Drug transporter proteins are critical to the distribution of a wide range of endogenous compounds and xenobiotics such as hormones, bile acids, peptides, lipids, sugars, and drugs. There are two classes of drug transporters– the solute carrier (SLC) transporters and ATP-binding cassette (ABC) transporters –which predominantly differ in the energy source utilized to transport substrates across a membrane barrier. Despite their hydrophobic nature and residence in the membrane bilayer, drug transporters have dynamic structures and adopt many conformations during the translocation process. Whereas there is significant literature evidence for the substrate specificity and structure-function relationship for clinically relevant drug transporters proteins, there is less of an understanding in the regulatory mechanisms that contribute to the functional expression of these proteins. Post-translational modifications have been shown to modulate drug transporter functional expression via a wide range of molecular mechanisms. These modifications commonly occur through the addition of a functional group (e.g. phosphorylation), a small protein (e.g. ubiquitination), sugar chains (e.g. glycosylation), or lipids (e.g. palmitoylation) on solvent accessible amino acid residues. These covalent additions often occur as a result of a signaling cascade and may be reversible depending on the type of modification and the intended fate of the signaling event. Here, we review the significant role in which post-translational modifications contribute to the dynamic regulation and functional consequences of SLC and ABC drug transporters and highlight recent progress in understanding their roles in transporter structure, function, and regulation.

药物转运蛋白对于分布广泛的内源性化合物和异种生物至关重要，例如激素，胆汁酸，肽，脂质，糖和药物。药物转运蛋白有两类-溶质载体（SLC）转运蛋白和ATP结合盒（ABC）转运蛋白-主要区别在于用于通过膜屏障转运底物的能源不同。尽管它们具有疏水性和驻留在膜双层中，但药物转运蛋白仍具有动态结构并在转运过程中采用许多构象。有大量文献证据证明临床相关药物转运蛋白的底物特异性和结构-功能关系，在有助于这些蛋白质功能表达的调控机制中，人们的了解还很少。已显示翻译后修饰可通过多种分子机制调节药物转运蛋白的功能性表达。这些修饰通常通过在溶剂可及的氨基酸残基上添加官能团（例如磷酸化），小蛋白（例如泛素化），糖链（例如糖基化）或脂质（例如棕榈酰化）而发生。这些共价添加通常是由于信号级联的结果而发生的，并且可能取决于信号类型的修饰类型和预期的命运是可逆的。这里，