Imidazole: synthesis, functionalization and physicochemical properties of a privileged structure in medicinal chemistry
HV Tolomeu, CAM Fraga - Molecules, 2023 - mdpi.com
Imidazole was first synthesized by Heinrich Debus in 1858 and was obtained by the reaction
of glyoxal and formaldehyde in ammonia, initially called glyoxaline. The current literature …
of glyoxal and formaldehyde in ammonia, initially called glyoxaline. The current literature …
Advances in covalent kinase inhibitors
A Abdeldayem, YS Raouf, SN Constantinescu… - Chemical Society …, 2020 - pubs.rsc.org
Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …
discovery. Covalency affords a unique set of advantages as well as challenges relative to …
Mitogen-activated protein (MAP) kinase pathways: regulation and physiological functions
G Pearson, F Robinson, T Beers Gibson, B Xu… - Endocrine …, 2001 - academic.oup.com
Mitogen-activated protein (MAP) kinases comprise a family of ubiquitous proline-directed,
protein-serine/threonine kinases, which participate in signal transduction pathways that …
protein-serine/threonine kinases, which participate in signal transduction pathways that …
Protein kinases—the major drug targets of the twenty-first century?
P Cohen - Nature reviews Drug discovery, 2002 - nature.com
Protein phosphorylation regulates most aspects of cell life, whereas abnormal
phosphorylation is a cause or consequence of disease. A growing interest in developing …
phosphorylation is a cause or consequence of disease. A growing interest in developing …
Specificity and mechanism of action of some commonly used protein kinase inhibitors
SP Davies, H Reddy, M Caivano… - Biochemical …, 2000 - portlandpress.com
The specificities of 28 commercially available compounds reported to be relatively selective
inhibitors of particular serine/threonine-specific protein kinases have been examined …
inhibitors of particular serine/threonine-specific protein kinases have been examined …
A small molecule–kinase interaction map for clinical kinase inhibitors
MA Fabian, WH Biggs III, DK Treiber, CE Atteridge… - Nature …, 2005 - nature.com
Kinase inhibitors show great promise as a new class of therapeutics. Here we describe an
efficient way to determine kinase inhibitor specificity by measuring binding of small …
efficient way to determine kinase inhibitor specificity by measuring binding of small …
MAPK signalling pathways as molecular targets for anti-inflammatory therapy—from molecular mechanisms to therapeutic benefits
B Kaminska - Biochimica et Biophysica Acta (BBA)-Proteins and …, 2005 - Elsevier
Excessive inflammation is becoming accepted as a critical factor in many human diseases,
including inflammatory and autoimmune disorders, neurodegenerative conditions, infection …
including inflammatory and autoimmune disorders, neurodegenerative conditions, infection …
The p38 signal transduction pathway activation and function
The p38 signalling transduction pathway, a Mitogen-activated protein (MAP) kinase
pathway, plays an essential role in regulating many cellular processes including …
pathway, plays an essential role in regulating many cellular processes including …
Protein kinase inhibitors: insights into drug design from structure
MEM Noble, JA Endicott, LN Johnson - Science, 2004 - science.org
Protein kinases are targets for treatment of a number of diseases. This review focuses on
kinase inhibitors that are in the clinic or in clinical trials and for which structural information is …
kinase inhibitors that are in the clinic or in clinical trials and for which structural information is …
p38 MAP kinases: key signalling molecules as therapeutic targets for inflammatory diseases
S Kumar, J Boehm, JC Lee - Nature reviews Drug discovery, 2003 - nature.com
The p38 MAP kinases are a family of serine/threonine protein kinases that play important
roles in cellular responses to external stress signals. Since their identification about 10 years …
roles in cellular responses to external stress signals. Since their identification about 10 years …