Structures of human folate receptors reveal biological trafficking states and diversity in folate and antifolate recognition.

ABSTRACT: Antifolates, folate analogs that inhibit vitamin B9 (folic acid)-using cellular enzymes, have been used over several decades for the treatment of cancer and inflammatory diseases. Cellular uptake of the antifolates in clinical use occurs primarily via widely expressed facilitative membrane transporters. More recently, human folate receptors (FRs), high affinity receptors that transport folate via endocytosis, have been proposed as targets for the specific delivery of new classes of antifolates or folate conjugates to tumors or sites of inflammation. The development of specific, FR-targeted antifolates would be accelerated if additional biophysical data, particularly structural models of the receptors, were available. Here we describe six distinct crystallographic models that provide insigh

SUBMITTER: Wibowo AS 

PROVIDER: S-EPMC3780903 | biostudies-literature | 2013 Sep

REPOSITORIES: biostudies-literature