Plexxikon Inc.

University of California

Heike I Krupka

Prabha N Ibrahim

Chao Zhang

Dean R Artis

Clarence R Hurt

Jack Lin

Weiru Wang

Michael V Milburn

James Arnold

Brent W Segelke

Bernhard Rupp

Jiazhong Zhang

Brian L West

Marika Nespi

Ryan Bremer

Shumeye Mamo

Rebecca Zuckerman

Gaston G Habets

Abhinav Kumar

Yong-Liang Zhu

Yong Zhu

Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.

PPAR active compounds

Compounds active on Ret are described, as well as methods of using such compounds. Also described are crystal structures of Ret surrogates that were determined using X-ray crystallography. The use of such Ret surrogate crystals and structural information can, for example, be used for identifying molecular scaffolds and for developing ligands that bind to and modulate Ret and for identifying improved ligands based on known ligands.

Compounds and methods for development of Ret modulators

A kit for prescreening protein concentration for crystallization includes a multiplicity of vials, a multiplicity of pre-selected reagents, and a multiplicity of sample plates. The reagents and a corresponding multiplicity of samples of the protein in solutions of varying concentrations are placed on sample plates. The sample plates containing the reagents and samples are incubated. After incubation the sample plates are examined to determine which of the sample concentrations are too low and which the sample concentrations are too high. The sample concentrations that are optimal for protein crystallization are selected and used.

Protein crystallography prescreen kit

An automated macromolecular crystallization screening system wherein a multiplicity of reagent mixes are produced. A multiplicity of analysis plates is produced utilizing the reagent mixes combined with a sample. The analysis plates are incubated to promote growth of crystals. Images of the crystals are made. The images are analyzed with regard to suitability of the crystals for analysis by x-ray crystallography. A design of reagent mixes is produced based upon the expected suitability of the crystals for analysis by x-ray crystallography. A second multiplicity of mixes of the reagent components is produced utilizing the design and a second multiplicity of reagent mixes is used for a second round of automated macromolecular crystallization screening. In one embodiment the multiplicity of reagent mixes are produced by a random selection of reagent components.

Automated macromolecular crystallization screening

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Livermore, CA, United States of America

Heike I Krupka