Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: ?-Substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-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 ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Abstract: Compositions and methods for protecting normal, healthy cells during chemotherapy are disclosed. The methods include administering one or more compounds that inhibit the cell cycle of rapidly regenerating normal cells and a chemotherapeutic agent. The cell cycle inhibitors can be administered prior to administration of a chemotherapeutic agent. The chemotherapeutic agents can be ?-substituted ?-amino acids, ?-substituted ?-amino acid derivatives, and ?-substituted ?-amino acid analogs. Pharmaceutical compositions comprising the ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs and uses thereof are also disclosed. The ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs can be administered in conjunction with one or more compounds that inhibit the cell cycle of rapidly proliferating normal healthy cells. The cell cycle inhibitors can ameliorate the adverse effects of the ?-substituted ?-amino acid derivatives and ?-substituted ?-amino acid analogs.

Abstract: Bivalent molecules that target cancer cells by simultaneously binding to at least two different compounds, and methods for their use in treating, diagnosing, imaging and staging cancers are provided.