Journal: Molecular pain

Article Title: AXL signaling in primary sensory neurons contributes to chronic compression of dorsal root ganglion-induced neuropathic pain in rats.

doi: 10.1177/1744806919900814

Figure Lengend Snippet: Figure 4. Effects of AXL inhibitor TP0903 on CCD-induced nociceptive hypersensitivities. The dose of TP0903 (0.05, 0.5, or 1 lg) or vehicle solution was intrathecally administered 1 h before CCD or sham surgery and once daily for five days after CCD or sham surgery. The doses of 0.5 and 1 lg inhibited (a) the decrease of PWTs to mechanical stimulation, (b) PWLs to thermal stimulation, and (c) positive response latencies to cold stimulation on the ipsilateral side of CCD rats. N ¼ 6 rats/group. Two-way repeated measure ANOVA (effect vs. group time interaction) followed by post hoc Tukey tests, **P < 0.01 versus the corresponding time point in the Sham þ Veh group. ##P < 0.01 versus the corresponding time point in the CCD þVeh group. PWT: paw-withdrawal threshold; PWL: paw-withdrawal latency; CCD: chronic compression of dorsal root ganglion.

Article Snippet: Intrathecal TP0903 (HY12963; MedChem Express, Shanghai, China) or vehicle (20% dimethyl sulfoxide) was administered 1 h before CCD surgery and then daily, from day 1 through day 5 post-CCD, TP0903 was injected intrathecally at three different doses (0.05, 0.50, and 1.00 lg).

Techniques:

Journal: Molecular pain

Article Title: AXL signaling in primary sensory neurons contributes to chronic compression of dorsal root ganglion-induced neuropathic pain in rats.

doi: 10.1177/1744806919900814

Figure Lengend Snippet: Figure 7. Mediation by the intracellular signaling molecule, mTOR, of nociceptive effects of AXL. (a) The protein amount of p-mTOR and total mTOR increased in the ipsilateral L4/L5 DRGs on days 7 and 14 after CCD surgery. N ¼ 3 rats/time point. One-way ANOVA (expression vs. time points) followed by post hoc Tukey test, *P < 0.05, **P < 0.01 versus day 0 (sham group). Repeatedly intrathecal injection of (b) TP0903 (1 lg) or (c) AXL siRNA (Si, 5 lM in 10 lL vehicle solution) reduced mTOR expression in compressed DRGs of CCD rats. N ¼ 3 rats/time point. One-way ANOVA (effect vs. the treated groups) followed by post hoc Tukey tests, *P < 0.05, **P < 0.01, versus the Sham þ Veh group; ##P < 0.01 versus the CCD þVeh group. DRG: dorsal root ganglion; CCD: chronic compression of DRG; mTOR: mammalian target of rapamycin.

Article Snippet: Intrathecal TP0903 (HY12963; MedChem Express, Shanghai, China) or vehicle (20% dimethyl sulfoxide) was administered 1 h before CCD surgery and then daily, from day 1 through day 5 post-CCD, TP0903 was injected intrathecally at three different doses (0.05, 0.50, and 1.00 lg).

Techniques: Expressing, Injection

Journal: Expert opinion on therapeutic targets

Article Title: Does Axl have potential as a therapeutic target in pancreatic cancer?

doi: 10.1080/14728222.2018.1527315

Figure Lengend Snippet: Clinical trials of therapies targeting Axl

Article Snippet: DDR1–2 1.5nM l/lb Advanced cancer MGCD516 NCT02219711 Mirati Therapeutics Inc. INCB081776 Axl/MerTK 0.61nM I Advanced solid tumors INCB081776 ± Nivolumab NCT03522142 Incyte Corporation Bemcentinib (BGB324) Axl, Tie-2, FLT4 14nM I and II Non-small cell lung cancer Bemcentinib + Erlotinib NCT02424617 BerGenBio ASA I and II Acute myeloid leukemia, myelodysplastic syndromes Bemcentinib ± Cytarabine or Decitabine NCT02488408 BerGenBio ASA II Lung cancer metastatic, NSCLC stage IV, Adenocarcinoma of lung Bemcentinib + Pembrolizumab NCT03184571 BerGenBio ASA II Triple negative breast cancer, inflammatory breast cancer stage IV Bemcentinib + Pembrolizumab NCT03184558 BerGenBio ASA TP-0903 Axl, MerTK, Tyro3, Aurora A/ B, JAK2, ALK.

Techniques: Clinical Proteomics, Modification