Sabizabulin, a Potent Orally Bioavailable Colchicine Binding Site Agent, Suppresses HER2+ Breast Cancer and Metastasis

Sabizabulin, a Potent Orally Bioavailable Colchicine Binding Site Agent, Suppresses HER2+ Breast Cancer and Metastasis

HER2+ breast cancer accounts for 15% of all breast cancer cases. Current frontline therapy for HER2+ metastatic breast cancer relies on targeted antibodies, trastuzumab and pertuzumab, combined with microtubule inhibitors in the taxane class (paclitaxel or docetaxel). It is well known that the clini...

Full description

Bibliographic Details
Main Authors:	Raisa I. Krutilina, Kelli L. Hartman, Damilola Oluwalana, Hilaire C. Playa, Deanna N. Parke, Hao Chen, Duane D. Miller, Wei Li, Tiffany N. Seagroves
Format:	Article
Language:	English
Published:	MDPI AG 2022-10-01
Series:	Cancers
Subjects:	HER2<sup>+</sup> breast cancer colchicine binding site inhibitor orally available tubulin inhibitor patient-derived xenograft tumor metastasis
Online Access:	https://www.mdpi.com/2072-6694/14/21/5336

Similar Items

Recurrence of the oxazole motif in tubulin colchicine site inhibitors with anti-tumor activity
by: Marilia Barreca, et al.
Published: (2021-07-01)

Synthesis, Antiproliferative Activity and Molecular Docking Studies of Novel Doubly Modified Colchicine Amides and Sulfonamides as Anticancer Agents
by: Julia Krzywik, et al.
Published: (2020-04-01)

Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation
by: Wei Liu, et al.
Published: (2023-12-01)

Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation
by: Mohamed Hagras, et al.
Published: (2021-01-01)

New Series of Double-Modified Colchicine Derivatives: Synthesis, Cytotoxic Effect and Molecular Docking
by: Julia Krzywik, et al.
Published: (2020-08-01)

First-in-Class Colchicine-Based Visible Light Photoswitchable Microtubule Dynamics Disrupting Agent
by: Filip Borys, et al.
Published: (2023-07-01)

Structural Changes, Biological Consequences, and Repurposing of Colchicine Site Ligands
by: Felipe Montecinos, et al.
Published: (2023-05-01)

Antiproliferative Activity and Molecular Docking of Novel Double-Modified Colchicine Derivatives
by: Urszula Majcher, et al.
Published: (2018-11-01)

A Water-Stable Zn-MOF Used as Multiresponsive Luminescent Probe for Sensing Fe<sup>3+</sup>/Cu<sup>2+</sup>, Trinitrophenol and Colchicine in Aqueous Medium
by: Xiaojing Zhou, et al.
Published: (2022-10-01)

Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review
by: Eavan C. McLoughlin, et al.
Published: (2020-01-01)

Colchicine Blocks Tubulin Heterodimer Recycling by Tubulin Cofactors TBCA, TBCB, and TBCE
by: Sofia Nolasco, et al.
Published: (2021-04-01)

Interaction of Colchicine-Site Ligands With the Blood Cell-Specific Isotype of β-Tubulin—Notable Affinity for Benzimidazoles
by: Felipe Montecinos, et al.
Published: (2022-05-01)

Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors
by: Shanbo Yang, et al.
Published: (2022-12-01)

Synthesis and Biological Evaluation of Novel Triple-Modified Colchicine Derivatives as Potent Tubulin-Targeting Anticancer Agents
by: Urszula Majcher, et al.
Published: (2018-11-01)

Quick and Simple Detection Technique to Assess the Binding of Antimicrotubule Agents to the Colchicine-Binding Site
by: Moreau Emmanuel, et al.
Published: (2010-01-01)

Quick and Simple Detection Technique to Assess the Binding of Antimicrotubule Agents to the Colchicine-Binding Site
by: Fortin Sébastien, et al.
Published: (2010-04-01)

Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity
by: Ehsan Karimikia, et al.
Published: (2019-10-01)

Synthesis and Anticancer Activity of Mitotic-Specific 3,4-Dihydropyridine-2(1<i>H</i>)-thiones
by: Magdalena Perużyńska, et al.
Published: (2021-02-01)

In Silico Conformation of the Drug Colchicine into Tubulin Models and Acute Phytotoxic Activity on <i>Cucumis sativus</i> Radicles
by: Omar Aristeo Peña-Morán, et al.
Published: (2022-07-01)

Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors
by: Monica-Cornelia Sardaru, et al.
Published: (2020-01-01)

Synthesis, biological evaluation, and molecular modelling of new naphthalene-chalcone derivatives as potential anticancer agents on MCF-7 breast cancer cells by targeting tubulin colchicine binding site
by: Guangcheng Wang, et al.
Published: (2020-01-01)

Novel Natural Product- and Privileged Scaffold-Based Tubulin Inhibitors Targeting the Colchicine Binding Site
by: Mengqi Dong, et al.
Published: (2016-10-01)

Hybridization Approach to Identify Salicylanilides as Inhibitors of Tubulin Polymerization and Signal Transducers and Activators of Transcription 3 (STAT3)
by: Marta Gargantilla, et al.
Published: (2022-07-01)

What is the lowest lethal dose of colchicine?
by: Vanyo Mitev
Published: (2023-11-01)

4’-O-Methylbroussochalcone B as a novel tubulin polymerization inhibitor suppressed the proliferation and migration of acute myeloid leukaemia cells
by: Ziying Liu, et al.
Published: (2021-01-01)

Plocabulin, a novel tubulin inhibitor, has potent antitumor activity in patient-derived xenograft models of gastrointestinal stromal tumors
by: Yannick Wang, et al.
Published: (2020-11-01)

Novel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells
by: Dong-Jun Fu, et al.
Published: (2020-01-01)

Colchicine Overdose in a Suicidal Attempt
by: Fatemeh Eghbali, et al.
Published: (2019-10-01)

Modulation of CD8<sup>+</sup> T Cell Responses by Radiotherapy—Current Evidence and Rationale for Combination with Immune Checkpoint Inhibitors
by: Seung Hyuck Jeon, et al.
Published: (2023-11-01)

Sensitive Fluorescence Assay for the Detection of Alkaline Phosphatase Based on a Cu<sup>2+</sup>-Thiamine System
by: Han Zhao, et al.
Published: (2021-01-01)

Contrasting Toxicity of a Fomesafen-Based Herbicide on Three Freshwater Phytoplanktonic Species
by: Jonathan Naoum, et al.
Published: (2023-01-01)

Toxicity Assessment of [<sup>177</sup>Lu]Lu−iFAP/iPSMA Nanoparticles Prepared under GMP-Compliant Radiopharmaceutical Processes
by: Tania Hernández-Jiménez, et al.
Published: (2022-11-01)

Molecular Characterization of the Dual Effect of the GPER Agonist G-1 in Glioblastoma
by: Alex Hirtz, et al.
Published: (2022-11-01)

Effects of colchicine on cardiac functions
by: Yusuf Ziya Şener, et al.
Published: (2019-11-01)

Suppressing Effect of Na<sup>+</sup>/Ca<sup>2+</sup> Exchanger (NCX) Inhibitors on the Growth of Melanoma Cells
by: Zikai Liu, et al.
Published: (2022-01-01)

Combination Therapy with a Bispecific Antibody Targeting the hERG1/β1 Integrin Complex and Gemcitabine in Pancreatic Ductal Adenocarcinoma
by: Tiziano Lottini, et al.
Published: (2023-03-01)

Perimyocarditis Associated with Immune Checkpoint Inhibitors: A Case Report and Review of the Literature
by: Walid Shalata, et al.
Published: (2024-01-01)

Systemic Blood Immune Cell Populations as Biomarkers for the Outcome of Immune Checkpoint Inhibitor Therapies
by: Carlos Hernandez, et al.
Published: (2020-03-01)

Physicochemical and Biological Characterization of rhC1INH Expressed in CHO Cells
by: Ekaterina Zubareva, et al.
Published: (2021-11-01)

Design, synthesis and evaluation of dihydro-1H-indene derivatives as novel tubulin polymerisation inhibitors with anti-angiogenic and antitumor potency
by: Shengtao Xu, et al.
Published: (2023-12-01)