Results 41 to 50 of about 920,394 (304)

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

Bacillus anthracis edema factor substrate specificity: evidence for new modes of action [PDF]

, 2012
Since the isolation of Bacillus anthracis exotoxins in the 1960s, the detrimental activity of edema factor (EF) was considered as adenylyl cyclase activity only.
Agrawal, Altaweel, Basler, Bauche, Bell, Benson, Beste, Bock, Bond, Boyd, Bradley, Brown, Burhenne, Carbonetti, Carbonetti, Carson-Walter, Casteel, Christensen, Christensen, Confer, Copsel, Crawford, Crowe, Cunningham, Dalkas, Defer, Deuquet, Ding, Drum, Duesbery, Feld, Firoved, Friedlander, Fu, Fukuhara, Gaion, Gille, Gordon, Göttle, Hammerschmidt, He, Helfman, Hong, Ivarsson, Jernigan, Johnson, Katayama, Katayama, Kaupp, Kintzer, Klimpel, Laine, Larabee, Larabee, Leppla, Liu, Martin Göttle, McDonough, Milne, Mogridge, Mogridge, Newton, Newton, Newton, Newton, Newton, Oncu, O´Brien, Park, Petosa, Pezard, Postea, Puhar, Roland Seifert, Santelli, Scobie, Scobie, Scorpio, Shapiro, Shen, Shirshev, Soelaiman, Stefan Dove, Sun, Tamayo, Taylor, Taylor, Tesmer, Thomas, Tournier, Vitale, Vitale, Vojtova, Yeager, Zong   +94 more
core   +2 more sources

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

New and developing non-adrenoreceptor small molecule drugs for the treatment of asthma [PDF]

, 2017
Introduction: Inhaled corticosteroids (ICS) alone or in combination with an inhaled long-acting beta2-agonist (LABA) are the preferred long-term treatment for adults and adolescents with symptomatic asthma.
Thomson, Neil C.
core   +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

Protein kinase Cδ and c-Abl kinase are required for transforming growth factor β induction of endothelial-mesenchymal transition in vitro. [PDF]

, 2011
OBJECTIVE: The origin of the mesenchymal cells responsible for the intimal fibrosis in systemic sclerosis (SSc) has not been fully identified. The present study was undertaken to investigate whether subendothelial mesenchymal cells may emerge through ...
Jimenez, Sergio A., Li, zhaodong
core   +2 more sources

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

Molecular pathogenesis and targeted therapy of sporadic pancreatic neuroendocrine tumors [PDF]

, 2015
Over the past few years, knowledge regarding the molecular pathology of sporadic pancreatic neuroendocrine tumors (PNETs) has increased substantially, and a number of targeted agents have been tested in clinical trials in this tumor type.
Ahn, Balogh, Bergers, Berruti, Capurso, Capurso, Carew, Castellano, Chamberlain, Chan, Chan, Chen, Clynes, Corbo, Corbo, Couvelard, De Wilde, Di Florio, Di Florio, Di Florio, Fazio, Fendrich, Gaur, Gurung, Han, Heaphy, Heaphy, Hobday, Hopfner, House, Jacinto, Jensen, Jiao, Karnik, Karnik, Komori, Kulke, Laplante, Loewith, Lovejoy, Luzi, Marinoni, Marion-Audibert, Mendel, Meric-Bernstam, Missiaglia, Mocellin, Panzuto, Papouchado, Passacantilli, Perren, Pàez-Ribes, Raymond, Sarbassov, Scoazec, Shah, Shi, Tang, Vinagre, Wang, Yang, Yao, Yuan, Zhang, Zhang   +64 more
core   +1 more source

1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors [PDF]

, 1983
We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to ...
Asquith, Christopher R.M., Godoi, Paulo H., Counago, Rafael M., Laitinen, Tuomo, Scott, John W., Langendorf, Christopher G., Oakhill, Jonathan S., Drewry, David H., Zuercher, William J., Koutentis, Panayiotis A., Willson, Timothy M., Kalogirou, Andreas S.   +11 more
core   +3 more sources