Results 91 to 100 of about 2,020,141 (269)

Discovery of natural anthraquinones as potent inhibitors against pancreatic lipase: structure-activity relationships and inhibitory mechanism

Journal of Enzyme Inhibition and Medicinal Chemistry
Obesity is acknowledged as a significant risk factor for various metabolic diseases, and the inhibition of human pancreatic lipase (hPL) can impede lipid digestion and absorption, thereby offering potential benefits for obesity treatment.
Zi-Qiang Chen, Wen-Yao He, Si-Yuan Yang, Hong-Hong Ma, Jing Zhou, Hao Li, Ya-Di Zhu, Xing-Kai Qian, Li-Wei Zou   +8 more
doaj   +1 more source

Degradation mechanism of the von Willebrand factor A2 domain by nattokinase

FEBS Letters, EarlyView.
Nattokinase, a natto‐derived protease, exhibits potent antithrombotic effects. This study demonstrates that nattokinase directly cleaves the von Willebrand factor (vWF) A2 domain in vitro. Unlike the native regulator ADAMTS13, nattokinase degrades folded vWF independently of shear stress.
Ryuichi Hyakumoto, Masatomo So, Ayako Furukawa, Kenji Sugase   +3 more
wiley   +1 more source

Pseudotumour in a Haemophiliac with Inhibitor

Indian Journal of Physical Medicine & Rehabilitation
A 41-year-old male haemophilic patient with inhibitor developed recurrent bleeding in the right thigh and eventually developed pseudotumour. Pseudotumour gradually progressed and ruptured on the evening of elective surgery.
Vasanthiamma Krishnannair Sreekala, Anila Das Greeshma   +1 more
doaj   +1 more source

The pyruvate generator is a common phenomenon in mitochondria from different rat and mouse brain regions

FEBS Letters, EarlyView.
The pyruvate generator, which causes activation of respiration by extra‐mitochondrial Ca2+, is also present and functional in rat brainstem mitochondria, as it is in other brain regions. This finding is confirmed by experiments with a fully reconstituted malate–aspartate shuttle (MAS).
Grazyna Debska‐Vielhaber, Niki Karavasili, Matthias Kunz, Zemfira Gizatullina, Timur Gainutdinov, Stefan Vielhaber, Wolfram S. Kunz, Frank N. Gellerich   +7 more
wiley   +1 more source

The ubiquitin‐proteasome system and autophagy as guardians of the cellular proteome

FEBS Letters, EarlyView.
This Perspective covers the three principles governing the crosstalk between the ubiquitin‐proteasome system and autophagy in cellular proteostasis: (1) a shared ubiquitin code routing substrates via shuttle factors or autophagy receptors; (2) spatial compartmentalization into phase‐separated degradation hubs and organelle‐specific modules (exemplified
Ivan Dikic
wiley   +1 more source

Structure-based design of new potent and highly selective PARP-1 inhibitor for treating colorectal cancer

Journal of Enzyme Inhibition and Medicinal Chemistry
Poly (ADP-ribose) polymerase 1 (PARP-1) exhibits high expression levels in colorectal cancer (CRC) patients and participates in multiple DNA damage repair pathways, thereby emerging as an attractive target.
Chunying Jiang, Shudan Yang, Yuting Wang, Liyuan Du, Miao-Miao Niu, Dongli Zhang   +5 more
doaj   +1 more source

An unexpected alternative viologen electron mediator site in tungsten‐containing formate dehydrogenase

FEBS Letters, EarlyView.
An unexpected alternative interaction site for ethyl viologen was identified in formate dehydrogenase 1 from Methylorubrum extorquens. Combined mutagenesis, kinetic analysis, and docking revealed that aromatic residues near an iron–sulfur cluster enable flavin mononucleotide‐independent electron transfer, offering a framework for engineering improved ...
Eleni G. Poloniataki, Yong Hwan Kim
wiley   +1 more source

Discovery of conformation constrained tetracyclic compounds as potent chitinase OfChi-h inhibitors with a novel binding mode

Journal of Enzyme Inhibition and Medicinal Chemistry
Chitinase h (Chi-h) has been identified as a promising pesticide target due to its exclusive distribution in lepidopteran insects and its essential role in the moulting processes.
Pengtao Yuan, Xi Jiang, Xintong Ni, Xusheng Shao, Xuhong Qian, Qing Yang   +5 more
doaj   +1 more source

Ubiquitination of secretory granules promotes their crinophagic degradation in Drosophila

FEBS Letters, EarlyView.
Ubiquitination of secretory granules in Drosophila larval salivary glands is a critical molecular trigger for crinophagy, the lysosomal degradation of unreleased, or low‐quality granules. The E3 ubiquitin ligase Cnot4 is recruited to the surface of secretory granules to induce crinophagy.
Tamás Csizmadia, Anna Dósa, Asha Kiran Maddali, András Jipa, Hajnalka Laczkó‐Dobos, Péter Lőw, Gábor Juhász   +6 more
wiley   +1 more source

Identification of chemical scaffolds for targeting ubiquitin-specific protease 11 (USP11) through high-throughput virtual screening

Journal of Enzyme Inhibition and Medicinal Chemistry
USP11 is a promising therapeutic target implicated in Alzheimer’s disease and various cancers; however, no specific inhibitors are currently available, with the only known inhibitor being mitoxantrone, which primarily targets topoisomerase II.
Hobin Lee, Sunghoon Hurh, Soomin Kang, Jihwan Yoon, Jong-Ik Hwang, Derek T. Logan, Hong-Rae Kim   +6 more
doaj   +1 more source