Results 181 to 190 of about 5,282,956 (341)

Structural insights into the binding mode of the hypnotic drug vornorexant to orexin receptors

Acta Crystallographica Section F, EarlyView.
The crystal structure of the human orexin type 2 receptor–vornorexant complex (3.29 Å resolution) and orexin type 1 receptor docking revealed a conserved U‐shaped binding conformation, explaining the high affinity and balanced dual antagonism of this dual orexin receptor antagonist. The structural data validate the rational design that incorporated a 1,
Masashi Mima, Chiemi Mishima-Tsumagari, Mayumi Sakata-Sakuta, Ryo Iwaoka, Kunihiko Iwamoto   +4 more
wiley   +1 more source

Covalent fluorescent probes for 2‐arachidonoylglycerol metabolic pathways

British Journal of Pharmacology, EarlyView.
Abstract Covalent fluorescent probes have emerged as versatile chemical tools to visualise active enzymes in complex biological systems. When tailored for specific applications, ranging from activity‐based protein profiling for drug development to high spatiotemporal resolution imaging of enzymatic activities, these probes provide unique insights into ...
Nick D. F. Puijmbroeck, Mario van der Stelt   +1 more
wiley   +1 more source

Enhancing antitumour response to proteasome inhibitors with inhibitors of insulin‐degrading enzyme, a new molecular vulnerability in multiple myeloma

British Journal of Pharmacology, EarlyView.
Inhibitors of insulin‐degrading enzyme boost PI cytotoxicity through an increased sensitivity of proteasome to PI inhibitors, induction of ISR, DNA damage and Myc down‐regulation. They overcome PI resistance in vitro and induce tumour regression in vivo.
Laetitia Lesire, Rebecca Deprez‐Poulain, Damien Bosc, Florence Leroux, Valerie Landry, Sarah Ourabah, Morgane Tardy, Clara Maillard, Ronan Gealageas, Julie Dumont, Adrien Herledan, Sandrine Warenghem, Manon Cruette, Celine Lenglart, Alexandre Biela, Catherine Piveteau, Eva De Smedt, Catharina Muylaert, Wenguang Liang, Elvira Garcia De Paco, Elina Alaterre, Sara Ovejero, Nicolas Robert, Fabien Delahaye, Wei‐Jen Tang, Peter van Endert, Elke De Bruyne, Jérôme Moreaux, Benoit Deprez   +28 more
wiley   +1 more source

Ring Transformation of Heterocycles Transformation of 4, 5-Dihydro-5, 5-Dimethyl-H-1, 2, 4-Triazoles Into 5-Methyl-H-1, 2, 4-Triazoles

, 2001
Reaction of 1-aryl-3-acetyl-4, 5-dihydro-5, 5-dimethyl-1H-1, 2, 4-triazoles (3) with acetyl chloride or acetic anhydride is found to give the ring transformation product 1-aryl-3-acetyl-5-methyl-1H-1, 2, 4-triazoles (4) instead of the expected N-acetyl derivative (5). This ring transformation is believed to start with N-acylation of the dihydrotriazole
openaire   +1 more source

Deep and disseminated dermatophytosis in immunocompromised populations—A systematic review

Journal of the European Academy of Dermatology and Venereology, EarlyView.
Dermatophyte infections of the dermis and subcutaneous tissue (i.e. deep dermatophytosis)—associated with secondary complications including pseudomycetoma and systemic dissemination—affect vulnerable populations with primary or acquired immunodeficiencies.
Aditya K. Gupta, Tong Wang, Susmita, Ditte Marie L. Saunte, Roderick Hay, Vincent Piguet   +5 more
wiley   +1 more source

Arabidopsis inositol polyphosphate kinase activities regulate COP9 deneddylation functions in phosphate homeostasis

Journal of Integrative Plant Biology, EarlyView.
Plant phosphate (Pi) homeostasis relies on coordinated activities of the inositol polyphosphate kinases IPK1 and ITPK1, which balance localized InsP7 biosynthesis to control COP9 signalosome (CSN)‐dependent deneddylation of cullin 1 (CUL1). Perturbation of this equilibrium affects the stability of SPX4, a key negative regulator of phosphate starvation ...
Yashika Walia, Medha Noopur, Ishana Bhattacharya, Bhaskar Chandra Sahoo, Mritunjay Kasera, Naga Jyothi Pullagurla, Smritikana Dutta, Guizhen Liu, Gabriel Schaaf, Henning Jessen, Debabrata Laha, Souvik Bhattacharjee, Saikat Bhattacharjee   +12 more
wiley   +1 more source

Platelet‐Rich Fibrins as Local Drug‐Delivery Carriers

Journal of Periodontal Research, EarlyView.
Autologous platelet concentrates (APCs), particularly platelet‐rich fibrin (PRF), act as biologically active fibrin scaffolds, capable of entrapping and gradually releasing therapeutic agents in oral and periodontal therapy. The incorporation of bioactive compounds, such as antibiotics, antifungals, vitamins, antidiabetic drugs, and exosomes, enhances ...
Karim M. Fawzy El‐Sayed, Christof E. Dörfer   +1 more
wiley   +1 more source

Nucleophilic substitution of a phthalimidyl group with morpholine in an N¹-methyl-1,2,3-triazole: crystallographic evidence for migration of the methylene bridge. [PDF]

Acta Crystallogr C Struct Chem
Palme PR, Goddard R, Leutzsch M, Richter A, Imming P, Seidel RW.   +5 more
europepmc   +1 more source

OsbHLH064, an IVb bHLH Transcription Factor, Regulates Iron Homeostasis and Enhances Grain Fe Accumulation in Rice

Plant Biotechnology Journal, EarlyView.
ABSTRACT Iron (Fe) is an essential micronutrient for plant growth and development. The maintenance of Fe homeostasis relies on sophisticated regulatory networks where bHLH transcription factors play a key role. However, how these factors coordinate to regulate this vital process is not fully understood.
Fei Gao, Zhikai Zhu, Kaixin Xue, Zijing Fu, Jitong Yue, Na Zhang, Hongli Zhou, Yaqin Deng, Jing Zhou, Liuhui Kuang, Tao Yan, Lin Li, Christian Dubos, Dezhi Wu   +13 more
wiley   +1 more source

MdRLKT1–MdRAX2–MdMKS1 Module Positively Regulating Resistance to Cytospora mali in Apple

Plant Biotechnology Journal, EarlyView.
ABSTRACT Valsa canker (caused by Cytospora mali = Valsa mali. C. mali) is one of the most destructive diseases affecting apple cultivation. The scarcity of natural germplasm resources with high resistance and immunity underscores the importance of exploring plant immune regulation factors of disease‐resistant breeding.
Yanan Tang, Guangyao Li, Yang Li, Yuzhu Wang, Hao Feng, Lili Huang   +5 more
wiley   +1 more source