Results 81 to 90 of about 4,906,436 (344)

Systemic Administration of a Brain Permeable Cdk5 Inhibitor Alters Neurobehavior

Frontiers in Pharmacology, 2022
Cyclin-dependent kinase 5 (Cdk5) is a crucial regulator of neuronal signal transduction. Cdk5 activity is implicated in various neuropsychiatric and neurodegenerative conditions such as stress, anxiety, depression, addiction, Alzheimer’s disease, and ...
Alan Umfress, Sarbjit Singh, Kevin J. Ryan, Ayanabha Chakraborti, Florian Plattner, Yogesh Sonawane, Jayapal Reddy Mallareddy, Edward P. Acosta, Amarnath Natarajan, James A. Bibb, James A. Bibb, James A. Bibb   +11 more
doaj   +1 more source

Phosphatidylinositol 4‐kinase as a target of pathogens—friend or foe?

FEBS Letters, EarlyView.
This graphical summary illustrates the roles of phosphatidylinositol 4‐kinases (PI4Ks). PI4Ks regulate key cellular processes and can be hijacked by pathogens, such as viruses, bacteria and parasites, to support their intracellular replication. Their dual role as essential host enzymes and pathogen cofactors makes them promising drug targets.
Ana C. Mendes, Guilherme M. Azevedo, Amanda P. Barcellos, Diana Bahia   +3 more
wiley   +1 more source

Prolonged and tunable residence time using reversible covalent kinase inhibitors. [PDF]

, 2015
Drugs with prolonged on-target residence times often show superior efficacy, yet general strategies for optimizing drug-target residence time are lacking.
Angelina Bisconte, Dane E. Karr, Danny Tam, David Finkle, David G. Loughhead, David M. Goldstein, Erik Verner, J. Hill, J. Michael Bradshaw, Jack Taunton, Jens Oliver Funk, Jesse M. Mcfarl, Jin Shu, Ken A. Brameld, Mary E, Philip A. Nunn, Principia Biopharma, Sergei Romanov, Timothy D. Owens, Tony Ton, Vaishali Patel, Vernon T. Phan, Ville O. Paavilainen, Xiaoyan Li   +23 more
core  

New targets for resolution of airway remodeling in obstructive lung diseases. [PDF]

, 2018
Airway remodeling (AR) is a progressive pathological feature of the obstructive lung diseases, including asthma and chronic obstructive pulmonary disease (COPD).
Deshpande, Deepak A., Nayak, Ajay P., Penn, Raymond B   +2 more
core   +2 more sources

Factors associated with efficacy of first-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer

Tumor Biology, 2017
The finding of epidermal growth factor receptor tyrosine kinase inhibitors, which reflects a classical process of translational research, is a critical milestone for non-small-cell lung cancer treatment.
Shaohua Cui, Liyan Jiang
doaj   +1 more source

A physicochemical descriptor-based scoring scheme for effective and rapid filtering of kinase-like chemical space

Journal of Cheminformatics, 2012
Background The current chemical space of known small molecules is estimated to exceed 1060 structures. Though the largest physical compound repositories contain only a few tens of millions of unique compounds, virtual screening of databases of this size ...
Singh Narender, Sun Hongmao, Chaudhury Sidhartha, AbdulHameed Mohamed, Wallqvist Anders, Tawa Gregory   +5 more
doaj   +1 more source

TYROSINE KINASE INHIBITORS AND PREGNANCY

Mediterranean Journal of Hematology and Infectious Diseases, 2014
The management of patients with chronic myeloid leukemia (CML) during pregnancy has became recently a matter of continuous debate.  The introduction of the Tyrosine Kinase Inhibitors (TKIs) in clinical practice has dramatically changed the prognosis of CML patients.
Elisabetta Abruzzese, Malgorzata Monika Trawinska, Paolo De Fabritiis, Alessio Pio Perrotti   +3 more
openaire   +4 more sources

Protein pyrophosphorylation by inositol pyrophosphates — detection, function, and regulation

FEBS Letters, EarlyView.
Protein pyrophosphorylation is an unusual signaling mechanism that was discovered two decades ago. It can be driven by inositol pyrophosphate messengers and influences various cellular processes. Herein, we summarize the research progress and challenges of this field, covering pathways found to be regulated by this posttranslational modification as ...
Sarah Lampe, Tanmay Kumar Mohanty, Rashna Bhandari, Dorothea Fiedler   +3 more
wiley   +1 more source

The dynamic switch mechanism that leads to activation of LRRK2 is embedded in the DFGψ motif in the kinase domain. [PDF]

, 2019
Leucine-rich repeat kinase 2 (LRRK2) is a large multidomain protein, and LRRK2 mutants are recognized risk factors for Parkinson's disease (PD). Although the precise mechanisms that control LRRK2 regulation and function are unclear, the importance of the
Boassa, Daniela, Ellisman, Mark H, Herberg, Friedrich W, Knape, Matthias J, Kornev, Alexandr P, Mumdey, Natascha, Schmidt, Sven H, Taylor, Susan S   +7 more
core  

Therapeutic choices in patients with Ph-Positive chronic myelogenous leukemia in Mexico in the era of tyrosine kinase inhibitors: stem cell transplantation or tyrosine kinase inhibitors? Fifteen years later

Revista de Investigación Clínica
Background: Chronic myelogenous leukemia is a neoplastic proliferation of the granulocytic series. In Mexico, chronic myelogenous leukemia accounts for approximately 10% of all leukemias.
Max Robles-Nasta, Daniela Sánchez-Bonilla, Moises M. Gallardo-Pérez, Edgar J. Hernández-Flores, Merittzel A. Montes-Robles, María de L. Pastelín-Martínez, Juan C. Olivares-Gazca, Guillermo J. Ruiz-Delgado, Guillermo J. Ruiz-Argüelles   +8 more
doaj   +1 more source