Results 251 to 260 of about 692,160 (279)

Discovery and Characterization of Allosteric WNK Kinase Inhibitors

ACS Chemical Biology, 2016
Protein kinases are known for their highly conserved adenosine triphosphate (ATP)-binding site, rendering the discovery of selective inhibitors a major challenge. In theory, allosteric inhibitors can achieve high selectivity by targeting less conserved regions of the kinases, often with an added benefit of retaining efficacy under high physiological ...
Ken, Yamada, Ji-Hu, Zhang, Xiaoling, Xie, Juergen, Reinhardt, Amy Qiongshu, Xie, Daniel, LaSala, Darcy, Kohls, David, Yowe, Debra, Burdick, Hajime, Yoshisue, Hiromichi, Wakai, Isabel, Schmidt, Jason, Gunawan, Kayo, Yasoshima, Q Kimberley, Yue, Mitsunori, Kato, Muneto, Mogi, Neeraja, Idamakanti, Natasha, Kreder, Peter, Drueckes, Pramod, Pandey, Toshio, Kawanami, Waanjeng, Huang, Yukiko I, Yagi, Zhan, Deng, Hyi-Man, Park   +25 more
openaire   +2 more sources

Thermodynamic Characterization of Allosteric Glycogen Phosphorylase Inhibitors

Biochemistry, 2008
Glycogen phosphorylase (GP) is a validated target for the treatment of type 2 diabetes. Here we describe highly potent GP inhibitors, AVE5688, AVE2865, and AVE9423. The first two compounds are optimized members of the acyl urea series. The latter represents a novel quinolone class of GP inhibitors, which is introduced in this study. In the enzyme assay,
Anderka, Oliver, Loenze, Petra, Klabunde, Thomas, Dreyer, Matthias K., Defossa, Elisabeth, Wendt, K. Ulrich, Schmoll, Dieter   +6 more
openaire   +2 more sources

Diverse Heterocyclic Scaffolds as Allosteric Inhibitors of AKT

Journal of Medicinal Chemistry, 2012
Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical properties. Examples showed predictable DMPK properties, and one such compound demonstrated pharmacodynamic knockdown of phosphorylation of AKT
Jason G, Kettle, Simon, Brown, Claire, Crafter, Barry R, Davies, Phillippa, Dudley, Gary, Fairley, Paul, Faulder, Shaun, Fillery, Hannah, Greenwood, Janet, Hawkins, Michael, James, Keith, Johnson, Clare D, Lane, Martin, Pass, Jennifer H, Pink, Helen, Plant, Sabina C, Cosulich   +16 more
openaire   +2 more sources

Novel Allosteric Inhibitors of Thrombin

2009
VCU Theses and ...
openaire   +1 more source

Rapid Identification of Novel Allosteric PRC2 Inhibitors

ACS Chemical Biology, 2019
Enhancer of zeste homologue 2 (EZH2), the catalytic subunit of polycomb repressive complex 2 (PRC2), regulates chromatin state and gene expression by methylating histone H3 lysine 27. EZH2 is overexpressed or mutated in various hematological malignancies and solid cancers.
Jon A. Read, Jonathan Tart, Philip B. Rawlins, Clare Gregson, Karen Jones, Ning Gao, Xiahui Zhu, Ron Tomlinson, Erin Code, Tony Cheung, Huawei Chen, Sameer P. Kawatkar, Andy Bloecher, Sharan Bagal, Daniel H. O’Donovan, James Robinson   +15 more
openaire   +2 more sources

Exploring the Allosteric Response of Fascin to Its Inhibitor

The Journal of Physical Chemistry B
Fascin is a major actin-binding protein (ABP) for stabilizing filopodia to support efficient adhesion and migration of cancer cells. Fascin is also highly expressed in metastatic tumors. Disrupting the actin-binding site (ABS) on fascin constitutes a critical approach to hindering tumor metastasis.
Jinmei Pan, Kai Chen, Lirui Lin, Li-Yan Xu, En-Min Li, Geng Dong   +5 more
openaire   +2 more sources

Systematic comparison of competitive and allosteric kinase inhibitors reveals common structural characteristics

European Journal of Medicinal Chemistry, 2021
Filip Miljković, Jürgen Bajorath, Oliver Laufkötter   +2 more
exaly  

Approach in Improving Potency and Selectivity of Kinase Inhibitors: Allosteric Kinase Inhibitors

Mini-Reviews in Medicinal Chemistry, 2021
Zhai Xin
exaly  

ALLOSTERIC INHIBITOR OF WEE1 KINASE

2021
MAHAJAN NUPAM, LAWRENCE NICHOLAS
openaire   +2 more sources

Allosteric Inhibitors of SHP2: An Updated Patent Review (2015-2020)

Current Medicinal Chemistry, 2021
Guilong Zhao, Jingwei Wu, Huan Zhang
exaly