Literature DB >> 32435392

Pharmacophore-Based Virtual Screening for Identification of Negative Modulators of GLI1 as Potential Anticancer Agents.

Fabrizio Manetti1,2, Barbara Stecca3, Roberta Santini3, Luisa Maresca3, Giuseppe Giannini4, Maurizio Taddei1,2, Elena Petricci1.   

Abstract

Starting from known GLI1 inhibitors, a pharmacophore-based virtual screening approach was applied to databases of commercially available compounds with the aim of identifying new GLI1 modulators. As a result, three different chemical scaffolds emerged that were characterized by a significant ability to reduce the transcriptional activity of the endogenous Hedgehog-GLI pathway and GLI1 protein level in murine NIH3T3 cells. They also showed a micromolar antiproliferative activity in human melanoma (A375) and medulloblastoma (DAOY) cell lines, without cytotoxicity in non-neoplastic mammary epithelial cells.
Copyright © 2020 American Chemical Society.

Entities:  

Year:  2020        PMID： 32435392      PMCID： PMC7236221          DOI： 10.1021/acsmedchemlett.9b00639

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  28 in total

1.  CAT3, a novel agent for medulloblastoma and glioblastoma treatment, inhibits tumor growth by disrupting the Hedgehog signaling pathway.

Authors:  Ju Chen; Haining Lv; Jinping Hu; Ming Ji; Nina Xue; Chao Li; Shuanggang Ma; Qin Zhou; Bin Lin; Yan Li; Shishan Yu; Xiaoguang Chen
Journal:  Cancer Lett       Date:  2016-08-02       Impact factor: 8.679

Review 2.  Design of Hedgehog pathway inhibitors for cancer treatment.

Authors:  Jitender Bariwal; Virender Kumar; Yuxiang Dong; Ram I Mahato
Journal:  Med Res Rev       Date:  2018-11-28       Impact factor: 12.944

3.  Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists.

Authors:  Matthias Lauth; Asa Bergström; Takashi Shimokawa; Rune Toftgård
Journal:  Proc Natl Acad Sci U S A       Date:  2007-05-09       Impact factor: 11.205

4.  Phase I Study of LY2940680, a Smo Antagonist, in Patients with Advanced Cancer Including Treatment-Naïve and Previously Treated Basal Cell Carcinoma.

Authors:  Johanna Bendell; Valerie Andre; Alan Ho; Ragini Kudchadkar; Michael Migden; Jeffrey Infante; Ramon V Tiu; Celine Pitou; Trevor Tucker; Les Brail; Daniel Von Hoff
Journal:  Clin Cancer Res       Date:  2018-02-26       Impact factor: 12.531

5.  Smoothened (SMO) receptor mutations dictate resistance to vismodegib in basal cell carcinoma.

Authors:  Sabrina Pricl; Barbara Cortelazzi; Valentina Dal Col; Domenico Marson; Erik Laurini; Maurizio Fermeglia; Lisa Licitra; Silvana Pilotti; Paolo Bossi; Federica Perrone
Journal:  Mol Oncol       Date:  2014-09-26       Impact factor: 6.603

6.  Loss of SUFU function in familial multiple meningioma.

Authors:  Mervi Aavikko; Song-Ping Li; Silva Saarinen; Pia Alhopuro; Eevi Kaasinen; Ekaterina Morgunova; Yilong Li; Kari Vesanen; Miriam J Smith; D Gareth R Evans; Minna Pöyhönen; Anne Kiuru; Anssi Auvinen; Lauri A Aaltonen; Jussi Taipale; Pia Vahteristo
Journal:  Am J Hum Genet       Date:  2012-09-07       Impact factor: 11.025

7.  Effects of oncogenic mutations in Smoothened and Patched can be reversed by cyclopamine.

Authors:  J Taipale; J K Chen; M K Cooper; B Wang; R K Mann; L Milenkovic; M P Scott; P A Beachy
Journal:  Nature       Date:  2000-08-31       Impact factor: 49.962

8.  Polymeric glabrescione B nanocapsules for passive targeting of Hedgehog-dependent tumor therapy in vitro.

Authors:  Cinzia Ingallina; Pedro M Costa; Francesca Ghirga; Rebecca Klippstein; Julie T Wang; Simone Berardozzi; Naomi Hodgins; Paola Infante; Steven M Pollard; Bruno Botta; Khuloud T Al-Jamal
Journal:  Nanomedicine (Lond)       Date:  2017-03-21       Impact factor: 5.307

9.  α-Mangostin-encapsulated PLGA nanoparticles inhibit pancreatic carcinogenesis by targeting cancer stem cells in human, and transgenic (Kras(G12D), and Kras(G12D)/tp53R270H) mice.

Authors:  Raj Kumar Verma; Wei Yu; Anju Shrivastava; Sharmila Shankar; Rakesh K Srivastava
Journal:  Sci Rep       Date:  2016-09-14       Impact factor: 4.379

10.  Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61.

Authors:  Andrea Calcaterra; Valentina Iovine; Bruno Botta; Deborah Quaglio; Ilaria D'Acquarica; Alessia Ciogli; Antonia Iazzetti; Romina Alfonsi; Ludovica Lospinoso Severini; Paola Infante; Lucia Di Marcotullio; Mattia Mori; Francesca Ghirga
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051
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  3 in total

1.  Quinolines and Oxazino-quinoline Derivatives as Small Molecule GLI1 Inhibitors Identified by Virtual Screening.

Authors:  Fabrizio Manetti; Luisa Maresca; Enrica Crivaro; Sara Pepe; Elena Cini; Snigdha Singh; Paolo Governa; Samuele Maramai; Giuseppe Giannini; Barbara Stecca; Elena Petricci
Journal:  ACS Med Chem Lett       Date:  2022-07-22       Impact factor: 4.632

Review 2.  Hedgehog Pathway Inhibitors as Targeted Cancer Therapy and Strategies to Overcome Drug Resistance.

Authors:  Ngoc Minh Nguyen; Jungsook Cho
Journal:  Int J Mol Sci       Date:  2022-02-03       Impact factor: 5.923

Review 3.  Functional Pyrazolo[1,5-a]pyrimidines: Current Approaches in Synthetic Transformations and Uses As an Antitumor Scaffold.

Authors:  Andres Arias-Gómez; Andrés Godoy; Jaime Portilla
Journal:  Molecules       Date:  2021-05-05       Impact factor: 4.411
  3 in total

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