Despite great progress in clinical treatment, cancer remains a serious health problem contributing to significant morbidity and mortality worldwide. Although chemotherapy is a common therapeutic measure, multidrug resistance (MDR) presents a major challenge that often leads to poor prognosis. The abnormal expression of glycosyltransferases (GTs) leading to aberrant glycosylation patterns are considered a marker of cancer. Furthermore, the biosynthesis of these glycoconjugates has been associated with tumor proliferation, invasion and metastasis. Recently, studies have found that GTs are involved in mediating MDR in cancer cells through complex mechanisms and can influence therapeutic effect. In this review, we focus on several types of cancers and summarize previous studies on the correlation between GTs and MDR.