Journal: Anti-Infective Agents
Introduction: Leishmaniasis is an endemic disease caused by the protozoan parasite Leishmania. Current treatments for the parasite are limited by cost, availability and drug resistance as the occurrence of leishmaniasis continues to be more prevalent. Sulfonamides are a class of compounds with medicinal properties which have been used to treat bacterial and parasitic disease via various pathways especially as antimetabolites for folic acid.
Methods: New derivatives of sulfonamide compounds were assessed for their impact on Leishmania cell viability and potential pathways for inhibition were evaluated. Leishmania tarentolae (ATCC Strain 30143) axenic promastigote cells were grown in brain heart infusion (BHI) medium and treated with varying concentrations of the new sulfonamide compounds. Light microscopy and viability tests were used to assess the cells with and without treatment.
Drug Metabolism Letters Volume 11, Issue 2
Current Organic Synthesis Volume 14, Issue 8
Current Drug Targets Volume 19, Issue 3
The Natural Products Journal Volume 8, Issue 1
Current Topics in Medicinal Chemistry Volume 17, Issue 30
Current Pharmaceutical Design Volume 23, Issue 37
Journal: Current Drug Metabolism
Background: Cancer cells use several mechanisms to resist the cytotoxic effects of drugs, resulting in tumor progression and invasion. One such mechanism capitalizes on the body’s natural defense against xenobiotics by increasing the rate of xenobiotic efflux and metabolic inactivation. Xenobiotic metabolism typically involves conversion of parent molecules to more soluble and easily excreted derivatives in reactions catalyzed by Phase I and Phase II drug metabolizing enzymes.
Methods: We performed a structured search of peer-reviewed literature on P450 (CYP) 3A, with a focus on CYP3A4 and CYP3A5.
Results: Recent reports indicate that components of the xenobiotic response system are upregulated in some diseases, including many cancers. Such components include the pregnane X receptor (PXR), CYP3A4 and CYP3A5 enzymes. The CYP3A enzymes are a subset of the numerous enzymes that are transcriptionally activated following the interaction of PXR and many ligands.
Conclusion: Intense research is ongoing to understand the functional ramifications of aberrant expression of these components in diseased states with the goal of designing novel drugs that can selectively target them.
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Medicinal Chemistry Volume 14, Issue 2
Clinical Immunology, Endocrine & Metabolic Drugs Volume 4, Issue 1
Anti-Cancer Agents in Medicinal Chemistry Volume 17, Issue 14
Letters in Organic Chemistry Volume 15, Issue 3
Current Molecular Medicine Volume 17, Issue 6
Protein & Peptide Letters Volume 24, Issue 12