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128 results about "Anti-Apoptotic Proteins" patented technology
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On the other hand, all pro-apoptotic proteins contain a BH3 domain necessary for dimerization with other proteins of Bcl-2 family and crucial for their killing activity, some of them also contain BH1 and BH2 domains (Bax and Bak). The BH3 domain is also present in some anti-apoptotic protein, such as Bcl-2 or Bcl-x(L).
Salts and crystalline forms of an apoptosis-inducing agent
Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Owner:ABBVIE INC
Methods and compositions for modulating bcl-2 family polypeptides
The present invention is based, at least in part, on the identification of a novel active site on BCL-2 family polypeptide such as BAX, which when bound by a compound, modifies the activity of the BCL-2 family polypeptide.
Owner:DANA FARBER CANCER INST INC +1
2 Methoxy antimycin a derivatives and methods of use
InactiveUS20050239873A1Inhibitory activityInduce apoptosisBiocideOrganic active ingredientsBcl-2 GenesAntimycin A
Disclosed are 2-methoxy antimycin derivatives or analogs that modulate apoptosis by binding to the hydrophobic groove of a Bcl-2 family member protein (e.g., Bcl-2 or BCl-xL). The 2-methoxy antimycin derivatives or analogs are used in disclosed methods for treating apoptosis-associated diseases such as, for example, neoplastic disease (e.g., cancer) or other proliferative diseases associated with the over-expression of a Bcl-2 family member protein.
Owner:FRED HUTCHINSON CANCER RES CENT
Formulation for oral administration of apoptosis promoter
InactiveUS20100297194A1Improve oral bioavailabilityConvenient route of administrationOrganic active ingredientsBiocideDiseaseAntioxidant
An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis-HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and / or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Owner:ABBOTT LAB INC +1
Small molecule antagonists of BCL-2 family proteins
InactiveUS20040214902A1Guaranteed long-term securityAntibacterial agentsBiocideChemical synthesisDisease
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer / chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer / chemotherapeutic agents) and / or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
Owner:RGT UNIV OF MICHIGAN +1
Methods and compositions for specific modulation of mcl-1
ActiveUS20120172285A1Inhibitory activityIncreased apoptosisAntibacterial agentsOrganic active ingredientsDisease causeHelix
A series of stapled BCL-2 family peptide helices were identified as able to target the survival protein MCL-I with high affinity and a subset with unprecedented selectivity. Agents and methods for selective pharmacologic neutralization of MCL-I are provided for drug discovery and therapeutic uses, including use in overcoming the apoptotic resistance of cancer and other diseases associated with impaired cell death.
Owner:DANA FARBER CANCER INST INC
Small molecule inhibitors of anti-apoptotic BCL-2 family members and the uses thereof
ActiveUS20060084647A1Great clinical benefitGreat tumor responseUrea derivatives preparationBiocideSensitized cellBcl-2 Genes
The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.
Owner:RGT UNIV OF MICHIGAN
Molecular vaccines employing nucleic acid encoding anti-apoptotic proteins
InactiveUS20070026076A1Increase the number ofEasy to demonstratePowder deliveryVirusesDendritic cellVaccine Potency
T cell immune responses are enhanced by presentation of antigen to CD8+ T cells using a chimeric nucleic acid immunogen or vaccine that links DNA encoding an antigen with DNA encoding a polypeptide that targets or translocates the antigenic polypeptide to which it is fused (immunogenicity-potentiating polypeptides or “IPP”). By inhibiting apoptosis in the vicinity of a T cell responses to such a nucleic acid immunogen, even more potent immune responses are attained. The present strategy prolongs the survival of DNA-transduced cells, including dendritic cells (DCs), thereby enhancing the priming of antigen-specific T cells and increase potency. Co-delivery of DNA encoding an inhibitor of apoptosis, including (a) BCL-xL, (b) BCL-2, (c) XIAP, (d) dominant negative caspase-9, or (e) dominant negative caspase-8, or (f) serine protease inhibitor 6 (SPI-6) which inhibits granzyme B, with DNA encoding an antigen, prolongs the survival of transduced DCs and results in significant enhancement of antigenspecific T cell immune responses that provide potent antitumor effects. Thus, co-administration of a DNA vaccine encoding antigen linked to an IPP along with one or more DNA constructs encoding an anti-apoptotic protein provides a novel way to enhance vaccine potency.
Owner:THE JOHN HOPKINS UNIV SCHOOL OF MEDICINE
Tricyclic indole mcl-1 inhibitors and uses thereof
The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
Owner:VANDERBILT UNIV
Compositions and methods for modulating apoptosis in cells over-expressing Bcl-2 family member proteins
The present invention provides agents and compositions for modulating the apoptotic state of a cell. The agents comprise derivatives of antimycins which bind to an anti-apoptotic Bcl-2 family member protein. Further, the agents preferentially induce apoptosis in cells that over-express anti-apoptotic Bcl-2 family member proteins and typically exhibit reduced binding affinity for cytochrome B. Pharmaceutical uses of the agents and compositions include treating apoptosis-associated disease, such as neoplasia and drug resistance, are also disclosed.
Owner:FRED HUTCHINSON CANCER CENT
COMPOSITIONS AND METHODS FOR MODULATING APOPTOSIS IN CELLS OVER-EXPRESSING Bcl-2 FAMILY MEMBER PROTEINS
The present invention provides agents and compositions for modulating the apoptotic state of a cell. The agents comprise derivatives of antimycins which bind to an anti-apoptotic Bcl-2 family member protein. Further, the agents preferentially induce apoptosis in cells that over-express anti-apoptotic Bcl-2 family member proteins and typically exhibit reduced binding affinity for cytochrome B. Pharmaceutical uses of the agents and compositions include treating apoptosis-associated disease, such as neoplasia and drug resistance, are also disclosed.
Owner:FRED HUTCHISON CANCER RES CENT
Small molecule antagonists of Bcl-2 family proteins
InactiveUS7432304B2Inhibition of activationLoss of p53Antibacterial agentsBiocideChemical synthesisDisease
Owner:RGT UNIV OF MICHIGAN +1
Naphthalene-based inhibitors of Anti-apoptotic proteins
Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided:wherein each R is independently selected from the group consisting of H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, and NHSO2X, wherein X is selected from the group consisting of an alkyl, a substituted alkyl, an aryl, a substituted aryl, an alkylaryl, and a heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.
Owner:BURNHAM INST FOR MEDICAL RES
Therapy with a chimeric molecule and a pro-apoptotic agent
InactiveUS20120276190A1Good curative effectIncrease killOrganic active ingredientsAntibody ingredientsADAMTS ProteinsCell biology
The present invention provides compositions comprising a chimeric molecule comprising a cytotoxin that inhibits protein synthesis and an agent that inactivates an anti-apoptotic BCL-2 family member protein and methods of inhibiting the growth of or promoting the apoptosis of an aberrantly proliferating cell population by co-administering the chimeric molecule and the agent that inactivates an anti-apoptotic BCL-2 family member protein.
Owner:UNITED STATES OF AMERICA
Drug-loading nano-micelles, and preparation method and application thereof
ActiveCN102920649AEasy to prepareEasy to operate and promoteOrganic active ingredientsGenetic material ingredientsDocetaxelPolyethylene glycol
The invention relates to drug-loading nano-micelles, and a preparation method and an application thereof. According to the to drug-loading nano-micelles, a polyethylene glycol derivative-polylysine-polyleucine amphiphilic triblock copolymer is adopted as a carrier, and self-assembly is carried out in a water solution, such that nano-micelles with a three-layer structure transferring gene and medicine are formed. With the hydrophobic effect between polyleucine, the copolymer forms a core of the micelles in water, such that a hydrophobic medicine docetaxel is entrapped. With polylysine, the nano-micelles are positively charged, such that negatively charged anti-apoptotic protein small interfering RNA can be bonded. Polyethylene glycol is used for protecting the stability of the nano-micelles loading the medicines and gene, and a cycle time of the nano-micelles in vivo is prolonged. The nano-micelles are used for loading both an anti-apoptotic protein small interfering RNA gene medicine and a docetaxel medicine, such that the gene treatment medicine and the chemotherapeutic medicine cooperates in treating cancer, and a synergetic effect of the two medicines can be developed. Therefore, a direction is provided for better treatment of breast cancer.
Owner:SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
Salt of abt-263 and solid-state forms thereof
InactiveUS20100305125A1Convenient route of administrationEasy to doOrganic active ingredientsOrganic chemistryDiseaseMedicine
Owner:ABBVIE INC
Pulsatile dosing of gossypol for treatment of disease
InactiveUS20090010878A1Reduction in adverse eventsInhibitory activityAntibacterial agentsBiocideDiseaseInducer
This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.
Owner:ASCENTA THERAPEUTICS
Abt-263 crystalline forms
ActiveUS20110071151A1Purification less economicalPurification difficult and expensiveOrganic active ingredientsOrganic chemistry methodsDiseaseProtein C
Owner:ABBVIE INC
Small molecule inhibitors targeted at Bcl-2
InactiveUS7354928B2Effective treatmentReduce overexpressionHeavy metal active ingredientsBiocideDiseaseCancer cell
Owner:GEORGETOWN UNIV +1
Assay system to identify therapeutic agents
Owner:EUTROPICS PHARMA
4-substituted naphthalimide compound and use thereof
The invention provides a 4-substituted naphthalimide compound and a use thereof. The compound has a structure shown in the general formula I. The compound can competitively bind and antagonize with Bcl-2 and Mcl-1 proteins in vitro and in cells so that apoptosis is induced and thus the compound is a high activity apoptosis inducing agent and an antitumor compound. The derivative based on the compound can be used as a bifunctional molecule for external and intracellular recognition, separation, enrichment and fluorescence detection of Bcl-2 family proteins or can be used as a PROTAC bifunctional complex for intracellular selective degradation of Bcl-2 and Mcl-1 proteins so that the level of the Bcl-2 family proteins in living cells can be adjusted and controlled.
Owner:DALIAN UNIV OF TECH
Methods and compositions useful for treating diseases involving bcl-2 family proteins with quinoline derivatives
Owner:EUTROPICS PHARMA
Stabilized lipid formulation of apoptosis promoter
InactiveUS20100278905A1Convenient route of administrationEasy to doOrganic active ingredientsDispersion deliveryLipid formationDisease
An orally deliverable pharmaceutical composition comprises a Bcl-2 family protein inhibitory compound, e.g., ABT-263, a heavier-chalcogen antioxidant and a substantially non-aqueous lipid carrier, wherein said compound and said antioxidant are in solution in the carrier. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Owner:ABBVIE INC
Therapeutic combination comprising a cdc7 inhibitor and an Anti-neoplastic agent
ActiveUS20120276093A1Less side effectsStrong synergyHeavy metal active ingredientsBiocideCell Surface ProteinsAntimitotic Agent
The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
Owner:NERVIANO MEDICAL SERVICES SRL
Thio/oxo-naphthalimide compound and application thereof
The invention provides a thio / oxo-naphthalimide compound and application thereof. The compound has a structure shown as a general formula I. The compounds are capable of realizing competitive binding and antagonism of Bcl-2 and Mcl-1 proteins in vitro and in cells so as to induce cell apoptosis, and refer to a type of apoptosis inducers and antitumor compounds with extremely high activities. In addition, the derivative designed based on the compound can serve as a bifunctional molecule and is capable of recognizing, separating, enriching and realizing fluorescence detection of Bcl-2 family proteins; or the derivative can serve as a PROTAC bifunctional complex for selectively degrading the Bcl-2 and Mcl-1 proteins in the cells, so that the level of the Bcl-2 family proteins in living cells is regulated. The structural formula is as shown in the specification.
Owner:DALIAN UNIV OF TECH
Methods and compositions useful for treating diseases involving bcl-2 family proteins with isoquinoline and quinoline derivatives
InactiveUS20160038503A1BiocideBoron compound active ingredientsAbnormal tissue growthAutoimmune condition
The present invention relates to a compositions for and methods for cancer treatment, for example, hematopoietic cancers (e.g. B-cell Lymphoma). In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more of the disclosed compounds and, for example, 26S proteasome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with the disclosed compounds. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
Owner:EUTROPICS PHARMA
Feeder layer and serum independent embryonic stem cells
InactiveUS7641897B2BiocideGenetic material ingredientsPluripotential stem cellInduced pluripotent stem cell
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
Pulsatile Dosing of Gossypol for Treatment of Disease
InactiveUS20090175869A1Reduction in adverse eventsInhibitory activityBiocideHeavy metal active ingredientsDiseaseInducer
This invention relates to pulsatile dose administration of gossypol, a gossypol-related compound or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol or gossypol-related compound, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.
Owner:ASCENTA THERAPEUTICS
Pulsatile Dosing of Gossypol for Treatment of Disease
InactiveUS20100189683A1Reduce in quantityReduction in adverse eventsBiocideHeavy metal active ingredientsDiseaseInducer
This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.
Owner:ASCENTA THERAPEUTICS
Thiazole couplet pyrazolone series compound and application of the same as Bcl-2 family protein antagonist
InactiveCN101343268ANovel structureHigh cytotoxic activityOrganic active ingredientsOrganic chemistryThiazoleMda mb 231
The invention discloses a thiazole bipyrazolone compound as well as applications thereof in preparing a small molecular inhibitor of Bcl-2 family proteins and antitumor drugs, the thiazole bipyrazolone compound has the above structural formula, and the thiazole bipyrazolone compound has the activity for inhibiting the combination of Bcl-xL and natural substrate polypeptide (Bid BH3 polypeptide) in the micromole range, and can serve as the small molecular inhibitor of the Bcl-2 family proteins for inhibiting the anti-apoptosis activity thereof; and the compound shows a certain inhibitory activity to human breast cancer MDA-MB-231 cells and MCF-7 cells, and is expected to be developed into the antitumor drugs of targeted Bcl-2 family proteins.
Owner:SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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