Quadriga Biosciences, Inc.

Maxymune Therapeutics, Inc.

Gordon Ringold

Bernd Jandeleit

Wolf-Nicolas Fischer

Kerry J Koller

Guangyao Gao

Phenylalanine-based inhibitors of the Large Amino Acid Transporter 1 (LAT1) are disclosed. The compounds are useful in modulating the transcellular transport of substrates of LAT1 such as large neutral amino acids. The compounds are useful in immunomodulation therapies.

Phenylalanine-based LAT1 inhibitors and uses thereof

&#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.

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

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

Growing community of inventors

Los Altos Hills, CA, United States of America

Gordon Ringold