Zobi Cengiz, Algul Oztekin
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Erzincan Binali Yildirim University, Erzincan, Turkiye.
Department of İliç Dursun Yildirim MYO, Erzincan Binali Yildirim University, Erzincan, Turkiye.
Chem Biol Drug Des. 2025 Jan;105(1):e70045. doi: 10.1111/cbdd.70045.
Invasive fungal infections (IFIs) pose significant challenges in clinical settings, particularly due to their high morbidity and mortality rates. The rising incidence of these infections, coupled with increasing antifungal resistance, underscores the urgent need for novel therapeutic strategies. Current antifungal drugs target the fungal cell membrane, cell wall, or intracellular components, but resistance mechanisms such as altered drug-target interactions, enhanced efflux, and adaptive cellular responses have diminished their efficacy. Recent research has highlighted the potential of dual inhibitors that simultaneously target multiple pathways or enzymes involved in fungal growth and survival. Combining pharmacophores, such as lanosterol 14α-demethylase (CYP51), heat shock protein 90 (HSP90), histone deacetylase (HDAC), and squalene epoxidase (SE) inhibitors, has led to the development of compounds with enhanced antifungal activity and reduced resistance. This dual-target approach, along with novel chemical scaffolds, not only represents a promising strategy for combating antifungal resistance but is also being utilized in the development of anticancer agents. This review explores the development of new antifungal agents that employ mono-, dual-, or multi-target strategies to combat IFIs. We discuss emerging antifungal targets, resistance mechanisms, and innovative therapeutic approaches that offer hope in managing these challenging infections.
侵袭性真菌感染(IFI)在临床环境中构成了重大挑战,特别是因其高发病率和死亡率。这些感染的发病率不断上升,再加上抗真菌耐药性的增加,凸显了对新型治疗策略的迫切需求。目前的抗真菌药物靶向真菌细胞膜、细胞壁或细胞内成分,但诸如改变药物-靶点相互作用、增强外排和适应性细胞反应等耐药机制已经削弱了它们的疗效。最近的研究突出了同时靶向参与真菌生长和存活的多种途径或酶的双重抑制剂的潜力。将诸如羊毛甾醇14α-去甲基酶(CYP51)、热休克蛋白90(HSP90)、组蛋白脱乙酰酶(HDAC)和角鲨烯环氧酶(SE)抑制剂等药效基团结合起来,已导致开发出具有增强抗真菌活性和降低耐药性的化合物。这种双靶点方法,连同新型化学支架,不仅是对抗抗真菌耐药性的一种有前途的策略,而且也被用于抗癌药物的开发。这篇综述探讨了采用单靶点、双靶点或多靶点策略来对抗IFI的新型抗真菌药物的开发。我们讨论了新兴的抗真菌靶点、耐药机制以及在应对这些具有挑战性的感染方面带来希望的创新治疗方法。