University of North Carolina at Chapel Hill

St. Jude Children's Research Hospital

North Carolina Central University

Albert Einstein College of Medicine

Matthew Robert Redinbo

Philip Michael Potter

Monika Weirdl

Li-An Yeh

John Scott

Alfred L Williams

Jian Jin

Stephen Frye

Sridhar Mani

Lindsey James

Ranathunga Arachchillage Yamuna Ariyarathna

Bret David Wallace

Sam Pellock

Kimberly Terry Lane

Compounds and compositions are provided that comprise selective b-glucuronidase inhibitors. The compounds and compositions can ameliorate the side effects of chemotherapeutic agents and can improve the efficacy of such agents, including irinotecan and non-steroidal anti-inflammatory drugs.

Inhibitors of microbial beta-glucuronidase enzymes and uses thereof

This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11.

Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase

Polynucleotides encoding a secreted mutant human carboxylesterase enzyme and polypeptides encoded by the polynucleotides which are capable of metabolizing a prodrug and inactive metabolites thereof to active drug are provided. Compositions and methods for sensitizing cells to a prodrug agent, inhibiting cell growth, treating drug addiction, and facilitating the metabolism of an organophosphate with this enzyme are also provided. In addition, a screening assay for identification of drugs activated by this enzyme is described.

Composition and method for inhibiting tumor cell growth

Compounds, compositions and methods are provided that comprise selective &#x3b2;-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial &#x3b2;-glucuronidase and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial &#x3b2;-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplasatic agents or glucuronidase-substrate agents or compounds.

Selective &#x3b2;-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents

Polynucleotides encoding a mutant human carboxylesterase enzyme and polypeptides encoded by the polynucleotides which are capable of metabolizing a prodrug and inactive metabolites thereof to active drug are provided. Compositions and methods for sensitizing cells to a prodrug agent, inhibiting cell growth, treating drug addiction, and facilitating the metabolism of an organophosphate with this enzyme are also provided. In addition, a screening assay for identification of drugs activated by this enzyme is described.

Method for sensitizing tumor cells to chemotherapeutic prodrug CPT-11

Compounds, compositions and methods are provided that comprise selective &#x3b2;-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial &#x3b2;-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial &#x3b2;-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.

Selective beta-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents

Compositions and methods for inducing or inhibiting activities of selected human cells

Growing community of inventors

Chapel Hill, NC, United States of America

Matthew Robert Redinbo