Results 31 to 40 of about 608,807 (260)

Identification of inactive conformation‐selective interleukin‐2‐inducible T‐cell kinase (ITK) inhibitors based on second‐harmonic generation

FEBS Open Bio, 2018
Many clinically approved protein kinase inhibitors stabilize an inactive conformation of their kinase target. Such inhibitors are generally highly selective compared to active conformation inhibitors, and consequently, general methods to identify ...
Yoshiji Hantani, Kiyosei Iio, Rie Hantani, Kayo Umetani, Toshihiro Sato, Tracy Young, Katelyn Connell, Sam Kintz, Joshua Salafsky   +8 more
doaj   +1 more source

Insights into the binding mode of MEK type-III inhibitors. A step towards discovering and designing allosteric kinase inhibitors across the human kinome. [PDF]

PLoS ONE, 2017
Protein kinases are critical drug targets for treating a large variety of human diseases. Type-III kinase inhibitors have attracted increasing attention as highly selective therapeutics.
Zheng Zhao, Lei Xie, Philip E Bourne
doaj   +1 more source

Is inhibition of kinase activity the only therapeutic strategy for LRRK2-associated Parkinson's disease?

BMC Medicine, 2012
Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are a common cause of familial Parkinson's disease (PD). Variation around the LRRK2 locus also contributes to the risk of sporadic PD.
Rudenko Iakov N, Chia Ruth, Cookson Mark R   +2 more
doaj   +1 more source

Targeting mTOR for cancer therapy

Journal of Hematology & Oncology, 2019
Mechanistic target of rapamycin (mTOR) is a protein kinase regulating cell growth, survival, metabolism, and immunity. mTOR is usually assembled into several complexes such as mTOR complex 1/2 (mTORC1/2).
Hui Hua, Qingbin Kong, Hongying Zhang, Jiao Wang, Ting Luo, Yangfu Jiang   +5 more
doaj   +1 more source

Deactivatable Bisubstrate Inhibitors of Protein Kinases

Molecules, 2022
Bivalent ligands, including bisubstrate inhibitors, are conjugates of pharmacophores, which simultaneously target two binding sites of the biomolecule. Such structures offer attainable means for the development of compounds whose ability to bind to the biological target could be modulated by an external trigger.
Tanel Sõrmus, Darja Lavogina, Erki Enkvist, Asko Uri, Kaido Viht   +4 more
openaire   +3 more sources

Involvement of different protein kinases and phospholipases A2 in phorbol ester (TPA)-induced arachidonic acid liberation in bovine platelets

Mediators of Inflammation, 2000
The effect of various phospholipase A2 and protein kinase inhibitors on the arachidonic acid liberation in bovine platelets induced by the protein kinase activator 12-O-tetradecanoylphorbol–13-acetate (TPA) was studied.
M. Lehr, K. Griessbach
doaj   +1 more source

Kinase-targeted cancer therapies: progress, challenges and future directions

Molecular Cancer, 2018
The human genome encodes 538 protein kinases that transfer a γ-phosphate group from ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with human cancer initiation and progression.
Khushwant S. Bhullar, Naiara Orrego Lagarón, Eileen M. McGowan, Indu Parmar, Amitabh Jha, Basil P. Hubbard, H. P. Vasantha Rupasinghe   +6 more
doaj   +1 more source

DeepPurpose-based drug discovery in chondrosarcoma

Chinese Journal of Plastic and Reconstructive Surgery, 2022
Background: Chondrosarcoma (CS) is the second most common primary bone tumor, accounting for approximately 30% of all malignant bone tumors. Unfortunately, the efficacy of currently available drug therapies is limited.
Jianrui Li, Mingyue Shi, Zhiwei Chen, Yuyan Pan   +3 more
doaj   +1 more source

Development of inhibitors for protein tyrosine kinases [PDF]

Oncogene, 2000
In the last 5 years, through combinatorial chemistry, high-throughput screening, computational chemistry, and traditional medicinal chemistry, numerous inhibitors for various protein tyrosine kinases (PTKs) have been developed. The majority of these compounds are small molecules that compete at the ATP binding site of the catalytic domain of the ...
F A, Al-Obeidi, K S, Lam
openaire   +2 more sources

Organoids in pediatric cancer research

FEBS Letters, EarlyView.
Organoid technology has revolutionized cancer research, yet its application in pediatric oncology remains limited. Recent advances have enabled the development of pediatric tumor organoids, offering new insights into disease biology, treatment response, and interactions with the tumor microenvironment.
Carla Ríos Arceo, Jarno Drost
wiley   +1 more source