Results 101 to 110 of about 401,752 (293)

Diversity of Penicillin-binding Proteins [PDF]

Journal of Biological Chemistry, 2007
Antibiotic-resistant Staphylococcus aureus is a major concern to public health. Methicillin-resistant S. aureus strains are completely resistant to all β-lactams antibiotics. One of the main factors involved in methicillin resistance in S. aureus is the penicillin-binding protein, PBP2a.
Xin Fan, Yuhong Liu, Daryl Smith, Lars Konermann, K. W. Michael Siu, Dasantila Golemi-Kotra   +5 more
openaire   +1 more source

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

Molecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka, Wioleta Cieślik, Wojciech Płaziński, Katarzyna Stępnik, Anna Boguszewska‐Czubara, Elżbieta Kot, Robert Musioł, Mateusz Jasica, Anna Mrozek‐Wilczkiewicz, Katarzyna Malarz   +9 more
wiley   +1 more source

Antibiotic Discovery with Synthetic Fermentation: Library Assembly, Phenotypic Screening, and Mechanism of Action of Beta-Peptides Targeting Penicillin-Binding Proteins

, 2019
In analogy to biosynthetic pathways leading to bioactive natural products, synthetic fermentation generates mixtures of molecules from simple building blocks under aqueous, biocompatible conditions, allowing for the resulting cultures to be directly ...
Satomi, Shimura, Bernd, Wollscheid, Anika, Koetemann, Iain A., Stepek, Trung, Cao, Jeffrey, Bode   +5 more
core   +1 more source

Reactivity of Penicillin-Binding Proteins with Peptidoglycan-Mimetic β-Lactams:  What's Wrong with These Enzymes?^†

, 2016
β-Lactams exert their antibiotic action through their inhibition of bacterial dd-peptidases (penicillin-binding proteins). Bacteria, in general, carry several such enzymes localized on the outside of their cell membrane to catalyze the final step in cell
Helen R. Josephine (1265070), Paulette Charlier (569617), Robert A. Nicholas (134565), Christopher Davies (67862), R. F. Pratt (1340403)   +4 more
core   +2 more sources

Patient therapy outcome modeling in cancer organoids is improved by cancer‐associated fibroblasts and organoid assembly convolution

Molecular Oncology, EarlyView.
Patient‐derived organoids (PDOs) from pancreatic, colorectal, and gastric cancers were used to evaluate standard and experimental therapies. Incorporating cancer‐associated fibroblasts (CAFs) into organoid cultures improved patient therapy outcome prediction.
Marcin Grochowski, Liudmyla Dolinchuk, Michał Jerzak, Albert Gandurski, Tomasz Grochowski, Weronika Wojtyś, Maciej Zadrożny, Wojciech Kaźmierczak, Małgorzata Lenarcik, Marta Matejak‐Górska, Radosław Samsel, Tomasz Olesiński, Dawid Walerych   +12 more
wiley   +1 more source

Characterisation of ATP-Dependent Mur Ligases Involved in the Biogenesis of Cell Wall Peptidoglycan in Mycobacterium tuberculosis [PDF]

, 2013
ATP-dependent Mur ligases (Mur synthetases) play essential roles in the biosynthesis of cell wall peptidoglycan (PG) as they catalyze the ligation of key amino acid residues to the stem peptide at the expense of ATP hydrolysis, thus representing ...
Nicholas H Keep, Munshi, T, Sanjib Bhakta (106475), Bhakta, S, Gupta, A, Gibbons, S., Simon Gibbons (391868), Nicholas H. Keep (392673), Antima Gupta, Keep, Nicholas H., Gibbons, Simon, Bhakta, Sanjib, Evangelopoulos, Dimitrios, Juan David Guzman (392672), Gibbons, S, Simon Gibbons, Dimitrios Evangelopoulos (392671), Tulika Munshi (392669), Antima Gupta (392670), Juan David Guzman, Evangelopoulos, D, Guzman, Juan David, Gupta, Antima, Dimitrios Evangelopoulos, Munshi, Tulika, Sanjib Bhakta, Keep, NH, Guzman, Juan D., Guzman, JD, Tulika Munshi   +29 more
core   +1 more source

PAK1 activation drives divergent resistance mechanisms to aromatase inhibition and tamoxifen in a luminal: A breast cancer model

Molecular Oncology, EarlyView.
Breast cancer remains a major cause of cancer death in women, frequently developing endocrine therapy resistance. This study demonstrates that upregulated p21‐activated kinase 1 (PAK1) activity drives resistance to tamoxifen and long‐term estrogen deprivation in ER+ breast cancer models.
Luisa Schwarzmüller, Janina Müller, Efstathios‐Iason Vlachavas, Lukas Beumers, Lena Fleischhacker, Sara Burmester, Angelika Wörner, Sabine Karolus, Dominic Helm, Cindy Körner, Stefan Wiemann   +10 more
wiley   +1 more source

Penicillin-binding proteins: evergreen drug targets.

, 2014
peer reviewedThe penicillin-binding proteins (PBPs) are well known targets for the beta-lactam antibiotics. They continue to be a focus of interest for pharmaceutical design, as exemplified by the number of new agents under clinical investigation as well
Page, Malcolm G. P., Frère, Jean-Marie
core   +1 more source

Inhibition of cyclin‐dependent kinases 12/13 using CT7439 as a treatment for colorectal cancer with CDK12 upregulation

Molecular Oncology, EarlyView.
The proposed mechanism of action for the CDK12/13 inhibitor and cyclin K degrader, CT7439. CDK12/13 inhibition interrupts transcription elongation, leading to increased DNA damage that results in cell death. This agent is a potentially novel treatment option for patients with colorectal cancer. Created in BioRender. Cyclin‐dependent kinase (CDK) 12 and
Wylie K. Watlington, Divya L. Dayanidhi, Mohammad Zokaasadi, John B. Mantyh, Pelumi D. Olawuni, Gabrielle Rupprecht, Jeremy M. Force, Shannon McCall, Ashwani K. Bahl, David S. Hsu, Jason A. Somarelli   +10 more
wiley   +1 more source

ZW4864‐mediated inhibition of the β‐catenin/BCL9/BCL9L complex reveals therapeutic potential in bladder cancer

Molecular Oncology, EarlyView.
BCL9 and BCL9L drive bladder cancer progression by enhancing β‐catenin signaling, promoting proliferation, migration, invasion, and organoid growth. Genetic depletion of BCL9(L) suppresses malignant phenotypes, while pharmacological disruption of the β‐catenin/BCL9(L) complex with ZW4864 inhibits canonical Wnt signaling and tumor‐associated cellular ...
Roland Kotolloshi, Mandy Berndt‐Paetz, Eileen Lerner, Gregoire Najjar, Anca Azoitei, Krishna Pal Singh, Shailendra Kumar Gupta, Olaf Wolkenhauer, Cagatay Günes, Otmar Huber, Marc‐Oliver Grimm, Daniel Steinbach   +11 more
wiley   +1 more source