Polymeric Glabrescione B Nanocapsules for Passive Targeting of Hedgehog-dependent Tumor Therapy
            <i>In Vitro</i>

Ingallina, Cinzia; Costa, Pedro M.; Ghirga, Francesca; Klippstein, Rebecca; Wang, Julie; Berardozzi, Simone; Hodgins, Naomi O.; Infante, Paola; Pollard, Steven M.; Botta, Bruno; Al‐Jamal, Khuloud T.

doi:10.2217/nnm-2016-0388

Cited by 28 publications

(13 citation statements)

References 51 publications

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“…Most of them have major drawbacks, including the use of special and expensive reagents in large excess, long reaction times, vigorous conditions and very low yields. We previously provided a synthetic route for the total synthesis of GlaB featuring six-step with an overall yield of 7% [52], based on a palladium catalyzed cross coupling reaction of 3-iodochromone with the corresponding arylboronic acid. However, this approach is overall unfeasible for the synthesis of GlaB-ring B derivatives, due to the challenging mono-functionalization of the two hydroxylgroups in ring B.…”

Section: Chemistrymentioning

confidence: 99%

Synergistic inhibition of the Hedgehog pathway by newly designed Smo and Gli antagonists bearing the isoflavone scaffold

Berardozzi

Bernardi

Infante

et al. 2018

European Journal of Medicinal Chemistry

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Aberrant activation of the Hedgehog (Hh) pathway is responsible for the onset and progression of several malignancies. Small molecules able to block the pathway at the upstream receptor Smoothened (Smo) or the downstream effector Gli1 have thus emerged recently as valuable anticancer agents. Here, we have designed, synthesized, and tested new Hh inhibitors taking advantage by the highly versatile and privileged isoflavone scaffold. The introduction of specific substitutions on the isoflavone's ring B allowed the identification of molecules targeting preferentially Smo or Gli1. Biological assays coupled with molecular modeling corroborated the design strategy, and provided new insights into the mechanism of action of these molecules. The combined administration of two different isoflavones behaving as Smo and Gli antagonists, respectively, in primary medulloblastoma (MB) cells highlighted the synergistic effects of these agents, thus paving the way to further and innovative strategies for the pharmacological inhibition of Hh signaling.

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Section: Chemistrymentioning

confidence: 99%

Synergistic inhibition of the Hedgehog pathway by newly designed Smo and Gli antagonists bearing the isoflavone scaffold

Berardozzi

Bernardi

Infante

et al. 2018

European Journal of Medicinal Chemistry

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“… Healthy Kunming mice and tumor-bearing BALB/c mice after subcutaneous injection of A20 (murine lymphoma) cells Passive PCLlipid core nanocarriers 134 Eugenol or acetyl eugenol Orally or i.p. Tumor-bearing C57Bl6 mice after subcutaneous injection of B16F10 (murine melanoma) cells Passive PEGylated lipid squalene nanocarriers 135 Gemcitabine Convection-enhanced delivery (the infusion of therapeutic molecules directly into the brain) Healthy Sprague- Dawley or tumor-bearing Fischer 344 rats after intracranial implantation of RG2 (rat glioma) cells Passive PEGylated PLGA nanoca r riers 136 Glabrescione b i.v. Tumor-bearing SCID/Beige mice after subcutaneous injection of PANC-1 (human pancreas carcinoma) cells Passive PCLnanocarriers 137 Methotrexate Orally or i.v.…”

Section: Polymeric Nanocarriers For Anti-cancer Drugsmentioning

confidence: 99%

<p>Biomedical Applications of Multifunctional Polymeric Nanocarriers: A Review of Current Literature</p>

Karabasz¹,

Bzowska²,

Szczepanowicz³

2020

IJN

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Polymeric nanomaterials have become a prominent area of research in the field of drug delivery. Their application in nanomedicine can improve bioavailability, pharmacokinetics, and, therefore, the effectiveness of various therapeutics or contrast agents. There are many studies for developing new polymeric nanocarriers; however, their clinical application is somewhat limited. In this review, we present new complex and multifunctional polymeric nanocarriers as promising and innovative diagnostic or therapeutic systems. Their multifunctionality, resulting from the unique chemical and biological properties of the polymers used, ensures better delivery, and a controlled, sequential release of many different therapeutics to the diseased tissue. We present a brief introduction of the classical formulation techniques and describe examples of multifunctional nanocarriers, whose biological assessment has been carried out at least in vitro. Most of them, however, also underwent evaluation in vivo on animal models. Selected polymeric nanocarriers were grouped depending on their medical application: anti-cancer drug nanocarriers, nanomaterials delivering compounds for cancer immunotherapy or regenerative medicine, components of vaccines nanomaterials used for topical application, and lifestyle diseases, ie, diabetes.

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“…Recently, an isoflavone derivative, named as Glabrescione B (GlaB), was produced. GlaB is a small-molecule binding GLI1ZF and showed potential for reducing the growth of Hh/GLI-dependent tumor and cancer stem cells by interfering with its interaction with DNA [61,62]. In medulloblastoma cells, GlaB behaved as SMO and GLI antagonist, respectively, inhibiting the cell growth [61,63].…”

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Targeting Hedgehog (Hh) Pathway for the Acute Myeloid Leukemia Treatment

Terao

Minami

2019

Cells

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The Hedgehog (Hh) pathway, containing the Patched (PTCH) and Smoothened (SMO) multitransmembrane proteins, is the main regulator of vertebrate embryonic development. A non-canonical Hh pathway was recently observed in numerous types of solid cancers and hematological malignancies. Although acute myeloid leukemia (AML) is a common and lethal myeloid malignancy, the chemotherapy for AML has not changed in the last three decades. The Hh pathway and other intracellular signaling pathways are important for the tumor cells’ cycle or therapeutic resistance of AML cells. In this article, we will review the current trends in Hh pathway inhibitors for treating AML.

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Polymeric Glabrescione B Nanocapsules for Passive Targeting of Hedgehog-dependent Tumor Therapy In Vitro

Cited by 28 publications

References 51 publications

Synergistic inhibition of the Hedgehog pathway by newly designed Smo and Gli antagonists bearing the isoflavone scaffold

Synergistic inhibition of the Hedgehog pathway by newly designed Smo and Gli antagonists bearing the isoflavone scaffold

<p>Biomedical Applications of Multifunctional Polymeric Nanocarriers: A Review of Current Literature</p>

Targeting Hedgehog (Hh) Pathway for the Acute Myeloid Leukemia Treatment

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