Journal: Cell Death & Disease

Article Title: MAL2 reprograms lipid metabolism in intrahepatic cholangiocarcinoma via EGFR/SREBP-1 pathway based on single-cell RNA sequencing

doi: 10.1038/s41419-024-06775-7

Figure Lengend Snippet: A The superimposed MAL2 protein (AlphaFold ID: AF-Q969L2-F1) alongside compounds chosen via computer-aided screening. B Conformational and docking advantages of sarizotan from the leading MAL2-compound scoring top-five interaction model. C A simplified depiction of sarizotan occupying the MAL2 protein’s active site. D MST analysis quantified the binding tenacity between sarizotan and MAL2. E The impact of sarizotan on the EGFR/PI3K/AKT signal pathway in HUCCT1 and RBE cells was explored using western blotting. F CCK-8 assay traced the growth trajectories of HUCCT1 and RBE cells under DMSO or sarizotan administration at 0, 24, 48, and 72 h intervals. G Cell propagation of ICC cells under DMSO or sarizotan treatment was scrutinized via EdU assay, scale bar, 50 μm. H Representative images of tumors from nude mice treated with DMSO or sarizotan. I , J Tumor growth curves and tumor weights of each group. K The expression level of Ki67 in nude mice-derived xenograft tumor was determined by IHC, scale bar, 50 μm. *** P < 0.001.

Article Snippet: Fatostatin (SREBP-1 inhibitor), EGF, CHX, AG1478 (EGFR inhibitor), Sarizotan, and PA were bought from MedChemExpress, China.

Techniques: Binding Assay, Western Blot, CCK-8 Assay, EdU Assay, Expressing, Derivative Assay

Journal: Cell Death & Disease

Article Title: MAL2 reprograms lipid metabolism in intrahepatic cholangiocarcinoma via EGFR/SREBP-1 pathway based on single-cell RNA sequencing

doi: 10.1038/s41419-024-06775-7

Figure Lengend Snippet: When EGF is instigated, MAL2 sustains the membrane presence of EGFR, averting endocytosis, and persistently triggers the PI3K/AKT/SREBP-1 route. This sequence of events consequently accelerates lipid accretion in ICC and induces cisplatin insensitivity. Increased PA succeeds in preserving the membrane localization of MAL2. Sarizotan is identified as a diminutive molecular disruptor of MAL2, signifying its prospective utility in ICC therapy.

Article Snippet: Fatostatin (SREBP-1 inhibitor), EGF, CHX, AG1478 (EGFR inhibitor), Sarizotan, and PA were bought from MedChemExpress, China.

Techniques: Membrane, Sequencing, Preserving

Journal: Neurotherapeutics

Article Title: Rett Syndrome: Reaching for Clinical Trials

doi: 10.1007/s13311-015-0353-y

Figure Lengend Snippet: Current translational trials

Article Snippet: Sarizotan , Mouse , Newron Pharmaceuticals , Agonist of 5-HT1 receptors , Improves breathing.

Techniques: Expressing, In Vitro, Knock-In

Journal: Psychopharmacology

Article Title: Antidepressant-like properties of sarizotan in experimental Parkinsonism

doi: 10.1007/s00213-011-2356-7

Figure Lengend Snippet: Acute treatment with sarizotan reduces immobility in the modified forced swim test (mFST) of unilaterally 6-OHDA-lesioned but not in the normal rats. a The effect of saline and sarizotan on immobility in the mFST in normal (saline n = 6; sarizotan 1 mg/kg n = 6; sarizotan 2.5 mg/kg n = 6) and unilaterally 6-OHDA-lesioned (saline n = 15; sarizotan 1 mg/kg n = 6; sarizotan 2.5 mg/kg n = 16) rats. b The effect of saline and sarizotan on the horizontal activity in the open field of normal and unilaterally 6-OHDA-lesioned rats. * p < 0.05, *** p < 0.001 versus saline in the unilaterally 6-OHDA-lesioned rats; two-way ANOVA followed by Bonferroni's test for pairwise comparisons

Article Snippet: 6-OHDA-lesioned rats were treated with saline ( n = 15), and sarizotan (1 mg/kg, n = 6 and 2.5 mg/kg, i.p., Merck KGA, n = 16) in the acute experiments studying mFST and motor activity.

Techniques: Modification, Saline, Activity Assay

Journal: Psychopharmacology

Article Title: Antidepressant-like properties of sarizotan in experimental Parkinsonism

doi: 10.1007/s00213-011-2356-7

Figure Lengend Snippet: Effects of acute and chronic treatment with sarizotan and l -DOPA/benserazide on thigmotaxis and corner time in unilaterally 6-OHDA-lesioned rats. a The effects of saline ( n = 4), sarizotan ( n = 5), and l -DOPA/benserazide ( n = 9) alone or sarizotan + l -DOPA/benserazide in combination ( n = 5) on thigmotaxis (i.e., peripheral activity divided by total horizontal activity). b The effects of saline, sarizotan, and l -DOPA/benserazide alone or sarizotan + l -DOPA/benserazide in combination on corner time. * p < 0.05, ** p < 0.01 versus saline from the same day; # p < 0.05, ## p < 0.01, ### p < 0.001 versus sarizotan from the same day. Two-way ANOVA followed by Bonferroni's test for pairwise comparisons

Article Snippet: 6-OHDA-lesioned rats were treated with saline ( n = 15), and sarizotan (1 mg/kg, n = 6 and 2.5 mg/kg, i.p., Merck KGA, n = 16) in the acute experiments studying mFST and motor activity.

Techniques: Saline, Activity Assay

Journal: Psychopharmacology

Article Title: Antidepressant-like properties of sarizotan in experimental Parkinsonism

doi: 10.1007/s00213-011-2356-7

Figure Lengend Snippet: Effects of acute and chronic treatment with sarizotan on l -DOPA/benserazide-induced rotations, abnormal involuntary movements (AIMs) and motor activity in unilaterally 6-OHDA-lesioned rats. a , b , c , d The effect of saline ( n = 4), sarizotan ( n = 5), and l -DOPA/benserazide ( n = 9) alone or sarizotan + l -DOPA/benserazide in combination ( n = 5) on contralateral rotations ( a ), AIMs ( b ), horizontal activity ( c ), and rearing activity ( d ) in unilaterally 6-OHDA-lesioned rat on days 1 and 24. * p < 0.05, ** p < 0.01, *** p < 0.001 versus saline from the same day; ## p < 0.01 versus sarizotan from the same day; + p <0.05, +++ p < 0.001 versus sarizotan + l -DOPA/benserazide from the same day; § p < 0.05, §§§ p <0.001 versus l -DOPA on day 1. Two-way ANOVA followed by Bonferroni's test for pairwise comparisons. AIMs were analyzed with non-parametric Kruskal–Wallis test followed by Dunn's multiple comparison test

Article Snippet: 6-OHDA-lesioned rats were treated with saline ( n = 15), and sarizotan (1 mg/kg, n = 6 and 2.5 mg/kg, i.p., Merck KGA, n = 16) in the acute experiments studying mFST and motor activity.

Techniques: Activity Assay, Saline, Comparison

Journal: Psychopharmacology

Article Title: Antidepressant-like properties of sarizotan in experimental Parkinsonism

doi: 10.1007/s00213-011-2356-7

Figure Lengend Snippet: Chronic treatment with sarizotan increases cell proliferation in the SVZ of the striatum. a Representative images show differences in numbers of BrdU cells in the SVZ of the striatum after treatment with saline ( n = 4), sarizotan ( n = 5), or l -DOPA/benserazide ( n = 9) alone or sarizotan + l -DOPA/benserazide in combination ( n = 5) in both the lesioned and intact sides both in low magnification and high magnification ( inserts ). b Quantification of BrdU positive cells in the SVZ revealed significant increases in cell proliferation on the 6-OHDA-lesioned side with sarizotan and l -DOPA/benserazide both alone or in combination. * p < 0.05, ** p < 0.01 versus saline lesioned side; two-way ANOVA followed by Bonferroni's test for pairwise comparisons

Article Snippet: 6-OHDA-lesioned rats were treated with saline ( n = 15), and sarizotan (1 mg/kg, n = 6 and 2.5 mg/kg, i.p., Merck KGA, n = 16) in the acute experiments studying mFST and motor activity.

Techniques: Saline

Journal: Psychopharmacology

Article Title: Antidepressant-like properties of sarizotan in experimental Parkinsonism

doi: 10.1007/s00213-011-2356-7

Figure Lengend Snippet: Chronic treatment with sarizotan increases cell proliferation in the SGZ of the dentate gyrus. a Representative images show differences in numbers of BrdU positive cells in the SGZ of the hippocampus after treatment with saline ( n = 4), sarizotan ( n = 5), or l -DOPA/benserazide ( n = 9) alone or sarizotan + l -DOPA/benserazide in combination ( n = 5) in both the lesioned and intact sides. b Quantification of BrdU positive cells in the SGZ revealed a significant increase in cell proliferation on the 6-OHDA-lesioned side with sarizotan alone or in combination with l -DOPA/benserazide. * p < 0.05, ** p < 0.01 versus saline in the lesioned side; ## p < 0.01 versus l -DOPA/benserazide in the lesion side; two-way ANOVA followed by Bonferroni's test for pairwise comparisons

Article Snippet: 6-OHDA-lesioned rats were treated with saline ( n = 15), and sarizotan (1 mg/kg, n = 6 and 2.5 mg/kg, i.p., Merck KGA, n = 16) in the acute experiments studying mFST and motor activity.

Techniques: Saline

Journal: Psychopharmacology

Article Title: Antidepressant-like properties of sarizotan in experimental Parkinsonism

doi: 10.1007/s00213-011-2356-7

Figure Lengend Snippet: Chronic treatment with sarizotan increases cell proliferation in the SGZ of the dentate gyrus. a Representative images show differences in numbers of Ki-67 positive cells in the SGZ of the hippocampus after treatment with saline ( n = 4), sarizotan ( n = 5), or l -DOPA/benserazide ( n = 9) alone or sarizotan + l -DOPA/benserazide in combination ( n = 5) in the lesioned sides. b Quantification of Ki-67 positive cells in the SGZ revealed significant increases in cell proliferation in the 6-OHDA-lesioned side with either sarizotan or l -DOPA/benserazide alone or their combination. * p < 0.05, ** p < 0.01 versus saline in the lesioned side; + p < 0.05; ++ p < 0.01 versus sarizotan + l -DOPA/benserazide in the intact side; two-way ANOVA followed by Bonferroni's test for pairwise comparisons

Article Snippet: 6-OHDA-lesioned rats were treated with saline ( n = 15), and sarizotan (1 mg/kg, n = 6 and 2.5 mg/kg, i.p., Merck KGA, n = 16) in the acute experiments studying mFST and motor activity.

Techniques: Saline

Journal: Psychopharmacology

Article Title: Antidepressant-like properties of sarizotan in experimental Parkinsonism

doi: 10.1007/s00213-011-2356-7

Figure Lengend Snippet: Chronic treatment with sarizotan increases neurogenesis in the SGZ of the hippocampus. a Representative images from the granular layer of the hippocampus showing differences in numbers of DCX positive cells after treatment with saline ( n = 4), sarizotan ( n = 5), or l -DOPA/benserazide ( n = 9) alone or sarizotan + l -DOPA/benserazide in combination ( n = 5) in the lesioned side. b Quantification of DCX positive cells in the granular layer revealed significant increases in neurogenesis after treatment with sarizotan + l -DOPA/benserazide in combination. * p < 0.05 versus saline in the lesioned side; # p < 0.05 versus l -DOPA/benserazide in the lesioned side; two-way ANOVA followed by Bonferroni's test

Article Snippet: 6-OHDA-lesioned rats were treated with saline ( n = 15), and sarizotan (1 mg/kg, n = 6 and 2.5 mg/kg, i.p., Merck KGA, n = 16) in the acute experiments studying mFST and motor activity.

Techniques: Saline

Journal: Frontiers in Pharmacology

Article Title: Development of an AmpliSeq TM Panel for Next-Generation Sequencing of a Set of Genetic Predictors of Persisting Pain

doi: 10.3389/fphar.2018.01008

Figure Lengend Snippet: Current targeting of the genes included in the proposed NGS panel of persisting pain by novel drugs that are currently under active clinical development and include analgesia as the main clinical target or at least as one of the intended clinical indication.

Article Snippet: DRD2 , Phase II/III , Sarizotan hydrochloride , Dopamine D2 Receptor (DRD2) Antagonists , Newron.

Techniques: Transduction, Expressing