An investigation of targeted inhibition of transcription factor activity with pyrrole imidazole polyamide (PA) in chronic myeloid leukemia (CML) blast crisis cells

Hayatigolkhatmi, Kourosh; Padroni, Giacomo; Wu, Songhua; Fang, Lijing; Gómez-Castañeda, Eduardo; Hsieh, Ya‐Ching; Jackson, Lorna; Pellicano, Francesca; Burley, Glenn A.; Jørgensen, Heather G.

doi:10.1016/j.bmcl.2019.07.049

Cited by 6 publications

(1 citation statement)

References 14 publications

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“…A variety of PIPs have been designed to target master transcription regulatory factors, such as NF‐κB, STAT3, and E2F1, which are involved in cellular processes like cell proliferation, apoptosis, and immune responses 47,48 . Recent studies have shown the effectiveness of PIPs in regulating transcription factor activity and downstream gene expression.…”

Section: Designing Pips To Modulate Diverse Transcriptional Targetsmentioning

confidence: 99%

Nucleic acid‐based small molecules as targeted transcription therapeutics for immunoregulation

Bai,

Ziadlou,

Vaijayanthi

et al. 2023

Allergy

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Transcription therapy is an emerging approach that centers on identifying the factors associated with the malfunctioning gene transcription machinery that causes diseases and controlling them with designer agents. Until now, the primary research focus in therapeutic gene modulation has been on small‐molecule drugs that target epigenetic enzymes and critical signaling pathways. However, nucleic acid‐based small molecules have gained popularity in recent years for their amenability to be pre‐designed and realize operative control over the dynamic transcription machinery that governs how the immune system responds to diseases. Pyrrole–imidazole polyamides (PIPs) are well‐established DNA‐based small‐molecule gene regulators that overcome the limitations of their conventional counterparts owing to their sequence‐targeted specificity, versatile regulatory efficiency, and biocompatibility. Here, we emphasize the rational design of PIPs, their functional mechanisms, and their potential as targeted transcription therapeutics for disease treatment by regulating the immune response. Furthermore, we also discuss the challenges and foresight of this approach in personalized immunotherapy in precision medicine.

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Section: Designing Pips To Modulate Diverse Transcriptional Targetsmentioning

confidence: 99%

Nucleic acid‐based small molecules as targeted transcription therapeutics for immunoregulation

Bai,

Ziadlou,

Vaijayanthi

et al. 2023

Allergy

View full text Add to dashboard Cite

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Photocatalyst‐Free Visible‐Light Enabled Synthesis of Substituted Pyrroles from α‐Keto Vinyl Azides

et al. 2020

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An efficient photocatalyst‐free visible light enabled synthesis of substituted pyrroles from α‐keto vinyl azides (readily prepared via Knoevenagel condensation of phenacyl azides with 2‐oxo‐2H‐chromene‐3‐carbaldehydes) was developed. The reaction proceeds through a denitrogenative photodecomposition of α‐keto vinyl azides, 1,3‐amino group migration, and coupling of intermediates with secondary amines.magnified image

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Access to Pyrrolocoumarins through DBU‐Mediated Coupling of 2‐Oxo‐2H‐chromene‐3‐carbaldehydes and Phenacyl Azides

2022

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1,8‐Diazabicyclo [5.4.0]undec‐7‐ene (DBU) mediated annulation of 4‐(benzylthio/arylthio)‐2‐oxo‐2H‐chromene‐3‐carbaldehydes with phenacyl azides for the synthesis of biologically relevant pyrrolocoumarins was developed. This operationally simple and unique synthetic strategy allows the formation of desired pyrrolocoumarin in good yields (67‐84 %), and generates a new C−C and C−N bond in the overall process.

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An investigation of targeted inhibition of transcription factor activity with pyrrole imidazole polyamide (PA) in chronic myeloid leukemia (CML) blast crisis cells

Cited by 6 publications

References 14 publications

Nucleic acid‐based small molecules as targeted transcription therapeutics for immunoregulation

Nucleic acid‐based small molecules as targeted transcription therapeutics for immunoregulation

Photocatalyst‐Free Visible‐Light Enabled Synthesis of Substituted Pyrroles from α‐Keto Vinyl Azides

Access to Pyrrolocoumarins through DBU‐Mediated Coupling of 2‐Oxo‐2H‐chromene‐3‐carbaldehydes and Phenacyl Azides

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