Results 321 to 330 of about 457,473 (371)

Chrysophanol attenuated isoproterenol‐induced cardiac hypertrophy by inhibiting Janus kinase 2/signal transducer and activator of transcription 3 signaling pathway

Cell Biology International, 2019
Cardiac hypertrophy is a common pathological change found in various cardiovascular diseases. Although it has long been recognized as an important risk factor responsible for heart failure, there is still a lack of effective treatments in clinic ...
Hongxin Li, Wei Zhao, Li Wang, Qianqian Luo, Na Yin, Xueyan Lu, Yun Hou, Jingjing Cui, Hongqin Zhang   +8 more
semanticscholar   +1 more source

Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.

Journal of Medicinal Chemistry, 2023
TYK2 is a key mediator of IL12, IL23, and type I interferon signaling, and these cytokines have been implicated in the pathogenesis of multiple inflammatory and autoimmune diseases such as psoriasis, rheumatoid arthritis, lupus, and inflammatory bowel ...
S. Leit, Jeremy Greenwood, S. Carriero, Sayan Mondal, R. Abel, M. Ashwell, Heather S. Blanchette, Nicholas A Boyles, Mark J. Cartwright, A. Collis, Shulu Feng, Phani Ghanakota, G. Harriman, V. Hosagrahara, N. Kaila, Rosanna Kapeller, Salma Rafi, D. Romero, P. Tarantino, Jignesh B. Timaniya, A. Toms, Ron Wester, W. Westlin, Bhaskar Srivastava, Wenyan Miao, P. Tummino, J. McElwee, S. Edmondson, Craig E. Masse   +28 more
semanticscholar   +1 more source

Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold.

Bioorganic & Medicinal Chemistry, 2019
Janus kinases (JAKs) regulate various cancers and immune responses and are targets for the treatment of cancers and immune diseases. A new series of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives were synthesized and optimized by introducing a ...
Yuan Yin, Chengjuan Chen, Ru-Nan Yu, Lei Shu, Tian-tai Zhang, Da-yong Zhang   +5 more
semanticscholar   +1 more source

Janus kinase 2 inhibitors in myeloproliferative disorders

Expert Opinion on Investigational Drugs, 2010
JAK2 is an obligatory kinase for the proliferation and differentiation of erythroid cells and megakaryocytes thus representing a relevant therapeutic target for agents that specifically inhibit its activity particularly in myeloproliferative disorders (MPD) harboring JAK2(V617F) mutations.We discuss the physiopathology of the JAK2 signaling pathway and
Lucia E, Recchia AG, Gentile M, Bossio S, Vigna E, Mazzone C, Madeo A, Morabito L, Gigliotti V, De Stefano L, Caruso N, Servillo P, Franzese S, Bisconte MG, Gentile C, Morabito F.   +15 more
openaire   +3 more sources

The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor

Blood, 2006
AbstractJAK2, a member of the Janus kinase (JAK) family of protein tyrosine kinases (PTKs), is an important intracellular mediator of cytokine signaling. Mutations of the JAK2 gene are associated with hematologic cancers, and aberrant JAK activity is also associated with a number of immune diseases, including rheumatoid arthritis.
Lucet, Isabelle S., Fantino, Emmanuelle, Styles, Michelle, Bamert, Rebecca, Patel, Onisha, Broughton, Sophie E., Walter, Mark, Burns, Christopher J., Treutlein, Herbert, Wilks, Andrew F., Rossjohn, Jamie   +10 more
openaire   +5 more sources

Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.

Bioorganic & Medicinal Chemistry Letters, 2019
Janus Kinase 2 (JAK2) is a kind of intracellular non-receptor protein tyrosine kinase and has been certified as an important target for the treatment of myeloproliferative neoplasms and rheumatoid arthritis.
Wanqiao Wang, Yanyan Diao, Wenjie Li, Yating Luo, Tingyuan Yang, Yuyu Zhao, Tiantian Qi, Fangling Xu, Xiangyu Ma, Huan Ge, Yingfan Liang, Zhenjiang Zhao, Xin Liang, Rui Wang, Lili Zhu, Honglin Li, Yufang Xu   +16 more
semanticscholar   +1 more source

An inhibitor of Janus kinase 2 prevents polycythemia in mice

Biochemical Pharmacology, 2009
Polycythemia vera (PV) is a myeloproliferative disorder characterized by increased red cell mass and splenomegaly in the absence of secondary causes [Tefferi A., Spivak J.L., Polycythemia vera: scientific advances and current practice. Semin Hematol 2005;42(4):206-20.].
Anjili, Mathur, Jan-Rung, Mo, Manfred, Kraus, Erin, O'Hare, Peter, Sinclair, Jonathan, Young, Shuxia, Zhao, Yuxun, Wang, Johnny, Kopinja, Xianlu, Qu, John, Reilly, Deborah, Walker, Lin, Xu, Daniel, Aleksandrowicz, Gary, Marshall, Martin L, Scott, Nancy E, Kohl, Eric, Bachman   +17 more
openaire   +2 more sources

Modulation of Janus kinase 2 by cisplatin in cancer cells

International Journal of Oncology, 2004
Constitutive activation of Janus kinases (JAKs) is frequently detected in various human cancers. The activation of JAKs results in the phosphorylation and activation of signal transducers and activators of transcription (STATs). The constitutive activation of JAK/STAT pathway may play an important role in growth and survival of human cancer cells.
Hui, Song, Vernon K, Sondak, Dwayne L, Barber, Thomas J, Reid, Jiayuh, Lin   +4 more
openaire   +2 more sources

Janus kinase inhibitors for atopic dermatitis: a promising treatment modality

Clincal and Experimental Dermatology, 2021
Atopic dermatitis (AD) is chronic, pruritic, inflammatory skin disease that affects a significant portion of the population in industrialized nations. For nonresponders to conventional therapies, AD can significantly reduce sleep quality and quality of ...
A. Cartron, T. H. Nguyen, Y. Roh, M. Kwatra, S. Kwatra   +4 more
semanticscholar   +1 more source

Up-regulation of Kv1.3 Channels by Janus Kinase 2

The Journal of Membrane Biology, 2015
The janus-activated kinase 2 JAK2 participates in the signalling of several hormones including interferon, a powerful regulator of lymphocyte function. Lymphocyte activity and survival depend on the activity of the voltage-gated K(+) channel KCNA3 (Kv1.3).
Hosseinzadeh, Zohreh, Warsi, Jamshed, Elvira, Bernat, Almilaji, Ahmad, Shumilina, Ekaterina, Lang, Florian   +5 more
openaire   +3 more sources