Total Synthesis and Microbiological Evaluation of Leopolic Acid A and Analogues [0.03%]
瑞香酸A及类似物的全合成和微生物评价
Jamie L Breunig,M Alejandro Valdes-Pena,Andrew W Ratchford et al.
Jamie L Breunig et al.
New antimicrobial scaffolds are scarce, and there is a great need for the development of novel therapeutics. In this study, we report a convergent 9-step synthesis of leopolic acid A and a series of targeted analogues. The designed compound...
Delineating the Role of GxxxG Motif in Amyloidogenesis: A New Perspective in Targeting Amyloid-Beta Mediated AD Pathogenesis [0.03%]
GxxxG基序在淀粉样变性中的作用的阐述：针对淀粉样-β介导的AD发病机制的新视角
Dibakar Sarkar,Anirban Bhunia
Dibakar Sarkar
The pursuit of a novel structural motif that can shed light on the key functional attributes is a primary focus in the study of protein folding disorders. Decades of research on Alzheimer's disease (AD) have centered on the Amyloid β (Aβ)...
Fusing Peptide Epitopes for Advanced Multiplex Serological Testing for SARS-CoV-2 Antibody Detection [0.03%]
用于SARS-CoV-2抗体检测的高级多重血清学检测的融合肽表位
Ali H Aldoukhi,Panayiotis Bilalis,Dana M Alhattab et al.
Ali H Aldoukhi et al.
The tragic COVID-19 pandemic, which has seen a total of 655 million cases worldwide and a death toll of over 6.6 million seems finally tailing off. Even so, new variants of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) contin...
Proteases Involved in Leader Peptide Removal during RiPP Biosynthesis [0.03%]
RiPP生物合成过程中涉及的领导肽去除蛋白酶
Sara M Eslami,Wilfred A van der Donk
Sara M Eslami
Ribosomally synthesized and post-translationally modified peptides (RiPPs) have received much attention in recent years because of their promising bioactivities and the portability of their biosynthetic pathways. Heterologous expression stu...
Conflicting Interfacial Electrostatic Interactions as a Design Principle to Modulate Long-Range Interdomain Communication [0.03%]
作为调节长程结构域间通讯的设计原则的相互冲突的界面静电相互作用
Adithi Kannan,Dhruv Kumar Chaurasiya,Athi N Naganathan
Adithi Kannan
The extent and molecular basis of interdomain communication in multidomain proteins, central to understanding allostery and function, is an open question. One simple evolutionary strategy could involve the selection of either conflicting or...
Xin Zhang,Squire J Booker
Xin Zhang
Deciphering the Synthetic and Refolding Strategy of a Cysteine-Rich Domain in the Tumor Necrosis Factor Receptor (TNF-R) for Racemic Crystallography Analysis and d-Peptide Ligand Discovery [0.03%]
破译肿瘤坏死因子受体(TNF-R)中富含半胱氨酸的结构域的合成和重构策略用于消旋晶体学分析和d-肽配体发现
Alexander J Lander,Yifu Kong,Yi Jin et al.
Alexander J Lander et al.
Many cell-surface receptors are promising targets for chemical synthesis because of their critical roles in disease development. This synthetic approach enables investigations by racemic protein crystallography and ligand discovery by mirro...
Katharine M Wright,Hanjie Jiang,Wendy Xia et al.
Katharine M Wright et al.
NaV1.7, the neuronal voltage-gated sodium channel isoform, plays an important role in the human body's ability to feel pain. Mutations within NaV1.7 have been linked to pain-related syndromes, such as insensitivity to pain. To date, the reg...
Karsten A S Eastman,Marcus C Mifflin,Paul F Oblad et al.
Karsten A S Eastman et al.
Ribosomally produced and post-translationally modified polypeptides (RiPPs) are a diverse group of natural products that are processed by a variety of enzymes to their biologically relevant forms. PapB is a member of the radical S-adenosyl-...
The Effect of Deuteration and Homologation of the Lactam Ring of Nirmatrelvir on Its Biochemical Properties and Oxidative Metabolism [0.03%]
乳酸环的氘代和同系列化对Nirmatrelvir的生化性质及其氧化代谢的影响
Elena Arutyunova,Alexandr Belovodskiy,Pu Chen et al.
Elena Arutyunova et al.
This study explores the relationship between structural alterations of nirmatrelvir, such as homologation and deuteration, and metabolic stability of newly synthesized derivatives. We developed a reliable synthetic protocol toward dideutero...