Small-molecule inhibitors of ferrochelatase are antiangiogenic agents

Sishtla, Kamakshi; Lambert-Cheatham, Nathan; Lee, Bit; Han, Duk Hee; Park, Jaehui; Pasha, Sheik Pran Babu Sardar; Lee, Sanha; Kwon, Sangil; Anbukkarasi, Muniyandi; Park, Bomina; Odell, Noa; Waller, Sydney; Park, Il Yeong; Lee, Soo Jae; Seo, Seung‐Yong; Corson, Timothy W.

doi:10.1016/j.chembiol.2022.01.001

Cited by 7 publications

(4 citation statements)

References 57 publications

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“…Ferrochelatase (FECH), the key enzyme for the final step of heme biosynthesis in eukaryotes, functions to insert a Fe 2+ ion into the center of the porphyrin ring of protoporphyrin IX (PPIX) [ 22 ]. In our previous study, we demonstrated that DMC binds to FECH to inhibit its enzymatic activity [ 12 ].…”

Section: Resultsmentioning

confidence: 99%

Flavonoid 4,4′-dimethoxychalcone selectively eliminates senescent cells via activating ferritinophagy

Wang,

Yang,

et al. 2024

Redox Biology

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Section: Resultsmentioning

confidence: 99%

Flavonoid 4,4′-dimethoxychalcone selectively eliminates senescent cells via activating ferritinophagy

Wang,

Yang,

et al. 2024

Redox Biology

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“…This strategy is based on the inhibition of enzyme activity, leading to the accumulation of PpIX in cells. Several inhibitors of ferrochelatase activity have been identified [90,91]. Sishtla et al [92] described that nearly 20,000 compounds from ChemDiv and ChemBridge libraries were evaluated on a high-throughput screen to assess their effect at 10 µM on ferrochelatase activity.…”

Section: -Ala In Antimicrobial Photodynamic Inactivationmentioning

confidence: 99%

On the Possibility of Using 5-Aminolevulinic Acid in the Light-Induced Destruction of Microorganisms

Zdubek,

Maliszewska

2024

IJMS

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Antimicrobial photodynamic inactivation (aPDI) is a method that specifically kills target cells by combining a photosensitizer and irradiation with light at the appropriate wavelength. The natural amino acid, 5-aminolevulinic acid (5-ALA), is the precursor of endogenous porphyrins in the heme biosynthesis pathway. This review summarizes the recent progress in understanding the biosynthetic pathways and regulatory mechanisms of 5-ALA synthesis in biological hosts. The effectiveness of 5-ALA-aPDI in destroying various groups of pathogens (viruses, fungi, yeasts, parasites) was presented, but greater attention was focused on the antibacterial activity of this technique. Finally, the clinical applications of 5-ALA in therapies using 5-ALA and visible light (treatment of ulcers and disinfection of dental canals) were described.

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“…Furthermore, FECH inhibition decreased HRECs oxidative phosphorylation and mitochondrial complex IV, reduced mitochondrial fusion and mass, indicating for the first time that FECH-mediated mitochondrial heme metabolism and dysfunction regulated ECs angiogenesis [ 249 ]. Through high-throughput screening, a class of triazolopyrimidinone was identified to competitively inhibit FECH and angiogenesis in vitro and in vivo, indicating FECH inhibitors could be effective in treating retinal neovascularization and other diseases [ 250 ].…”

Section: Other Mitochondrial Protein In Ecs Angiogenesismentioning

confidence: 99%

Mitochondria in endothelial cells angiogenesis and function: current understanding and future perspectives

et al. 2023

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Endothelial cells (ECs) angiogenesis is the process of sprouting new vessels from the existing ones, playing critical roles in physiological and pathological processes such as wound healing, placentation, ischemia/reperfusion, cardiovascular diseases and cancer metastasis. Although mitochondria are not the major sites of energy source in ECs, they function as important biosynthetic and signaling hubs to regulate ECs metabolism and adaptations to local environment, thus affecting ECs migration, proliferation and angiogenic process. The understanding of the importance and potential mechanisms of mitochondria in regulating ECs metabolism, function and the process of angiogenesis has developed in the past decades. Thus, in this review, we discuss the current understanding of mitochondrial proteins and signaling molecules in ECs metabolism, function and angiogeneic signaling, to provide new and therapeutic targets for treatment of diverse cardiovascular and angiogenesis-dependent diseases.

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Small-molecule inhibitors of ferrochelatase are antiangiogenic agents

Cited by 7 publications

References 57 publications

Flavonoid 4,4′-dimethoxychalcone selectively eliminates senescent cells via activating ferritinophagy

Flavonoid 4,4′-dimethoxychalcone selectively eliminates senescent cells via activating ferritinophagy

On the Possibility of Using 5-Aminolevulinic Acid in the Light-Induced Destruction of Microorganisms

Mitochondria in endothelial cells angiogenesis and function: current understanding and future perspectives

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