Results 21 to 30 of about 4,906,436 (344)
Chiral Kinase Inhibitors [PDF]
Current Topics in Medicinal Chemistry, 2011 Small molecule kinase inhibitors are important tools for studying cellular signaling pathways, phenotypes and are, occasionally, useful clinical agents. With stereochemistry pervasive throughout the molecules of life it is no surprise that a single stereocenter can bestow a ligand with distinct binding affinities to various protein targets.
Jian-kang, Jiang +3 more
openaire +2 more sources
Lessons from LIMK1 enzymology and their impact on inhibitor design [PDF]
, 2019 LIM domain kinase 1 (LIMK1) is a key regulator of actin dynamics. It is thereby a potential therapeutic target for the prevention of fragile X syndrome and amyotrophic lateral sclerosis.
Beltrami, A +10 more
core +2 more sources
The Kinase Specificity of Protein Kinase Inhibitor Peptide [PDF]
Frontiers in Pharmacology, 2021 G-protein-coupled-receptor (GPCR) signaling is exquisitely controlled to achieve spatial and temporal specificity. The endogenous protein kinase inhibitor peptide (PKI) confines the spatial and temporal spread of the activity of protein kinase A (PKA), which integrates inputs from three major types of GPCRs.
Yao Chen, Yao Chen, Bernardo L. Sabatini
openaire +4 more sources
Potential role of immunotherapy in advanced non-small-cell lung cancer [PDF]
, 2016 Immuno checkpoint inhibitors have ushered in a new era with respect to the treatment of advanced non-small-cell lung cancer. Many patients are not suitable for treatment with epidermal growth factor receptor tyrosine kinase inhibitors (eg, gefitinib ...
Antoniou, Georgios +4 more
core +3 more sources
Nonspecific, Reversible Inhibition of Voltage-Gated Calcium Channels by CaMKII Inhibitor CK59 [PDF]
, 2013 Investigation of kinase-related processes often uses pharmacological inhibition to reveal pathways in which kinases are involved. However, one concern about using such kinase inhibitors is their potential lack of specificity.
Kahrls, Andrew S., Mynlieff, Michelle
core +2 more sources
Targeting the phosphoinositide 3-kinase pathway in hematologic malignancies
Haematologica, 2014 The phosphoinositide 3-kinase pathway represents an important anticancer target because it has been implicated in cancer cell growth, survival, and motility. Recent studies show that PI3K may also play a role in the development of resistance to currently
Elias Jabbour +3 more
doaj +1 more source
Thoracic Cancer, 2021 Background T790M mutation causes resistance to tyrosine kinase inhibitors (TKIs) in approximately 49% of patients with epidermal growth receptor‐mutant non‐small cell lung cancer (NSCLC).
Tadashi Nishimura +12 more
doaj +1 more source
Kinase Inhibitors and Ovarian Cancer [PDF]
Cancers, 2019 Ovarian cancer is fifth in the rankings of cancer deaths among women, and accounts for more deaths than any other gynecological malignancy. Despite some improvement in overall-(OS) and progression-free survival (PFS) following surgery and first-line chemotherapy, there is a need for development of novel and more effective therapeutic strategies.
Periklis Katopodis +9 more
openaire +3 more sources
Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. [PDF]
, 2018 FMS-like Tyrosine Kinase 3 (FLT3) is a clinically validated target for acute myeloid leukemia (AML). Inhibitors targeting FLT3 have been evaluated in clinical studies and have exhibited potential to treat FLT3-driven AML.
Bharate, Jaideep B +8 more
core +2 more sources
Journal for ImmunoTherapy of Cancer, 2019 Background In non-small cell lung cancer, response rates to chemotherapy given after immune checkpoint inhibitors has been reported to be higher compared to response rates to chemotherapy given before immune checkpoint inhibitors.
Rayan Alsuwaigh +4 more
doaj +1 more source