Results 81 to 90 of about 2,154,176 (393)

Structure-based design and activity modeling of novel epidermal growth factor receptor kinase inhibitors; an in silico approach

Scientific African, 2020
The development of EGFR kinase inhibitors to treat non-small cell lung cancers is an important medical necessity due to persistent development of resistance by the mutations.
Muhammad Tukur Ibrahim, Adamu Uzairu, Gideon Adamu Shallangwa, Sani Uba   +3 more
doaj   +1 more source

Potential and limitations of PKA/ PKG inhibitors for platelet studies

Platelets, 2022
Cyclic nucleotides (cAMP and cGMP) and corresponding protein kinases, protein kinase A (PKA) and protein kinase G (PKG), are the main intracellular mediators of endothelium-derived platelet inhibitors. Pharmacological PKA/PKG inhibitors are often used to
Valentina Shpakova, Natalia Rukoyatkina, Ulrich Walter, Stepan Gambaryan   +3 more
doaj   +1 more source

Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK)

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Phosphoinositide 3-kinases (PI3K) and phosphoinositide 3-kinase-related protein kinases (PIKK) are two structurally related families of kinases that play vital roles in cell growth and DNA damage repair.
Xueqin Huang, Li You, Eugenie Nepovimova, Miroslav Psotka, David Malinak, Marian Valko, Ladislav Sivak, Jan Korabecny, Zbynek Heger, Vojtech Adam, Qinghua Wu, Kamil Kuca   +11 more
doaj   +1 more source

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, Bullock, Alexander, Canning, P, Chaikuad, A, Chatterjee, D, Knapp, S, Knaus, P, Mathea, S, Preuss, F, Salah, E, Tumber, A   +10 more
core   +2 more sources

Crosstalk between the ribosome quality control‐associated E3 ubiquitin ligases LTN1 and RNF10

FEBS Letters, EarlyView.
Loss of the E3 ligase LTN1, the ubiquitin‐like modifier UFM1, or the deubiquitinating enzyme UFSP2 disrupts endoplasmic reticulum–ribosome quality control (ER‐RQC), a pathway that removes stalled ribosomes and faulty proteins. This disruption may trigger a compensatory response to ER‐RQC defects, including increased expression of the E3 ligase RNF10 ...
Yuxi Huang, Satoshi Hashimoto, Sota Ito, Chisato Kikuguchi, Miho Hoshi, Kiyoshi Yamaguchi, Yoichi Furukawa, Toru Suzuki, Toshifumi Inada   +8 more
wiley   +1 more source

Statistical and Clustering Analysis of Safety Profiles of FDA-Approved Protein Kinase Inhibitors

Applied Sciences
Protein kinases are vital regulators in cell biology, modifying protein functions through phosphorylation. Protein kinase inhibitors (PKIs), which impede these kinases’ activities, have broadened their therapeutic scope from cancer treatment to ...
Ioana Lavinia Radulian, Georgiana Nitulescu, Anca Zanfirescu, George Mihai Nitulescu   +3 more
doaj   +1 more source

Palmitoleic acid prevents palmitic acid-induced macrophage activation and consequent p38 MAPK-mediated-skeletal muscle insulin resistance [PDF]

, 2014
Obesity and saturated fatty acid (SFA) treatment are both associated with skeletal muscle insulin resistance (IR) and increased macrophage infiltration. However, the relative effects of SFA and unsaturated fatty acid (UFA)-activated macrophages on muscle
Aguirre, Antonescu, Bain, Boppart, Cancello, Cao, Carlson, Caroline P. Wheeler-Jones, Cazzolli, Chavez, Cleasby, Coll, Corraliza, de Alvaro, De Paepe, Devaraj, Diamond-Stanic, Dimopoulos, Elgazar-Carmon, Festa, Fink, Fujishiro, Gao, Griffin, Haversen, Hemi, Hevener, Hirabara, Hirosumi, Hoehn, Hommelberg, Hotamisligil, Hotamisligil, Hwang, Kadotani, Karten, Kewalramani, Kuma, Lee, Lee, Liang, Lumeng, Lumeng, Maekawa, Mark E. Cleasby, McCall, Nguyen, Nicola A. Talbot, Patel, Pillon, Pinnick, Plomgaard, Polkinghorne, Prieur, Samokhvalov, Schilling, Sell, Shi, Solinas, Storlien, Suganami, Tardif, Thong, Turner, Uysal, Varma, Weisberg, Yuan   +67 more
core   +2 more sources

Recent developments of protein kinase inhibitors as potential AD therapeutics

Frontiers in Cellular Neuroscience, 2013
Present Alzheimer’s disease (AD) therapies suffer from inefficient effects on AD symptoms like memory or cognition, especially in later states of the disease.
V. Tell, A. Hilgeroth
semanticscholar   +1 more source

Real‐time assay of ribonucleotide reductase activity with a fluorescent RNA aptamer

FEBS Letters, EarlyView.
Ribonucleotide reductases (RNR) synthesize DNA building blocks de novo, making them crucial in DNA replication and drug targeting. FLARE introduces the first single‐tube real‐time coupled RNR assay, which enables isothermal tracking of RNR activity at nanomolar enzyme levels and allows the reconstruction of allosteric regulatory patterns and rapid ...
Jacopo De Capitani, Noemi E. Nwosu, Viktoria Gocke, Müge Kasanmascheff, Hannes Mutschler   +4 more
wiley   +1 more source

Disordered but rhythmic—the role of intrinsic protein disorder in eukaryotic circadian timing

FEBS Letters, EarlyView.
Unstructured domains known as intrinsically disordered regions (IDRs) are present in nearly every part of the eukaryotic core circadian oscillator. IDRs enable many diverse inter‐ and intramolecular interactions that support clock function. IDR conformations are highly tunable by post‐translational modifications and environmental conditions, which ...
Emery T. Usher, Jacqueline F. Pelham
wiley   +1 more source