title: 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine: a nucleoside reverse transcriptase inhibitor with highly potent activity against wide spectrum of HIV-1 strains, favorable toxic profiles, and stability in plasma.
abstract: Working hypotheses to solve the critical problems of the existing highly active anti-retroviral therapy were proposed. The study based on the hypotheses proved the validity of the hypotheses and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine, a nucleoside reverse transcriptase inhibitor, with highly potent activity against all HIV-1, very favorable toxic profiles, and stability in plasma. The nucleoside will prevent or delay the emergence of drug-resistant HIV-1 variants and be an ideal therapeutic agent for both HIV-1 and HBV infections.
authors: Yokomama College of Pharmacy, 601 Matano-cho, Totsuka, Yokohama, Japan. h.ohrui@hamayaku.ac.jp
authors: Hiroshi
authors: H
authors: Ohrui
authors: Satoru
authors: S
authors: Kohgo
authors: Hiroyuki
authors: H
authors: Hayakawa
authors: Eiichi
authors: E
authors: Kodama
authors: Masao
authors: M
authors: Matsuoka
authors: Tomohiro
authors: T
authors: Nakata
authors: Hiroaki
authors: H
authors: Mitsuya
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D003839:Deoxyadenosines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D051379:Mice; D013329:Structure-Activity Relationship
chemical_list: C520539:2'-deoxy-4'-C-ethynyl-2-fluoroadenosine; D019380:Anti-HIV Agents; D003839:Deoxyadenosines; D054303:HIV Reverse Transcriptase