Binding Modes of Two Novel Non-Nucleoside Reverse Transcriptase Inhibitors, YM-215389 and YM-228855, to HIV Type-1 Reverse Transcriptase

  title={Binding Modes of Two Novel Non-Nucleoside Reverse Transcriptase Inhibitors, YM-215389 and YM-228855, to HIV Type-1 Reverse Transcriptase},
  author={Eiichi N Kodama and Masaya Orita and Naoyuki Masuda and Osamu Yamamoto and Masahiro Fujii and Tetsuro Ohgami and Shunji Kageyama and Mitsuaki Ohta and T Hatta and Hiroshi Inoue and Hiroshi Suzuki and Kenji Sudo and Yasuaki Shimizu and Masao Matsuoka},
  journal={Antiviral Chemistry and Chemotherapy},
  pages={133 - 141}
Background: YM-215389 and YM-228855 are thiazolidenebenzenesulfonamide (TBS) derivatives and novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) that inhibit not only wild-type, but also the K103N- and Y181C-substituted reverse transcriptase (RT) of HIV type-1 (HIV-1). Methods: To characterize the binding modes of the TBS derivatives in detail, the anti-HIV-1 activities of YM-215389 and YM-228855 against various NNRTI-resistant clones were examined. Docking studies with HIV-1 RT were… 

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