National Institutes of Health, a Component of the US Dept. of Health & Human Services

Arizona Board of Regents on Behalf of the University of Arizona

Curtis J Henrich

James Brislin McMahon

Heidi R Bokesch

Kirk R Gustafson

Michael C Dean

Susan Elaine Bates

Robert W Robey

Suneet Shukla

Suresh V Ambudkar

Richard W Fuller

Thomas Joseph Sayers

Alan David Brooks

Laura K Cartner

Kentaro Takada

Karen L Erickson

Leslie Gunatilaka

Nancy H Colburn

Kithsiri Wijeratne

Poonam Tewary

Nancy Lynn Booth

Moon-II Kang

Ya-Ming Xu

Matthew R Young

Disclosed is a method of enhancing the response of cancer cells in a mammal to treatment with an apoptosis inducing ligand, which method comprises contacting the cancer cells with an apoptosis inducing ligand in conjunction with an effective amount of a compound of the formula: (I), wherein R-Rare as described herein. Also disclosed is a method of inducing apoptosis in cancer cells in a mammal, comprising contacting the cancer cells with the compound described herein and also contacting the cancer cells with an apoptosis inducing ligand, whereby apoptosis is induced in the cancer cells. 

Method of sensitizing cancer cells to the cytotoxic effects of apoptosis inducing ligands in cancer treatment

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2 or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering peliomycin and other compounds described herein.

Method of inhibiting ABCG2 and related treatments

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R, R, R, X, X, X, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.

Method of inhibiting ABCG2 and other treatment methods

Disclosed is a method of enhancing the response of cancer cells in a mammal to treatment with a death receptor ligand, which method comprises contacting the cancer cells with a death receptor ligand in conjunction with an effective amount of a compound described herein, for example, a cucurbitacin (I) or a withanolide (II). Also disclosed is a method of inducing apoptosis in cancer cells in a mammal, comprising contacting the cancer cells with a compound described herein, for example, a cucurbitacin (I) or a withanolide (II) and also contacting the cancer cells with a death receptor ligand, whereby apoptosis is induced in the cancer cells. 

Method of sensitizing cancer cells to the cytotoxic effects of death receptor ligands in cancer treatment

An embodiment of the invention provides a pharmaceutical composition comprising a compound of formula (I) a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Another embodiment of the invention provides a method of treating or preventing a condition associated with increased expression and/or activity of an NF&#x3ba;B pathway using same compounds. A further embodiment of the invention provides a method of diagnosing a condition in an individual using same compounds. 

Nuclear factor kappa B pathway inhibitor composition and use of same

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): Formula (I), wherein R, R, R, X, X, X, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof. 

Botryllamides and method of inhibiting PGP in a mammal afflicted with cancer

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Rockville, MD, United States of America

Curtis J Henrich