Carbonic anhydrases

Supuran, Claudiu T.

doi:10.1016/b978-0-12-823974-2.00014-0

Cited by 6 publications

(1 citation statement)

References 176 publications

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“…The hypoxia-triggered metabolic shi towards alternative glycolytic pathways to meet the energy requirements is critical to the survival of dividing cancer cells. 9 Fig. 1 gives insight of hCA IX role in hypoxic tumor cells.…”

Section: Introductionmentioning

confidence: 99%

Ligand based pharmacophore modelling and integrated computational approaches in the quest for small molecule inhibitors against hCA IX

Saravanan,

Chagaleti,

Packiapalavesam

et al. 2024

RSC Adv.

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Section: Introductionmentioning

confidence: 99%

Ligand based pharmacophore modelling and integrated computational approaches in the quest for small molecule inhibitors against hCA IX

Saravanan,

Chagaleti,

Packiapalavesam

et al. 2024

RSC Adv.

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Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles

Hefny,

El-Moselhy,

El-Din

et al. 2024

J. Med. Chem.

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A dual-targeting approach is predicted to yield better cancer therapy outcomes. Consequently, a series of coumarin-based thiazoles (5a−h, 6, and 7a−e) were designed and constructed as potential carbonic anhydrase (CA) and VEGFR-2 suppressors. The inhibitory actions of the target compounds were assessed against CA isoforms IX and VEGFR-2. The assay results showed that coumarin-based thiazoles 5a, 5d, and 5e can effectively inhibit both targets. 5a, 5d, and 5e cytotoxic effects were tested on pancreatic, breast, and prostate cancer cells (PANC1, MCF7, and PC3). Further mechanistic investigation disclosed the ability of 5e to interrupt the PANC1 cell progression in the S stage by triggering the apoptotic cascade, as seen by increased levels of caspases 3, 9, and BAX, alongside the Bcl-2 decline. Moreover, the in vivo efficacy of compound 5e as an antitumor agent was evaluated. Also, molecular docking and dynamics displayed distinctive interactions between 5e and CA IX and VEGFR-2 binding pockets.

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Coassembly of Cell-Penetrating Peptide Octaarginine with Acetazolamide: Emergent Interactions with E. coli

Choubey,

Chatterjee,

Pandey

et al. 2024

ACS Omega

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The investigation of established pharmaceutical agents for recalibrating usage strongly supplements new drug development. In this work, we have prepared coassembled complexes of acetazolamide (AZM) with the cationic peptide octaarginine (R8) in an attempt to enhance its potency and scope of use. R8 and AZM in different weight ratios coassemble into remarkable nano-and microstructures such as ribbons, sheets, and stick-like structures. A combination of FTIR, XRD, SEM, and DSC has been used to characterize the R8:AZM coassemblies. The sulfonamide SO 2 and NH 2 groups of AZM are associated with the guanidinium amine, free amine, and terminal carbonyl groups of R8 resulting in distinctive topologies. Treatment of Escherichia coli with the complexes results in a distinctive pattern of membrane disruption and pore formation. The R8:AZM coassemblies inhibit carbonic anhydrase and E. coli growth with greater efficiency compared to bare AZM. The 1:5 w/w complex leads to pronounced outer and inner membrane rupture and significantly restricts glucose uptake by E. coli. The ability of R8 and AZM to coassemble into a distinctive set of structures based solely on differences in their relative proportions and their engagement with E. coli as more than the sum of their parts are novel facets of R8 and AZM behavior and underscore a straightforward and elegant approach for enhancing the scope of use of small molecule drugs.

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Carbonic anhydrases

Cited by 6 publications

References 176 publications

Ligand based pharmacophore modelling and integrated computational approaches in the quest for small molecule inhibitors against hCA IX

Ligand based pharmacophore modelling and integrated computational approaches in the quest for small molecule inhibitors against hCA IX

Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles

Coassembly of Cell-Penetrating Peptide Octaarginine with Acetazolamide: Emergent Interactions with E. coli

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