Quadriga Biosciences, Inc.

Affymax Technologies, N.v.

Glaxo Wellcome Inc.

Kerry J Koller

Bernd Jandeleit

Wolf-Nicolas Fischer

William J Dower

Ronald W Barrett

Steven E Cwirla

Jung K Lee

Christine L Martens

Gordon Ringold

Beatrice Ruhland-Fritsch

Haim Kedar

Edward Perry Wallerstein

Beatrice Ruhland

&#x3b2;-Substituted &#x3b2;-amino acids, &#x3b2;-substituted &#x3b2;-amino acid derivatives, and &#x3b2;-substituted &#x3b2;-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The &#x3b2;-substituted &#x3b2;-amino acid derivatives and &#x3b2;-substituted &#x3b2;-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the &#x3b2;-substituted &#x3b2;-amino acid derivatives and &#x3b2;-substituted &#x3b2;-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The &#x3b2;-substituted &#x3b2;-amino acid derivatives and &#x3b2;-substituted &#x3b2;-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The &#x3b2;-substituted &#x3b2;-amino acid derivatives and &#x3b2;-substituted &#x3b2;-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

&#x3b2;-substituted &#x3b2;-amino acids and analogs as chemotherapeutic agents

Beta-substituted beta-amino acids and analogs as chemotherapeutic agents and uses thereof

Beta-substituted beta-amino acids and analogs as chemotherapeutic agents

&#x3b2;-substituted &#x3b2;-amino acids and analogs as chemotherapeutic agents and uses thereof

&#x3b2;-Substituted &#x3b3;-amino acids, &#x3b2;-substituted &#x3b3;-amino acid derivatives, and &#x3b2;-substituted &#x3b3;-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The &#x3b2;-substituted &#x3b3;-amino acid derivatives and &#x3b2;-substituted &#x3b3;-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the &#x3b2;-substituted &#x3b3;-amino acid derivatives and &#x3b2;-substituted &#x3b3;-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The &#x3b2;-substituted &#x3b3;-amino acid derivatives and &#x3b2;-substituted &#x3b3;-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The &#x3b2;-substituted &#x3b3;-amino acid derivatives and &#x3b2;-substituted &#x3b3;-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

&#x3b2;-substituted &#x3b3;-amino acids and analogs as chemotherapeutic agents

A multiple element color-corrected doubly telecentric lens and imaging system useful for imaging multiwell plates is described. The lens contains a biconvex field lens element L,, a positive meniscus lens element L,, concave toward the incident light side, a double-Gauss lens element group, a positive meniscus lens element L,, convex toward the incident light, a positive meniscus lens element L,, convex toward the incident light, and a plano concave field flattener lens element L,, concave toward the incident light side. The lens is very sensitive, and can be used to image scintillation proximity assays in multiwell plates.

Doubly telecentric lens and imaging system for multiwell plates

Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking adhesion of leukocytes to the selectins for the purpose of inhibiting inflammation as well as in diagnostic methods employing labeled peptides and peptide mimetics that bind selectins for the purpose of determining the site of inflammation in mammals which inflammation is mediated by the presence of one or more selectins.

Peptides and compounds that bind selectins including endothelium

Peptides and compounds that bind selectins including endothelial

Growing community of inventors

San Francisco, CA, United States of America

Kerry J Koller