نتایج جستجو برای: akt1 inhibitors

تعداد نتایج: 190478  

Journal: :the iranian journal of pharmaceutical research 0
sohrab ghanei ghoshkaneh department of chemistry, school of sciences, payam nour university of mashhad, mashhad, iran hossein eshghi department of chemistry, school of sciences, ferdowsi university of mashhad, mashhad, iran mohammad saadatmandzadeh department of chemistry, school of sciences, ferdowsi university of mashhad, mashhad, iran

abstract: objective(s): in recent years, the chemistry of 2-chloroquinoline-3-carbaldehydes have received considerable attention owing to their synthetic and effective biological importance which exhibits a wide variety of biological activity, n1,n4-bis((2-chloroquinolin-3-yl)methylene)benzene-1,4-diamine derivatives that synthesized from 2-chloroquinoline-3-carbaldehydes may have biological ef...

Abstract: Objective(s): In recent years, the chemistry of 2-chloroquinoline-3-carbaldehydes have received considerable attention owing to their synthetic and effective biological importance which exhibits a wide variety of biological activity, N1,N4-bis((2-chloroquinolin-3-yl)methylene)benzene-1,4-diamine derivatives that synthesized from 2-chloroquinoline-3-carbaldehydes may have biological ef...

Journal: :Molecular cancer therapeutics 2015
Barry R Davies Nin Guan Armelle Logie Claire Crafter Lyndsey Hanson Vivien Jacobs Neil James Philippa Dudley Kelly Jacques Brendon Ladd Celina M D'Cruz Michael Zinda Justin Lindemann Makoto Kodaira Kenji Tamura Emma L Jenkins

AKT1(E17K) mutations occur at low frequency in a variety of solid tumors, including those of the breast and urinary bladder. Although this mutation has been shown to transform rodent cells in culture, it was found to be less oncogenic than PIK3CA mutations in breast epithelial cells. Moreover, the therapeutic potential of AKT inhibitors in human tumors with an endogenous AKT1(E17K) mutation is ...

Abstract: Objective(s): In recent years, the chemistry of 2-chloroquinoline-3-carbaldehydes have received considerable attention owing to their synthetic and effective biological importance which exhibits a wide variety of biological activity, N1,N4-bis((2-chloroquinolin-3-yl)methylene)benzene-1,4-diamine derivatives that synthesized from 2-chloroquinoline-3-carbaldehydes may have biological ef...

2010
Zhiyong Ding Jiyong Liang Jin Li Yiling Lu Vathsala Ariyaratna Zhimin Lu Michael A. Davies John K. Westwick Gordon B. Mills

Frequent activation of the AKT serine-threonine kinase in cancer confers resistance to therapy. AKT is activated by a multi-step process involving phosphatidylinositide (PtdIns) phosphate-mediated recruitment of AKT and its upstream kinases, including 3-Phosphoinositide-dependent kinase 1 (PDK1), to the inner surface of the cell membrane. PDK1 in the appropriate context phosphorylates AKT at th...

2015
Barry R. Davies Nin Guan Armelle Logie Claire Crafter Lyndsey Hanson Vivien Jacobs Neil James Philippa Dudley Kelly Jacques Brendon Ladd Celina M. D'Cruz Michael Zinda Justin Lindemann Makoto Kodaira Emma L. Jenkins

AKT1mutations occur at low frequency in a variety of solid tumors, including those of the breast and urinary bladder. Although this mutation has been shown to transform rodent cells in culture, it was found to be less oncogenic than PIK3CA mutations in breast epithelial cells. Moreover, the therapeutic potential of AKT inhibitors in human tumorswith an endogenous AKT1mutation is not known. Expr...

Journal: :Bioorganic & medicinal chemistry letters 2005
Craig W Lindsley Zhijian Zhao William H Leister Ronald G Robinson Stanley F Barnett Deborah Defeo-Jones Raymond E Jones George D Hartman Joel R Huff Hans E Huber Mark E Duggan

This letter describes the development of two series of potent and selective allosteric Akt kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo.

Journal: :Molecular cancer research : MCR 2003
Luca M Neri Paola Borgatti Pier Luigi Tazzari Roberta Bortul Alessandra Cappellini Giovanna Tabellini Alfonso Bellacosa Silvano Capitani Alberto M Martelli

Disruption of the apoptotic pathways may account for resistance to chemotherapy and treatment failures in human neoplastic disease. To further evaluate this issue, we isolated a HL-60 cell clone highly resistant to several drugs inducing apoptosis and to the differentiating chemical all-trans-retinoic acid (ATRA). The resistant clone displayed an activated phosphoinositide 3-kinase (PI3K)/AKT1 ...

Journal: :Molecular cancer research : MCR 2015
Jaclyn F Hechtman Justyna Sadowska Jason T Huse Laetitia Borsu Rona Yaeger Jinru Shia Efsevia Vakiani Marc Ladanyi Maria E Arcila

UNLABELLED The PI3K/AKT/mTOR pathway is activated through multiple mechanisms in colorectal carcinoma. Here, the clinicopathologic and molecular features of AKT1 E17K-mutated colorectal carcinoma in comparison with PIK3CA-mutated colorectal carcinoma are described in detail. Interestingly, in comparison with PIK3CA mutants, AKT1 E17K was significantly associated with mucinous morphology and con...

2010
Wen-I Wu Walter C. Voegtli Hillary L. Sturgis Faith P. Dizon Guy P. A. Vigers Barbara J. Brandhuber

AKT1 (NP_005154.2) is a member of the serine/threonine AGC protein kinase family involved in cellular metabolism, growth, proliferation and survival. The three human AKT isozymes are highly homologous multi-domain proteins with both overlapping and distinct cellular functions. Dysregulation of the AKT pathway has been identified in multiple human cancers. Several clinical trials are in progress...

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