Ruxolitinib binding to human serum albumin: bioinformatics, biochemical and functional characterization in JAK2V617F⁺ cell models.

ABSTRACT: Ruxolitinib is a type I JAK inhibitor approved by FDA for targeted therapy of Philadelphia-negative myeloproliferative neoplasms (MPNs), all characterized by mutations activating the JAK2/STAT signaling pathway. Treatment with ruxolitinib improves constitutional symptoms and splenomegaly. However, patients can become resistant to treatment and chronic therapy has only a mild effect on molecular/pathologic remissions. Drugs interaction with plasma proteins, i.e. human serum albumin (HSA), is an important factor affecting the intensity and duration of their pharmacological actions. Here, the ruxolitinib recognition by the fatty acid binding sites (FAs) 1, 6, 7, and 9 of HSA has been investigated from the bioinformatics, biochemical and/or biological viewpoints. Docking simulations indicate t

SUBMITTER: De Marinis E 

PROVIDER: S-EPMC6841977 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature