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Table 3 IC50 values obtained in inhibition experimentsa.

From: The V1-V3 region of a brain-derived HIV-1 envelope glycoprotein determines macrophage tropism, low CD4 dependence, increased fusogenicity and altered sensitivity to entry inhibitors

  SK3 anti-CD4 (ng/ml) T-1249 (nM) T-1249-BR (nM) BMS-378806 (nM) HNG-105 (μM)
Br 119 (58–246) 173 (129–230) 195 (157–298) 15 (9.4–23) 3.8 (2.2–6.5)
BS 79 (60–102) 140 (113–172) 155 (83–289) 20 (13–31) 1.8 (0.9–3.7)
Bv1v3 94 (55–158) 227 (110–468) 245 (156–387) 8.2 (5.7–12) 21 (12–36)
Bv1v2 22 (13–36) 224 (174–288) 155 (123–195) 4.8 (3.5–6.6) 48 (9.8–231)
Br(N283T) 60 (32–114) 166 (102–271) 221 (148–329) 13 (4.6–35) 7.2 (2.2–24)
Spl 5.7 (2.3–14) 37 (19–71) 27 (17–43) 1.8 (1.3–2.7) 16 (6.7–39)
SB 11 (6.4–18) 83 (53–129)b 41 (30–56)b 2.0 (1.2–3.5) 25 (12–50)
Sv1v3 n.d. n.d. n.d. 0.9 (0.6–1.3) n.d.
Sv1v2 n.d. n.d. n.d. 1.2 (0.7–2.2) n.d.
Spl(T283N) 11 (7.3–18) n.d. n.d. 0.9 (0.7–1.3) n.d.
DS17 5.4 (3.8–7.7) 210 (160–274)b 92 (73–116)b 41 (29–58) 4.1 (2.7–6.2)
DS17(N283T) 5.1 (4.0–6.4) 155 (119–202) 104 (72–150) 32 (24–41) 2.6 (1.0–6.6)
BaL n.d. 102 (85–122) 124 (103–149) 29 (15–59) 58 (14–241)
HxB n.d. n.d. n.d. 3.9 (2.8–5.4) 1.6 (0.7–3.6)
  1. a Non-linear regression analysis of dose response curves generated for various viruses and inhibitors was performed with GraphPad Prism software; IC50 values are shown, with 95% confidence limits between parenthesis.
  2. b SB and DS17 were the only Env that demonstrated statistically significant greater sensitivity to T-1249-BR than to parental T-1249 (F test, p < 0.05 and p < 0.001, respectively).
  3. n.d., not determined.