1. Articles in category: Small Molecules

    1-24 of 51 1 2 3 »
    1. GD2 ganglioside-binding antibody 14G2a and specific aurora A kinase inhibitor MK-5108 induce autophagy in IMR-32 neuroblastoma cells.

      GD2 ganglioside-binding antibody 14G2a and specific aurora A kinase inhibitor MK-5108 induce autophagy in IMR-32 neuroblastoma cells.

      Apoptosis. 2018 Jul 19;:

      Authors: Durbas M, Pabisz P, Wawak K, Wiśniewska A, Boratyn E, Nowak I, Horwacik I, Woźnicka O, Rokita H

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      Mentions: Antibody
    2. Somatic mutations in specific and connected sub-pathways are associated to short neuroblastoma patients' survival and indicate proteins targetable at onset of disease.

      Somatic mutations in specific and connected sub-pathways are associated to short neuroblastoma patients' survival and indicate proteins targetable at onset of disease.

      Int J Cancer. 2018 Jul 11;:

      Authors: Esposito MR, Binatti A, Pantile M, Coppe A, Mazzocco K, Longo L, Capasso M, Lasorsa VA, Luksch R, Bortoluzzi S, Tonini GP

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    3. Harmine, a dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor induces caspase-mediated apoptosis in neuroblastoma.

      Harmine, a dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor induces caspase-mediated apoptosis in neuroblastoma.

      Cancer Cell Int. 2018;18:82

      Authors: Uhl KL, Schultz CR, Geerts D, Bachmann AS

      Abstract Background: Neuroblastoma (NB) is an early childhood malignancy that arises from the developing sympathetic nervous system. Harmine is a tricyclic β-carboline alkaloid isolated from the harmal plant that exhibits both cytostatic and cytotoxic effects.

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      Mentions: MYCN
    4. S-trityl-L-cysteine, a novel Eg5 inhibitor, is a potent chemotherapeutic strategy in neuroblastoma.

      S-trityl-L-cysteine, a novel Eg5 inhibitor, is a potent chemotherapeutic strategy in neuroblastoma.

      Oncol Lett. 2018 Jul;16(1):1023-1030

      Authors: Wu W, Jingbo S, Xu W, Liu J, Huang Y, Sheng Q, Lv Z

      Abstract Eg5 is a member of the kinesin-5 family. It is involved in the formation of the bipolar spindle and serves a crucial role in mitosis; meaning that mitotic activation may serve as a chemotherapeutic strategy.

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    5. A High-Content Screening of Anticancer Compounds Suggests the Multiple Tyrosine Kinase Inhibitor Ponatinib for Repurposing in Neuroblastoma Therapy

      A High-Content Screening of Anticancer Compounds Suggests the Multiple Tyrosine Kinase Inhibitor Ponatinib for Repurposing in Neuroblastoma Therapy

      Novel druggable targets have been discovered in neuroblastoma (NB), paving the way for more effective treatments. However, children with high-risk NB still show high mortality rates prompting for a search of novel therapeutic options. Here, we aimed at repurposing FDA-approved drugs for NB treatment by performing a high-content screening of a 349 anticancer compounds library.

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      Mentions: Treatment
    6. The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines.

      The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines.

      Arch Toxicol. 2018 Jun 09;:

      Authors: Kolbinger FR, Koeneke E, Ridinger J, Heimburg T, Müller M, Bayer T, Sippl W, Jung M, Gunkel N, Miller AK, Westermann F, Witt O, Oehme I

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    7. Nano-targeted induction of dual ferroptotic mechanisms eradicates high-risk neuroblastoma

      Nano-targeted induction of dual ferroptotic mechanisms eradicates high-risk neuroblastoma

      High-risk neuroblastoma is a devastating malignancy with very limited therapeutic options. Here, we identify withaferin A (WA) as a natural ferroptosis-inducing agent in neuroblastoma, which acts through a novel double-edged mechanism. WA dose-dependently either activates the nuclear factor–like 2 pathway through targeting of Kelch-like ECH-associated protein 1 (noncanonical ferroptosis induction) or inactivates glutathione peroxidase 4 (canonical ferroptosis induction).

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    8. Antiproliferative and apoptotic effect of LY2090314, a GSK-3 inhibitor, in neuroblastoma in vitro.

      Antiproliferative and apoptotic effect of LY2090314, a GSK-3 inhibitor, in neuroblastoma in vitro.

      BMC Cancer. 2018 May 11;18(1):560

      Authors: Kunnimalaiyaan S, Schwartz VK, Jackson IA, Clark Gamblin T, Kunnimalaiyaan M

      Abstract BACKGROUND: Neuroblastoma (NB) is a devastating disease. Despite recent advances in the treatment of NB, about 60% of high-risk NB will have relapse and therefore long-term event free survival is very minimal.

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    9. Autophagy inhibition improves the cytotoxic effects of receptor tyrosine kinase inhibitors.

      Autophagy inhibition improves the cytotoxic effects of receptor tyrosine kinase inhibitors.

      Cancer Cell Int. 2018;18:63

      Authors: Aveic S, Pantile M, Polo P, Sidarovich V, De Mariano M, Quattrone A, Longo L, Tonini GP

      Abstract Background: A growing field of evidence suggests the involvement of oncogenic receptor tyrosine kinases (RTKs) in cell transformation.

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    10. A high-content screening of anti-cancer compounds suggests the multiple tyrosine kinase inhibitor ponatinib for repurposing in neuroblastoma therapy.

      A high-content screening of anti-cancer compounds suggests the multiple tyrosine kinase inhibitor ponatinib for repurposing in neuroblastoma therapy.

      Mol Cancer Ther. 2018 Apr 25;:

      Authors: Sidarovich V, De Mariano M, Aveic S, Pancher M, Adami V, Gatto P, Pizzini S, Pasini L, Croce M, Parodi F, Cimmino F, Avitabile M, Emionite L, Cilli M, Ferrini S, Pagano A, Capasso M, Quattrone A, Tonini GP, Longo L

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    11. PIM Kinases Are a Potential Prognostic Biomarker and Therapeutic Target in Neuroblastoma

      PIM Kinases Are a Potential Prognostic Biomarker and Therapeutic Target in Neuroblastoma

      The majority of high-risk neuroblastoma patients are refractory to, or relapse on, current treatment regimens, resulting in 5-year survival rates of less than 50%. This emphasizes the urgent need to identify novel therapeutic targets. Here, we report that high PIM kinase expression is correlated with poor overall survival. Treatment of neuroblastoma cell lines with the pan-PIM inhibitors AZD1208 or PIM-447 suppressed proliferation through inhibition of mTOR signaling.

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    12. Good clinical response to alectinib, a second generation ALK inhibitor, in refractory neuroblastoma

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      Mentions: Refractory ALK
    13. Induction of MEK/ERK activity by AZD8055 confers acquired resistance in neuroblastoma.

      Induction of MEK/ERK activity by AZD8055 confers acquired resistance in neuroblastoma.

      Biochem Biophys Res Commun. 2018 Mar 20;:

      Authors: Xu DQ, Toyoda H, Qi L, Morimoto M, Hanaki R, Iwamoto S, Komada Y, Hirayama M

      Abstract Mammalian target of rapamycin (mTOR) complex (mTORC) is frequently activated in diverse cancers. Although dual mTORC1/2 inhibitors are currently under development to treat various malignancies, the emergence of drug resistance has proven to be a major complication.

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    14. Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.

      Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.

      Eur J Med Chem. 2018 Mar 06;150:282-291

      Authors: Zhao C, Zang J, Ding Q, Inks ES, Xu W, Chou CJ, Zhang Y

      Abstract In the past decade, although research and development of histone deacetylase (HDAC) inhibitors as therapeutic agents have achieved great accomplishments, especially in oncology field, there is still an urgent need for the discovery of isoform-selective HDAC inhibitors considering the side effects caused by nonselective HDAC inhibitors. HDAC8, a unique class I zinc-dependent HDAC, is becoming a potential target in cancer and other diseases. In the current study ...

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      Mentions: Side Effects
    15. Combination therapy in neuroblastoma: It`s all about the mix

      The combination of two cell division inhibitors causes malignant nervous system tumors to die off, as scientists from the “Hopp Children’s Cancer Center at the NCT Heidelberg” (KiTZ) have shown in experimental studies.The combination strategy could be the key to new targeted therapies against this aggressive type of tumor. The Hopp Children’s Cancer Center at […]

      The post Combination therapy in neuroblastoma: It`s all about the mix appeared first on Healthcanal.com.

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      Mentions: ALK
    16. A kinome-wide RNAi screen identifies ALK as a target to sensitize neuroblastoma cells for HDAC8-inhibitor treatment.

      A kinome-wide RNAi screen identifies ALK as a target to sensitize neuroblastoma cells for HDAC8-inhibitor treatment.

      Cell Death Differ. 2018 Mar 07;:

      Authors: Shen J, Najafi S, Stäble S, Fabian J, Koeneke E, Kolbinger FR, Wrobel JK, Meder B, Distel M, Heimburg T, Sippl W, Jung M, Peterziel H, Kranz D, Boutros M, Westermann F, Witt O, Oehme I

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      Mentions: Treatment ALK
    17. PIM kinases are a potential prognostic biomarker and therapeutic target in neuroblastoma.

      PIM kinases are a potential prognostic biomarker and therapeutic target in neuroblastoma.

      Mol Cancer Ther. 2018 Feb 13;:

      Authors: Brunen D, de Vries RC, Lieftink C, Beijersbergen RL, Bernards R

      Abstract The majority of high-risk neuroblastoma patients are refractory to, or relapse on current treatment regimens, resulting in 5-year survival rates of less than 50%. This emphasizes the urgent need to identify novel therapeutic targets.

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    18. Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma.

      Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma.

      Oncotarget. 2018 Jan 05;9(2):2304-2319

      Authors: Arnhold V, Schmelz K, Proba J, Winkler A, Wünschel J, Toedling J, Deubzer HE, Künkele A, Eggert A, Schulte JH, Hundsdoerfer P

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      Mentions: MYCN
    19. The novel kinase inhibitor ponatinib is an effective anti-angiogenic agent against neuroblastoma.

      The novel kinase inhibitor ponatinib is an effective anti-angiogenic agent against neuroblastoma.

      Invest New Drugs. 2016 Dec;34(6):685-692

      Authors: Whittle SB, Patel K, Zhang L, Woodfield SE, Du M, Smith V, Zage PE

      Abstract Background High-risk neuroblastoma has poor outcomes with high rates of relapse despite aggressive treatment, and novel therapies are needed to improve these outcomes.

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      Mentions: Treatment Relapse
    20. Small molecule inhibitor regorafenib inhibits RET signaling in neuroblastoma cells and effectively suppresses tumor growth in vivo.

      Small molecule inhibitor regorafenib inhibits RET signaling in neuroblastoma cells and effectively suppresses tumor growth in vivo.

      Oncotarget. 2017 Nov 28;8(61):104090-104103

      Authors: Chen Z, Zhao Y, Yu Y, Pang JC, Woodfield SE, Tao L, Guan S, Zhang H, Bieerkehazhi S, Shi Y, Patel R, Vasudevan SA, Yi JS, Muscal JA, Xu GT, Yang J

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      Mentions: MYCN
    21. High expression of β-catenin contributes to the crizotinib resistant phenotype in the stem-like cell population in neuroblastoma.

      High expression of β-catenin contributes to the crizotinib resistant phenotype in the stem-like cell population in neuroblastoma.

      Sci Rep. 2017 Dec 04;7(1):16863

      Authors: Alshareef A, Gupta N, Zhang HF, Wu C, Haque M, Lai R

      Abstract ALK has been identified as a novel therapeutic target in neuroblastoma (NB), but resistance to ALK inhibitors (such as crizotinib) is well recognized.

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      Mentions: ALK
    22. Structure-based design and biological characterization of selective histone deacetylase 8 (HDAC8) inhibitors with anti-neuroblastoma activity.

      Structure-based design and biological characterization of selective histone deacetylase 8 (HDAC8) inhibitors with anti-neuroblastoma activity.

      J Med Chem. 2017 Nov 30;:

      Authors: Heimburg T, Kolbinger FR, Zeyen P, Ghazy E, Herp D, Schmidtkunz K, Melesina J, Shaik TB, Erdmann F, Schmidt M, Romier C, Robaa D, Witt O, Oehme I, Jung M, Sippl W

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    1-24 of 51 1 2 3 »
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