AI Article Synopsis
- Researchers developed new compounds that combine amino acids (glutamine and tyrosine) with inhibitors targeting monocarboxylate transporters (MCT1/2) to fight B lymphoma cells.
- The study found that adding an amino acid transporter recognition element enhanced the compounds' ability to inhibit tumor growth in specific human cells.
- These amino acid-conjugated inhibitors also showed improved effectiveness in their drug-like properties, making them potential candidates for cancer treatment.
Article Abstract
Glutamine and tyrosine-based amino acid conjugates of monocarboxylate transporter types 1 and 2 inhibitors (MCT1/2) were designed, synthesized and evaluated for their potency in blocking the proliferation of a human B lymphoma cell line that expresses the transporters Asct2, LAT1 and MCT1. Appropriate placement of an amino acid transporter recognition element was shown to augment anti-tumour efficacy vs. Raji cells. Amino acid conjugation also improves the pharmacodynamic properties of experimental MCT1/2 inhibitors.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4917231 | PMC |
| http://dx.doi.org/10.1039/C5MD00579E | DOI Listing |
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