Results 71 to 80 of about 9,317 (205)

Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation. [PDF]

, 2015
Constitutively active mutant KRas displays a reduced rate of GTP hydrolysis via both intrinsic and GTPase-activating protein-catalyzed mechanisms, resulting in the perpetual activation of Ras pathways.
Alexander L. Breeze, Boriack-Sjodin P. A., Bosch J., Burns M. C., Christine Chresta, Claire Brassington, Congreve M., Edfeldt F. N., Gail Wrigley, Gary Fairley, Giordanetto F., Haigh J. A., Henchey L. K., Jason G. Kettle, Johnson D. S., Jon J. G. Winter, Jonathan Tart, Julie A. Tucker, Kalgutkar A. S., Karnoub A. E., Kathman S. G., Kevin Blades, Kevin Embrey, Lim S. M., Loredana Spadola, M. Raymond V. Finlay, MacFaul P. A., Mah R., Malcolm Anderson, Margarit M. S., Maurer T., Ostrem J. M., Paul Faulder, Paula Perkins, Peyroche A., Potashman M. H., Renault L., Ross Overman, Rusconi P., S. Joe Patel, Shutes A., Spiegel J., Sun Q., Thorsten Nowak, Ward R. A., Ward R. A.   +45 more
core   +1 more source

Discovery of a novel PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy

Journal of Enzyme Inhibition and Medicinal Chemistry
PLK1 is essential for cell cycle regulation and proliferation, and its elevated expression in prostate cancer is associated with high tumour grade. Therefore, PLK1 inhibition is considered a promising strategy for the treatment of prostate cancer.
Zhen Xu, Lixia Guan, Yuting Wang, Miao-Miao Niu, Yashi Ruan, Cen Xu, Li Yang   +6 more
doaj   +1 more source

Synthesis of Bispecific Conjugates by ADP‐Ribosyl Cyclases

Advanced Science, EarlyView.
Genetic fusion of a CD38 enzymatic domain to antibody scaffolds allows site‐specific conjugation of small‐molecule ligands. Using this approach, a PSMA ligand DUPA is conjugated with an anti‐human CD3 Fab antibody. The resulting bispecific anti‐CD3‐DUPA conjugate facilitates recruitment and activation of cytotoxic T cells against PSMA‐expressing ...
Sunny H. Kim, Arshad J. Ansari, Lei Zhang, Guoyun Kao, Thuc Oanh Hoang, Zeyu Zhang, Srinivasarao Singireddi, Benjamin B. Katz, Yong Zhang   +8 more
wiley   +1 more source

Protective effect of different anti-rabies virus VHH constructs against rabies disease in mice. [PDF]

PLoS ONE, 2014
Rabies virus causes lethal brain infection in about 61000 people per year. Each year, tens of thousands of people receive anti-rabies prophylaxis with plasma-derived immunoglobulins and vaccine soon after exposure. Anti-rabies immunoglobulins are however
Sanne Terryn, Aurélie Francart, Sophie Lamoral, Anna Hultberg, Heidi Rommelaere, Angela Wittelsberger, Filip Callewaert, Thomas Stohr, Kris Meerschaert, Ingrid Ottevaere, Catelijne Stortelers, Peter Vanlandschoot, Michael Kalai, Steven Van Gucht   +13 more
doaj   +1 more source

Nanozymes Integrated Biochips Toward Smart Detection System

Advanced Science, EarlyView.
This review systematically outlines the integration of nanozymes, biochips, and artificial intelligence (AI) for intelligent biosensing. It details how their convergence enhances signal amplification, enables portable detection, and improves data interpretation.
Dongyu Chen, Wang Zheng, Zhihui Zhang, Shenping Yu, Xinxin Hang, Han Wu, Xiao‐Wei Xiang, Wei Mu, Yanli Jiao, Zaizai Dong, Lingqian Chang   +10 more
wiley   +1 more source

The role of endothelin-1 in pulmonary arterial hypertension. [PDF]

, 2014
Pulmonary arterial hypertension (PAH) is a rare but debilitating disease, which if left untreated rapidly progresses to right ventricular failure and eventually death. In the quest to understand the pathogenesis of this disease differences in the profile,
Chester, AH, Yacoub, MH
core   +1 more source

TR1801‐ADC: a highly potent cMet antibody–drug conjugate with high activity in patient‐derived xenograft models of solid tumors

Molecular Oncology, 2020
cMet is a well‐characterized oncogene that is the target of many drugs including small molecule and biologic pathway inhibitors, and, more recently, antibody–drug conjugates (ADCs).
Marco Gymnopoulos, Oscar Betancourt, Vincent Blot, Ryo Fujita, Diana Galvan, Vincent Lieuw, Sophie Nguyen, Jeanette Snedden, Christine Stewart, Jose Villicana, Jon Wojciak, Eley Wong, Raul Pardo, Neki Patel, Francois D’Hooge, Balakumar Vijayakrishnan, Conor Barry, John A. Hartley, Philip W. Howard, Roland Newman, Julia Coronella   +20 more
doaj   +1 more source

Machine Learning‐Assisted Infectious Disease Detection in Low‐Income Areas: Toward Rapid Triage of Dengue and Zika Virus Using Open‐Source Hardware

Advanced Intelligent Discovery, EarlyView.
This study introduces an affordable machine learning platform for simultaneous dengue and zika detection using fluorine‐doped tin oxide thin films modified with gold nanoparticles and DNA aptamers. Designed for low‐cost, hardware‐limited devices (< $25), the model achieves 95.3% accuracy and uses only 9.4 kB of RAM, demonstrating viability for resource‐
Marina Ribeiro Batistuti Sawazaki, Bassam Bachour Junior, Marcelo Mulato, José Ilton de Oliveira Filho   +3 more
wiley   +1 more source

Analysis of Single Particles of Amyloid Beta and α‐Synuclein With Seeded Amplification for the Diagnosis of Alzheimer's and Parkinson's Disease

Biotechnology and Applied Biochemistry, EarlyView.
ABSTRACT Neurodegenerative diseases, including Alzheimer's disease (AD) and Parkinson's disease (PD), are characterized by the pathological aggregation of specific proteins such as amyloid beta (Aβ) and α‐synuclein, respectively. Early detection of these protein aggregates in biological fluids could facilitate timely diagnosis and therapeutic ...
Alexandra Dybala, Marlene Pils, Oliver Bannach, Gültekin Tamgüney, Detlev Riesner   +4 more
wiley   +1 more source

Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N -Diethyl-Substituted AmidoMoieties [PDF]

, 2012
Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities.
Ajani, Olayinka O., Echeme, Johnbull O, Familoni, Oluwole B, Sujiang, Zheng, Wu, Feipeng   +4 more
core   +5 more sources