Results 301 to 310 of about 4,906,436 (344)

Benzimidazole Derivatives as Kinase Inhibitors

Current Medicinal Chemistry, 2014
Benzimidazole is a common kinase inhibitor scaffold and benzimidazole-based compounds interact with enzymes by multiple binding modes. In some cases, the benzimidazole acts as part of the hinge-binding motif, in others it has a scaffolding role without evidence for direct hinge binding. Several of these compounds are ATP-competitive inhibitors and show
GARUTI, LAURA, ROBERTI, MARINELLA, BOTTEGONI, GIOVANNI   +2 more
openaire   +4 more sources

Polo-Like Kinases Inhibitors

Current Medicinal Chemistry, 2012
Polo-like kinases (PLKs) are a family of serine/threonine kinases that play crucial roles in multiple stages of mitosis. PLK1 is the most studied member of the family. It is overexpressed in a wide spectrum of cancer types and is a promising target in oncology. Most of PLK1 inhibitors are ATP-competitive.
GARUTI, LAURA, ROBERTI, MARINELLA, BOTTEGONI, GIOVANNI   +2 more
openaire   +3 more sources

Irreversible Protein Kinase Inhibitors

Current Medicinal Chemistry, 2011
Targeting cancer with small molecule irreversible inhibitors of kinases represents an emerging challenge in drug discovery. Irreversible inhibitors bind to kinase active site in a covalent and irreversible form, most frequently by reacting with a nucleophilic cysteine residue, located near the ATP binding pocket.
GARUTI, LAURA, ROBERTI, MARINELLA, BOTTEGONI, GIOVANNI   +2 more
openaire   +4 more sources

Kinase inhibitors

2006
Abstract Normal ceJl growth is a strictly regulated process with well-balanced activity between growth-stimulating and growth-inhibiting factors. In tumour cells, mechanisms of growth control are severely altered, shifting the balance towards uncontrolled proliferation.
Sleijfer, Stefan, Nooter, K (Kees), Verweij, Jaap   +2 more
openaire   +2 more sources

Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.

Journal of Medicinal Chemistry, 2018
Small molecule inhibitors targeting autoimmune and inflammatory processes have been an area of intense focus within academia and industry. Much of this work has been aimed at key kinases operating as central nodes in inflammatory signaling pathways ...
M. Bryan, N. Rajapaksa
semanticscholar   +1 more source

Protein kinase inhibitors in melanoma

Expert Opinion on Pharmacotherapy, 2013
The most commonly mutated oncogene identified to date in melanoma is BRAF (∼ 50%), an upstream mediator of the mitogen-activated protein kinase (MAPK) pathway. Recently, BRAF-kinase inhibitors as well as MEK-kinase inhibitors were introduced into the clinics.Substantial Phase II and III clinical trials were searched in patients with advanced melanoma ...
Thomas K, Eigentler, Friedegund, Meier, Claus, Garbe   +2 more
openaire   +2 more sources

The specificity of JAK3 kinase inhibitors

Blood, 2008
PF-956980 is a selective inhibitor of JAK3, related in structure to CP-690550, a compound being evaluated in clinical trials for rheumatoid arthritis and prevention of allograft rejection. PF-956980 has been evaluated against a panel of 30 kinases, and found to have nanomolar potency against only JAK3. Cellular and whole blood activity of this compound
Paul S, Changelian, Deborah, Moshinsky, Cyrille F, Kuhn, Mark E, Flanagan, Michael J, Munchhof, Thomas M, Harris, David A, Whipple, Jonathan L, Doty, Jianmin, Sun, Craig R, Kent, Kelly S, Magnuson, David G, Perregaux, Perry S, Sawyer, Elizabeth M, Kudlacz   +13 more
openaire   +2 more sources

Triazolopyridazine LRRK2 kinase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2013
Leucine-rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series of [1,2,4]triazolo[4,3-b]pyridazines that are potent against both wild-type and mutant LRRK2 kinase ...
Maurizio, Franzini, Xiaocong M, Ye, Marc, Adler, Danielle L, Aubele, Albert W, Garofalo, Shawn, Gauby, Erich, Goldbach, Gary D, Probst, Kevin P, Quinn, Pam, Santiago, Hing L, Sham, Danny, Tam, Anh, Truong, Zhao, Ren   +13 more
openaire   +2 more sources

Kinase inhibitors for cardiovascular disease

Journal of Molecular and Cellular Cardiology, 2007
Over the last decade, there has been substantial progress toward understanding the pathophysiology and treatment of cardiovascular diseases (CVDs). Elucidating cellular responses to the extracellular environment and signal transduction mechanisms have provided the opportunity to explore novel molecular therapeutic approaches for the treatment of CVDs ...
Rajesh, Kumar, Vivek P, Singh, Kenneth M, Baker   +2 more
openaire   +2 more sources

Neoadjuvant Tyrosine Kinase Inhibitors

Thoracic Surgery Clinics
Neoadjuvant tyrosine kinase inhibitor (TKI) therapy has appeal given the potential for early systemic disease control and tumor downstaging prior to surgery. Until recently, data has have come from smaller series with outcomes from larger trials, including NeoADAURA, ALNEO, and NAUTIKA1, reporting early results. Neoadjuvant use of TKI has been shown to
Gavitt A, Woodard, Ryan J, Kramer, Collin M, Blakely   +2 more
openaire   +2 more sources