162 results about "Apoptosis inducer" patented technology

The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

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.

Pharmaceutical compositions are made from extracts obtained from ethnobotanical plants for inducing apoptosis in selected cells. Therapeutically effective amounts of the composition are administered to a mammal. Assays are used to determine the efficacy of such extracts in inducing apoptosis.

The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Disclosed are N-aryl-thienopyrimidin-4-amines and analogs thereof, represented by the Formulae I-II:

wherein Ar and R₁-R₄ are defined herein. The present invention relates to the discovery that compounds having Formulae I-II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

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.

According to the present invention, an apoptosis-inducing agent for prostate cancer comprising REIC/Dkk-3 DNA or an REIC/Dkk-3 protein, and a therapeutic agent for prostate cancer and an agent for inhibiting prostate cancer metastasis that comprise such apoptosis-inducing agent are provided.

An apoptosis-inducing agent for prostate cancer, comprising, as an active ingredient, an REIC/Dkk-3 protein (a) or (b) or REIC/Dkk-3 DNA (c) or (d):

• • (a) a protein consisting of the amino acid sequence represented by SEQ ID NO: 2;
  • (b) a protein consisting of an amino acid sequence derived from the amino acid sequence represented by SEQ ID NO: 2 by substitution or deletion of 1 or more amino acids;
  • (c) DNA consisting of the nucleotide sequence represented by SEQ ID NO: 1; or
  • (d) DNA that hybridizes under stringent conditions to DNA consisting of a nucleotide sequence complementary to the nucleotide sequence represented by SEQ ID NO: 1 and encodes a protein having apoptosis activity; and
  • a therapeutic agent for prostate cancer comprising such apoptosis-inducing agent are provided

The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I:

wherein A, B, X, Y, Z and R₅ are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

The present invention is directed to substituted 4H-chromenes, 2H-chromenes, chromans and analogs thereof, represented by the general Formula (I) wherein R₅, A, B, X, Y, Z and dotted lines are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

The invention relates to a preparation method and a use of two dimer citrinin compounds. The dimer citrinin compounds with novel structures are produced by adopting Penicillium Citrinum HGY1-5 in samples collected from a crater. Tests prove that the compounds can be used as a cell proliferation inhibitor, an apoptosis inducer or an anti-tumor agent.

The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.