A novel SadP-scFv UCHT1 lectibody activates T cells and mediates lysis of Burkitt's lymphoma cells [0.03%]
Jana Tomisch,Jonas Gräber,Olga N Makshakova et al.
Jana Tomisch et al.
Abnormal glycosylation has been long considered a hallmark of cancer progression. Carbohydrate-binding proteins, also known as lectins, offer a unique way to target glycosylation changes in malignant cells. The present study repurposes SadP...
Pratchaya Watthaisong,Chadaporn Kantiwiriyawanitch,Watcharapa Jitkaroon et al.
Pratchaya Watthaisong et al.
d-Luciferin (d-LH2) is the most used substrate for beetle luciferases in various bioluminescence applications. Here, we successfully synthesized six d-LH2 analogues including 5',7'-dimethoxy-d-LH2 and 7'-methylnaphthol-d-LH2 as novel compou...
Xanthine-based photoaffinity probes allow assessment of ligand engagement by TRPC5 channels [0.03%]
基于黄嘌呤的光亲和探针可评估TRPC5通道配体结合状况
Claudia C Bauer,Aisling Minard,Isabelle B Pickles et al.
Claudia C Bauer et al.
TRPC1/4/5 cation channels are emerging drug targets for the treatment of, amongst others, central nervous system (CNS) disorders, kidney disease, and cardiovascular and metabolic disease. Various small-molecule TRPC1/4/5 modulators have bee...
Dual spatio-functional control of a fission yeast-based bioprocessor upon chemical induction [0.03%]
一种裂殖酵母生物处理器在化学诱导下的双功能空间控制
Stavroula Melina Sakellakou,Valérie Migeot,Laure-Elie Carloni et al.
Stavroula Melina Sakellakou et al.
Next-generation therapies are advancing beyond small molecules and proteins toward engineered living microorganisms that interact symbiotically with their host and respond to signals precisely when and where needed. Despite progress in the ...
From loops to caps: discriminating peptide binding to distinct G-quadruplex tetrads using 5-furyl-2'-deoxyuridine fluorescent probes [0.03%]
从环到帽：使用5-呋喃基-2'-脱氧尿苷荧光探针区分肽结合至不同的G-四链体四联体
Jack Barr,Tayler D Prieto Otoya,Christine Cardin et al.
Jack Barr et al.
We report the use of 5-furyl-2'-deoxyuridine (5FU) as a fluorescent probe to distinguish ligand binding to distinct G-quadruplex tetrads. Site-specific incorporation of 5FU into T95-2T at the capping regions enabled discrimination of peptid...
High-resolution structure of proIAPP(1-48) fibrils suggests a mechanistic pathway for diabetes-associated IAPP fibril polymorphs [0.03%]
高分辨率的前IAPP(1-48)原纤维结构提出了糖尿病相关IAPP原纤维多态性的机理路径
Dylan Valli,Michał Maj
Dylan Valli
The human islet amyloid polypeptide (hIAPP) aggregates into amyloid fibrils that contribute to β-cell failure in type 2 diabetes. hIAPP is produced from a 67-residue precursor, proIAPP, but incomplete cleavage by prohormone convertase 2 (P...
A novel class of small-molecule inhibitors targeting bacteriophage infection [0.03%]
一类针对噬菌体感染的新式小分子抑制剂
Konstantin Plöchl,Thomas Böttcher
Konstantin Plöchl
Bacteriophages have emerged as important factors in human health and disease, with elevated phage levels associated with exacerbated inflammatory bowel disease, type 2 diabetes and poor outcomes in skin and lung infections. The mechanisms l...
Covalent fragment screening to inhibit the E3 ligase activity of bacterial NEL enzymes SspH1 and SspH2 [0.03%]
用于抑制细菌NEL酶SspH1和SspH2E3连接酶活性的共价片段筛选
Cassandra R Kennedy,Katherine A McPhie,Aini Vuorinen et al.
Cassandra R Kennedy et al.
As the global fight against antimicrobial resistance in bacteria becomes increasingly pressing, new tool compounds are needed to study and evaluate novel therapeutic targets. Here, cysteine-directed fragment-based drug discovery is coupled ...
Nucleobase catalysts for the enzymatic activation of 8-oxoguanine DNA glycosylase 1 [0.03%]
用于激活8-氧鸟嘌呤DNA糖基化酶1的核苷酸催化剂
Emily C Hank,Nicholas D D&#x;Arcy-Evans,Emma Rose Scaletti et al.
Emily C Hank et al.
Bifunctional DNA glycosylases employ an active site lysine or the N-terminus to form a Schiff base with an abasic (AP) site base excision repair intermediate. For 8-oxoguanine DNA glycosylase 1 (OGG1), cleaving this reversible structure is ...
RNA-binding fluorogenic probes: G-clamp conjugated with a thiazole orange derivative for screening RNA-binding small molecules [0.03%]
用于筛选结合RNA的小分子的G-钳与噻唑橙衍生物连接而成的RNA结合荧光探针
Ryosuke Nagasawa,Kazumitsu Onizuka,Ryohei Iwata et al.
Ryosuke Nagasawa et al.
RNA has emerged as an attractive target for drug discovery, increasing the importance of methods for identifying RNA-binding small molecules. Fluorescent indicator displacement (FID) assays are commonly used for screening such molecules. Ho...