Results 241 to 250 of about 692,160 (279)

Allosteric Integrase Inhibitors

, 2016
In the recent years, integrase (IN) has emerged as an important new target for the development of anti-HIV-1 agents. The enzyme is involved in a key stage of the retroviral replicative cycle, and interacts with a range of cellular co-factors.
Victoria Hann, Peter Dawson, Mark Ashton
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Covalent‐Allosteric Kinase Inhibitors

Angewandte Chemie International Edition, 2015
AbstractTargeting and stabilizing distinct kinase conformations is an instrumental strategy for dissecting conformation‐dependent signaling of protein kinases. Herein the structure‐based design, synthesis, and evaluation of pleckstrin homology (PH) domain‐dependent covalent‐allosteric inhibitors (CAIs) of the kinase Akt is reported.
Weisner, Jörn, Gontla, Rajesh, van der Westhuizen, Leandi, Oeck, Sebastian, Ketzer, Julia, Janning, Petra, Richters, André, Mühlenberg, Thomas, Fang, Zhizhou, Taher, Abu, Jendrossek, Verena, Pelly, Stephen C, Bauer, Sebastian, van Otterlo, Willem A L, Rauh, Daniel   +14 more
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Selective Detection of Allosteric Phosphatase Inhibitors

Journal of the American Chemical Society, 2013
Normal cellular function, such as signal transduction, is largely controlled by the reversible phosphorylation of cellular proteins catalyzed by two major classes of enzymes, kinases and phosphatases. A misbalance in this complex and dynamic interplay leads to a variety of severe diseases, such as cancer, inflammation, or autoimmune diseases.
Schneider, R., Beumer, C., Simard, J., Grütter, C., Rauh, D.   +4 more
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Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase

Journal of Medicinal Chemistry, 2020
Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in turn, plays a key role in regulating protein translation of selected mRNA that are associated with the synthesis of oncoproteins,
Yuta Tanaka, Osamu Kurasawa, Akihiro Yokota, Michael G. Klein, Koji Ono, Bunnai Saito, Shigemitsu Matsumoto, Masanori Okaniwa, Geza Ambrus-Aikelin, Daisuke Morishita, Satoshi Kitazawa, Noriko Uchiyama, Kazumasa Ogawa, Hiromichi Kimura, Shinichi Imamura   +14 more
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A new screening assay for allosteric inhibitors of cSrc

Nature Chemical Biology, 2009
Targeting kinases outside the highly conserved ATP pocket is thought to be a promising strategy for overcoming bottlenecks in kinase inhibitor research, such as limited selectivity and drug resistance. Here we report the development and application of a direct binding assay to detect small molecules that stabilize the inactive conformation of the ...
Simard, Jeffrey R., Klüter, Sabine, Grütter, Christian, Getlik, Matthäus, Rabiller, Matthias, Rode, Haridas B., Rauh, Daniel   +6 more
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Allosteric Lariat Peptide Inhibitors of Abl Kinase

ChemBioChem, 2013
Going against tradition: although most kinase inhibitors are ATP competitive, lariat peptides inhibit Abl kinase activity in an ATP-uncompetitive manner. Further, lariat peptides discriminated Src family kinases, and recognize the allosteric region that lies adjacent to the ATP binding pocket in the Abl kinase catalytic cleft.
V M, Bharathikumar, Kris, Barreto, John F, Decoteau, C Ronald, Geyer   +3 more
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Discovery of USP7 small-molecule allosteric inhibitors

Bioorganic & Medicinal Chemistry Letters, 2020
Ubiquitin specific protease-7 (USP7) is considered an attractive target for cancer therapy by promoting degradation of the tumor suppressor p53 and negatively affecting the immune response to tumors. However, the development of selective non-covalent USP7 inhibitors has proven challenging.
Olof Engström, Oscar Belda, Mari Kullman-Magnusson, Mikaela Rapp, Kerstin Böhm, Ralf Paul, Ian Henderson, Dean Derbyshire, Sofia Karlström, Kevin E.B. Parkes, Hongtao Zhao   +10 more
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Discovery and characterization of novel allosteric FAK inhibitors

European Journal of Medicinal Chemistry, 2013
Focal adhesion kinase (FAK) regulates cell survival and proliferation pathways. Here we report the discovery of a highly selective series of 1,5-dihydropyrazolo[4,3-c][2,1]benzothiazines that demonstrate a novel mode of allosteric inhibition of FAK.
Misa, Iwatani, Hidehisa, Iwata, Atsutoshi, Okabe, Robert J, Skene, Naoki, Tomita, Yoko, Hayashi, Yoshio, Aramaki, David J, Hosfield, Akira, Hori, Atsuo, Baba, Hiroshi, Miki   +10 more
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Allosteric Site Inhibitors for Caspases

Science's STKE, 2004
The active sites of proteins with enzymatic activity are not always suitable for drug targeting. Hardy et al. report the application of a method called "Tethering" to identify an allosteric site inhibitor on the executioner caspases, caspase-3. Tethering, a commercial method, uses reversible disulfide bond formation
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Development of thioquinazolinones, allosteric Chk1 kinase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2009
A high throughput screening campaign was designed to identify allosteric inhibitors of Chk1 kinase by testing compounds at high concentration. Activity was then observed at K(m) for ATP and at near-physiological concentrations of ATP. This strategy led to the discovery of a non-ATP competitive thioquinazolinone series which was optimized for potency ...
Antonella, Converso, Timothy, Hartingh, Robert M, Garbaccio, Edward, Tasber, Keith, Rickert, Mark E, Fraley, Youwei, Yan, Constantine, Kreatsoulas, Steve, Stirdivant, Bob, Drakas, Eileen S, Walsh, Kelly, Hamilton, Carolyn A, Buser, Xianzhi, Mao, Marc T, Abrams, Stephen C, Beck, Weikang, Tao, Rob, Lobell, Laura, Sepp-Lorenzino, Joan, Zugay-Murphy, Vinod, Sardana, Sanjeev K, Munshi, Sylvie Marie, Jezequel-Sur, Paul D, Zuck, George D, Hartman   +24 more
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