumor, with no effect on normal tissues and no systemic toxicity. The engineered bacteria can penetrate the dense tumor matrix and colonize the tumor, solving the problem of poor tissue penetration of small molecule inhibitors. The engineered bacteria continuously multiply and produce enzymes in the tumor, achieving continuous release of glutaminase. The half-life is significantly longer than that of recombinant enzymes, eliminating the need for frequent dosing. The glutaminase optimized by protein engineering has significantly reduced immunogenicity.
Owner:GUANGZHOU SINOGEN PHARMA CO LTD +1

Boron-based enolase ligands and methods of use for treatment of cancer

PendingUS20260183322A1MelanomaPharmaceutical medicine
Pharmaceutical compositions and methods for using boron-based ligands of enolases to treat cancer are disclosed. One such pharmaceutical composition includes a therapeutically effective amount of a ligand of enolase (1) having a general formula III or a pharmaceutically acceptable derivative thereof. The cancer can be a carcinoma, sarcoma, lymphoma, leukemia, or melanoma. The cancer can be prostate cancer.
Owner:LOMA LINDA UNIVERSITY

Modulators of proteolysis and associated methods of use

ActiveUS12552783B2Tetrapeptide ingredientsEnzymesDiseaseCereblon
The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation / inhibition of target protein. Diseases or disorders that result from aggregation, accumulation, and / or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Owner:ARVINAS OPERATIONS INC +1