Results 81 to 90 of about 149 (148)

PLK4: Master Regulator of Centriole Duplication and Its Therapeutic Potential

Cytoskeleton, EarlyView.
ABSTRACT Centrosomes catalyze the assembly of a microtubule‐based bipolar spindle, essential for the precise chromosome segregation during cell division. At the center of this process lies Polo‐Like Kinase 4 (PLK4), the master regulator that controls the duplication of the centriolar core to ensure the correct balance of two centrosomes per dividing ...
Muhammad Hamzah, Franz Meitinger, Midori Ohta   +2 more
wiley   +1 more source

First Phosphonic‐Type Inhibitors and Activity‐Based Probes Specific to the O'nyong‐nyong Virus Capsid Protease

ChemMedChem, EarlyView.
The serine capsid protease (CP) catalyzes a crucial process of the alphaviral replication cycle; therefore, it constitutes an interesting therapy target. Herein, the O'nyong‐nyong virus CP profile activity with a specific fluorogenic substrate is analyzed and examines the inhibitory activity of a new series of phosphonic analogs of tryptophan and ...
Karolina Torzyk‐Jurowska, Agnieszka Łupicka‐Słowik, Renata Grzywa, Yuliya Chykunova, Krzysztof Pyrć, Marcin Sieńczyk   +5 more
wiley   +1 more source

Ligand Screening and Discovery Using Cocktail Soaking and Automated Microcrystal Electron Diffraction

ChemMedChem, EarlyView.
Cocktail soaking using single‐crystal X‐ray diffraction allows high‐throughput crystallographic ligand screening against protein targets. However, protein microcrystals are not amenable to this approach. Herein, a workflow integrating cocktail soaking with automated microcrystal electron diffraction to allow rapid ligand screening, structure ...
Jieye Lin, Marc J. Gallenito, Johan Hattne, Tamir Gonen   +3 more
wiley   +1 more source

New Pyridobenothiazolone Derivatives Display Nanomolar Pan‐Serotype Anti‐Dengue Virus Activity

ChemMedChem, EarlyView.
A ligand‐based strategy is employed, starting from hit compound 2, to develop the C‐2 modified pyridobenzothiazolone 19 as a pan‐serotype nanomolar DENV‐1‐4 inhibitor. Investigations of the mechanism reveal the peculiar ability to abolish the infectivity of virions in a second infection.
Tommaso Felicetti, Chin Piaw Gwee, Kitti Wing Ki Chan, Giacomo Pepe, Ciro Milite, Pietro Campiglia, Satoru Watanabe, Muhammad Danial Bin Mohd Mazlan, Stefano Sabatini, Serena Massari, Oriana Tabarrini, Gianluca Sbardella, Subhash G. Vasudevan, Giuseppe Manfroni   +13 more
wiley   +1 more source

Deferasirox Derivatives as Inhibitors of Kallikrein‐Related Peptidases Associated to Neurodegenerative Diseases

ChemMedChem, EarlyView.
Dysregulated proteolysis mediated by kallikrein‐related peptidases (KLKs) and iron overload are involved in the progression of neurodegenerative diseases. Deferasirox, an clinically‐approved iron chelator, and its newly synthesized derivatives have been identified as inhibitors of major central nervous system KLKs with low cytotoxicity and effective ...
Rilès Boumali, Elodie David, Nancy Chaaya, Morane Lucas, Sabrina Aït Amiri, Valérie Lefort, Anthony Nina‐Diogo, Michèle Salmain, Isabelle Petropoulos, Vincent Corcé, Chahrazade El Amri, Candice Botuha   +11 more
wiley   +1 more source

Correction to “Inhibitor Complexes of the Pseudomonas Serine-Carboxyl Proteinase” [PDF]

Biochemistry, 2018
Alexander Wlodawer, Mi Li, Alla Gustchina, Zbigniew Dauter, Kenichi Uchida, Hiroshi Oyama, Nathan E. Goldfarb, Ben M. Dunn, Kohei Oda   +8 more
openaire   +3 more sources

Novel para‐phenylenediamine‐based derivatives as Receptor Tyrosine Kinase‐like Orphan Receptor 1 (ROR1) Inhibitors: An in vitro preliminary characterization

ChemMedChem, Accepted Article.
ROR1 kinase is an underexplored promising target for the development of novel anticancer drugs, being strongly expressed in several cancer cell lines, but poorly in non‐tumor cells. This property, together with the scarce number of molecules effective against ROR1, led us to design and develop a research program aimed to the discovery of new chemical ...
Gerardina Smaldone, Maria Rosaria Miranda, Francesca Di Matteo, Valeria Napolitano, Michela Aliberti, Simona Musella, Veronica Di Sarno, Gianluigi Lauro, Giuseppe Bifulco, Giacomo Pepe, Giovanna Aquino, Mario Felice Tecce, Isabel Maria Gomez-Monterrey, Pietro Campiglia, Carmine Ostacolo, Alessia Bertamino, Vincenzo Vestuto, Tania CIAGLIA   +17 more
wiley   +1 more source

A Phase 1C, Open Label, Single Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of DM199 Administered Intravenously with a Polyvinyl Chloride Bag in Adult Healthy Subjects and Adults Recently Taking Angiotensin‐Converting Enzyme Inhibitors

Clinical Pharmacology in Drug Development, EarlyView.
Abstract This small phase 1C, open‐label, single ascending dose study evaluated the safety, tolerability, and pharmacokinetics (PKs) of DM199, a recombinant form of human tissue kallikrein‐1 (KLK1). A small sample size of both healthy subjects and hypertensive adults recently taking angiotensin‐converting enzyme inhibitors was studied. KLK1 has a known
Michael Giuffre, Annette D. Lista, Nick Paulson, Lorianne Masuoka   +3 more
wiley   +1 more source

Annual Banned‐Substance Review 17th Edition—Analytical Approaches in Human Sports Drug Testing 2023/2024

Drug Testing and Analysis, EarlyView.
Scenarios of drug exposure and administration as well as detection assays for drugs and methods of sports doping published between 2023 and 2024 are critically reviewed and evaluated in context with the Prohibited List 2024 as established by the World Anti‐Doping Agency.
Mario  Thevis, Tiia  Kuuranne, Hans  Geyer   +2 more
wiley   +1 more source

β‐Catenin localization in the ctenophore Mnemiopsis leidyi suggests an ancestral role in cell adhesion and nuclear function

Developmental Dynamics, EarlyView.
Abstract Background The emergence of multicellularity in animals marks a pivotal evolutionary event, which was likely enabled by molecular innovations in the way cells adhere and communicate with one another. β‐Catenin is significant to this transition due to its dual role as both a structural component in the cadherin–catenin complex and as a ...
Brian M. Walters, Lucas J. Guttieres, Mayline Goëb, Stanley J. Marjenberg, Mark Q. Martindale, Athula H. Wikramanayake   +5 more
wiley   +1 more source