TY - JOUR
T1 - HIV-1 resistance mechanism to an electrostatically constrained peptide fusion inhibitor that is active against t-20-resistant strains
AU - Shimane, Kazuki
AU - Kawaji, Kumi
AU - Miyamoto, Fusako
AU - Oishi, Shinya
AU - Watanabe, Kentaro
AU - Sakagami, Yasuko
AU - Fujii, Nobutaka
AU - Shimura, Kazuya
AU - Matsuoka, Masao
AU - Kaku, Mitsuo
AU - Sarafianos, Stefan G.
AU - Kodama, Eiichi N.
PY - 2013/8
Y1 - 2013/8
N2 - T-20EK is a novel fusion inhibitor designed to have enhanced-helicity over T-20 (enfuvirtide) through engineered electrostatic interactions between glutamic acid (E) and lysine (K) substitutions. T-20EK efficiently suppresses wild-type and T-20-resistant variants. Here, we selected T-20EK-resistant variants. A combination of L33S and N43K substitutions in gp41 were required for high resistance to T-20EK. While these substitutions also caused resistance to T-20, they did not cause cross-resistance to other known fusion inhibitors.
AB - T-20EK is a novel fusion inhibitor designed to have enhanced-helicity over T-20 (enfuvirtide) through engineered electrostatic interactions between glutamic acid (E) and lysine (K) substitutions. T-20EK efficiently suppresses wild-type and T-20-resistant variants. Here, we selected T-20EK-resistant variants. A combination of L33S and N43K substitutions in gp41 were required for high resistance to T-20EK. While these substitutions also caused resistance to T-20, they did not cause cross-resistance to other known fusion inhibitors.
UR - http://www.scopus.com/inward/record.url?scp=84880264271&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84880264271&partnerID=8YFLogxK
U2 - 10.1128/AAC.00237-13
DO - 10.1128/AAC.00237-13
M3 - Article
C2 - 23689710
AN - SCOPUS:84880264271
SN - 0066-4804
VL - 57
SP - 4035
EP - 4038
JO - Antimicrobial Agents and Chemotherapy
JF - Antimicrobial Agents and Chemotherapy
IS - 8
ER -
