Kai Pharmaceuticals, Inc.

Exelixis, Inc.

Felix D Karim

Qun Yin

Derek Maclean

Amos Baruch

Kanad Das

Gregory Bell

Geoffrey Duyk

Gregory D Plowman

Timothy S Heuer

Lynn Margaret Bjerke

Sarah Walter

Candace Swimmer

Casey Kopczynski

Torsten Bernhard Trowe

Gordon Mark Stott

Andreas Michael Vogel

Joerg Heinrich Odenthal

Jochen Konrad Scheel

Torsten Tilmann Will

Yinsheng Jin

Jenny Kopczynski

Hinrich Alexander Habeck

Thomas I Koblizek

Stefan Schulte-Merker

Ulrike Eisenmann

Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X-X-X-X-X-X-X, wherein the Xsubunit comprises a thiol-containing moiety and the distribution of charge on the X-Xsubunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

Therapeutic agents for reducing parathyroid hormone levels

Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X&#x2014;X&#x2014;X&#x2014;X&#x2014;X&#x2014;X&#x2014;X, wherein the Xsubunit comprises a thiol-containing moiety and the distribution of charge on the X-Xsubunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

The present invention provides methods and kits for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders. In particular, methods for lowering serum PTH and serum calcium using polycationic calcium modulator peptides are provided. The calcium modulator peptides can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

Polycationic calcium modulator peptides for the treatment of hyperparathyroidism and hypercalcemic disorders

Methods for modulating serum phosphorus levels are described, wherein calcimimetic agents are administered to a subject in need thereof. In one embodiment, the compound is cinacalcet, and in other embodiments the compound is comprised of a contiguous sequence of subunits, X&#x2014;X&#x2014;X&#x2014;X&#x2014;X&#x2014;X&#x2014;X, wherein the Xsubunit comprises a thiol-containing moiety and the distribution of charge on the X-Xsubunits. The compound, when administered at selected times to a patient undergoing dialysis, lowers serum phosphorus levels, relative to pre-dosing levels, and achieves a sustained reduced level for a period of time after administration.

Therapeutic agents for regulating serum phosphorus

Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X&#x2014;X&#x2014;X&#x2014;X&#x2014;X&#x2014;X&#x2014;X, wherein the Xsubunit comprises a thiol-containing moiety and the distribution of charge on the X&#x2014;Xsubunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

Human MYLK genes are identified as modulators of branching morphogenesis, and thus are therapeutic targets for disorders associated with defective branching morphogenesis function. Methods for identifying modulators of branching morphogenesis, comprising screening for agents that modulate the activity of MYLK are provided.

Mylks as modifiers of branching morphogenesis and methods of use

Methods, transformation constructs, and transgenic animals for identifying anti-tumor agents and anti-tumor drug targets are described. The transformation constructs are used to generate transgenic animals that have altered expression of an oncogene or tumor suppressor gene in a target tissue that is dispensable for viability and reproduction. In some embodiments, the altered expression results in abnormal proliferation of the target tissue and normal proliferation in all other tissues. Anti-tumor drug targets can be identified by generating progeny of the transgenic animals that have mutations in various genes. Gene mutations that result in a specific reduction or killing of the target tissue are identified as possible anti-tumor drug targets and are further evaluated. Anti-tumor agents are identified that mimic the effect of the gene mutations that result in specific reduction of the target tissue. Alternatively, anti-tumor agents can be identified by administering various compounds directly to the transgenic animals, or their progeny, and selecting as putative therapeutic agents, compounds that result in target-tissue specific antiproliferation.

Methods for identifying anti-cancer drug targets

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Menlo Park, CA, United States of America

Felix D Karim