Results 181 to 190 of about 132,691 (210)

Über die Bindungsstelle hinausgedacht: Ein sich selbsteinkapselnder Kinase‐Inhibitor modelliert seine Bindetasche und erzielt so Selektivität

Angewandte Chemie, EarlyView.
Um außergewöhnlich wirksame Wirkstoffe zu entwickeln, ist es erforderlich, über die Bindungsstelle hinaus zu denken. Diese Arbeit zeigt, dass die auf den ersten Blick kontraintuitive Adressierung einer konservierten Region der Kinase zu einer hochselektiven Bindung führen kann.
Nico J. Seidler, Monica R. MacDonald, Athina A. Moschopoulou, Sahba Cunningham, Tess M. Weber, Nader N. Nasief, Lorenz Mayer, Frederik W. Hacker, Ekaterina Hermann, Mareike B. Möllers, Yuliia Skliarenko, Tahereh Damghani, Abid N. Manzar, Kaly S. Lin, Ramona Rudalska, Marcia I. Goettert, Lars Zender, Daniel Dauch, Michael Forster, Stefan A. Laufer, David E. Heppner   +20 more
wiley   +1 more source

Click‐Spaltung quartärer Anilinium‐Tetrazine ermöglicht Kaskadenaufbau multifunktioneller biomolekularer Gerüste

Angewandte Chemie, EarlyView.
Die Click‐Chemie hat sich von dem Aufbau kovalenter Bindungen hin zum Spalten von Bindungen weiterentwickelt. Hier wird über einen Kaskaden‐Aufbau berichtet, der diese Verfahren kombiniert, um multifunktionale biomolekulare Gerüste in einer modularen Ein‐Topf‐Reaktion aufzubauen.
Markus Staudt, Christian B. M. Poulie, Andreas Löffler, Peter R. Meinig, Riley J. Deutsch‐Williams, Barbara Herrmann, Ralph Weissleder, Hannes Mikula, Jonathan C. T. Carlson, Matthias M. Herth   +9 more
wiley   +1 more source

Thinking Outside the Binding Site: A Self‐Encapsulating Kinase Inhibitor Remodels Its Pocket to Achieve Selectivity

Angewandte Chemie International Edition, EarlyView.
To make exceptionally effective drugs, thinking “outside the binding site” is required. This work reveals that counterintuitive targeting of a kinase‐conserved region can lead to highly selective binding. Inhibitor discovery coupled to x‐ray crystallography shows that a network of noncanonical interactions and long‐range effects of distant unique amino
Nico J. Seidler, Monica R. MacDonald, Athina A. Moschopoulou, Sahba Cunningham, Tess M. Weber, Nader N. Nasief, Lorenz Mayer, Frederik W. Hacker, Ekaterina Hermann, Mareike B. Möllers, Yuliia Skliarenko, Tahereh Damghani, Abid N. Manzar, Kaly S. Lin, Ramona Rudalska, Marcia I. Goettert, Lars Zender, Daniel Dauch, Michael Forster, Stefan A. Laufer, David E. Heppner   +20 more
wiley   +1 more source

Click‐to‐Release Reactivity of Quaternary Anilinium Tetrazines Enables Cascade Assembly of Multifunctional Biomolecular Scaffolds

Angewandte Chemie International Edition, EarlyView.
Click chemistry has evolved from making covalent connections to also breaking bonds. Here, a cascade assembly is reported that combines these maneuvers to build multifunctional biomolecular scaffolds in a modular one‐pot reaction. The unifying azide release‐tetrazine hub clicks with a trans‐cyclooctene tag, rapidly liberates N,N‐dimethylaniline to ...
Markus Staudt, Christian B. M. Poulie, Andreas Löffler, Peter R. Meinig, Riley J. Deutsch‐Williams, Barbara Herrmann, Ralph Weissleder, Hannes Mikula, Jonathan C. T. Carlson, Matthias M. Herth   +9 more
wiley   +1 more source

Recent Advances in Virus–Host Interactions, Antiviral Bioactive Compounds, and Breeding for Disease Resistance of Porcine Epidemic Diarrhea Virus

Animal Research and One Health, EarlyView.
Basic research on the PEDV infection cycle and virus–host interactions advances the development of anti‐PEDV drugs and disease‐resistant breeding and helps strengthen disease prevention and control while reducing economic losses in the swine industry.
Heyong Wu, Aosi Qi, Shuyu Zhong, Haozhen Du, Shimeng Guo, Hongsheng Ouyang, Hongming Yuan, Daxin Pang, Zicong Xie   +8 more
wiley   +1 more source

Modulation of Animal Gut Health by Milk Oligosaccharide

Animal Research and One Health, EarlyView.
This review summarizes the composition and structural characteristics of MOs across different mammalian species, and elucidates their roles and mechanisms in maintaining intestinal homeostasis by regulating gut microbiome and enhancing intestinal chemical, physical and immune barriers.
Ningtao Chen, Nana Jing, Shiyu Tao, Mingyue Fei, Wentao Lv, Hua Yang, Yingping Xiao, Haiqin Wu   +7 more
wiley   +1 more source

Kidney Hematopoietic Stem and Progenitor Cells Contribute to Myeloid Development and Pathology in Lupus Nephritis

Arthritis &Rheumatology, EarlyView.
Objective The hematopoietic system maintains homeostasis by balancing myeloid and lymphoid cell production in the bone marrow (BM). In response to increased hematopoietic demand, extramedullary hematopoiesis (EMH) may occur in nonlymphoid organs. We investigated the role of EMH and kidney‐resident hematopoietic stem and progenitor cells (HSPCs) in ...
Hansol Yi, Seyoung Jung, Jeong Ho Joo, Young‐Eun Kim, Heounjeong Go, Yong‐Gil Kim, Chang‐Keun Lee, Bin Yoo, Jeong Seok Lee, Seokchan Hong   +9 more
wiley   +1 more source

Integrated Clinical and Proteomic Profiling of CD19 Chimeric Antigen Receptor T Cell Therapy in Progressive Systemic Sclerosis

Arthritis &Rheumatology, EarlyView.
Objective To characterize the clinical, immunologic, and proteomic changes associated with CD19 chimeric antigen receptor T cell therapy in patients with progressive systemic sclerosis (SSc). Methods Patients with progressive SSc received CD19 chimeric antigen receptor (CAR)‐T cell therapy and were observed longitudinally for safety, clinical efficacy,
Chenhan Jia, Wanyi Lin, Zhangyi Zhao, Fenglin Wu, Chaoyu Gu, Yuankai Sun, Zhe Ding, Chang Wei, Xinyu Li, Cuiwei Xie, Peng Xia, Zhen Xia, Xuesong Liu, Shaoying Yang, Chunyan Zhang, Hanlin Yin, Liangjing Lu   +16 more
wiley   +1 more source

Efficacy and Safety of Nanoencapsulated Sirolimus Plus Pegadricase: Results From the Randomized, Placebo‐Controlled Phase 3 Trials

Arthritis &Rheumatology, EarlyView.
Objective DISSOLVE I and II examined the efficacy and safety of nanoencapsulated sirolimus (NAS) plus pegadricase (NASP) in patients with uncontrolled gout (UG). Methods In these double‐blind, placebo‐controlled Phase 3 trials of NASP, patients were randomized 1:1:1 to infusions of high‐dose (HD) or low‐dose (LD) NAS plus pegadricase (HD NASP, LD NASP,
Herbert S. B. Baraf, Puja P. Khanna, Milan Petronijevic, Mamuka Lortkipanidze, Anand Patel, Kwabena Ayesu, Michael H. Pillinger, Atul Singhal, Joanna Sobierska, Jacquie Christie, Peter Traber, Rehan Azeem, Wesley DeHaan, Hugues Santin‐Janin, Bhavisha Desai, Alan Kivitz   +15 more
wiley   +1 more source

Exploring the Potential of Cluster Analysis in Identifying Disease Phenotypes in Calcium Pyrophosphate Deposition: Moving From Intuition to Insight

Arthritis &Rheumatology, EarlyView.
Objective Calcium pyrophosphate deposition (CPPD) disease is a heterogeneous condition and is frequently misdiagnosed due to the different clinical presentations and variable disease progression. Aim of this study is to identify clinical phenotypes of CPPD disease by integrating real‐world data from two data sets. Methods Data from the COLCHICORT trial
Greta Pellegrino, Laurène Norberciak, Silvia Sirotti, Abhishek Abhishek, Mariano Andrès, Edoardo Cipolletta, Julien Damart, Renaud Desbarbieux, Pilar Diez, Vincent Ducoulombier, Hang‐Korng Ea, Emilio Filippucci, Charlotte Jauffret, Augustin Latourte, Jean‐Guillaume Letarouilly, Sébastien Ottaviani, Laura Pezzoni, Pascal Richette, Pierre Robinet, Georgios Filippou, Tristan Pascart   +20 more
wiley   +1 more source