Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt
N Uhlenbrock, S Smith, J Weisner, I Landel… - Chemical …, 2019 - pubs.rsc.org
The Ser/Thr kinase Akt (Protein Kinase B/PKB) is a master switch in cellular signal
transduction pathways. Its downstream signaling influences cell proliferation, cell growth …
transduction pathways. Its downstream signaling influences cell proliferation, cell growth …
Covalent‐allosteric kinase inhibitors
J Weisner, R Gontla… - Angewandte Chemie …, 2015 - Wiley Online Library
Targeting and stabilizing distinct kinase conformations is an instrumental strategy for
dissecting conformation‐dependent signaling of protein kinases. Herein the structure‐based …
dissecting conformation‐dependent signaling of protein kinases. Herein the structure‐based …
Novel inhibitors of AKT: assessment of a different approach targeting the pleckstrin homology domain
EJ Meuillet - Current medicinal chemistry, 2011 - ingentaconnect.com
Protein kinase B/AKT plays a central role in cancer. The serine/threonine kinase is over-
expressed or constitutively active in many cancers and has been validated as a therapeutic …
expressed or constitutively active in many cancers and has been validated as a therapeutic …
Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition
WI Wu, WC Voegtli, HL Sturgis, FP Dizon, GPA Vigers… - PloS one, 2010 - journals.plos.org
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 …
involved in cellular metabolism, growth, proliferation and survival. The three human AKT …
The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation
SF Barnett, MT Bilodeau… - Current Topics in …, 2005 - ingentaconnect.com
This article describes recent advances in the development and biological evaluation of small
molecule inhibitors for the serine/threonine kinase Akt (PKB). Akt plays a pivotal role in cell …
molecule inhibitors for the serine/threonine kinase Akt (PKB). Akt plays a pivotal role in cell …
Covalent‐allosteric inhibitors to achieve Akt isoform‐selectivity
L Quambusch, I Landel, L Depta… - Angewandte Chemie …, 2019 - Wiley Online Library
Isoforms of protein kinase Akt are involved in essential processes including cell proliferation,
survival, and metabolism. However, their individual roles in health and disease have not …
survival, and metabolism. However, their individual roles in health and disease have not …
The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation: a 2009 update
CW Lindsley - Current topics in medicinal chemistry, 2010 - ingentaconnect.com
This article describes recent advances in the development and biological evaluation of small
molecule inhibitors for the serine/threonine kinase Akt (PKB) as a reprise of our 2005 review …
molecule inhibitors for the serine/threonine kinase Akt (PKB) as a reprise of our 2005 review …
Recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors
LW Craig, BF Stanley, Y Melissa… - Current topics in …, 2007 - ingentaconnect.com
This article describes recent advances in the development and biological evaluation of small
molecule inhibitors for the serine/threonine kinase Akt (PKB). Akt plays a pivotal role in cell …
molecule inhibitors for the serine/threonine kinase Akt (PKB). Akt plays a pivotal role in cell …
In vitro and In vivo Activity of Novel Small-Molecule Inhibitors Targeting the Pleckstrin Homology Domain of Protein Kinase B/AKT
SA Moses, MA Ali, S Zuohe, L Du-Cuny, LL Zhou… - Cancer research, 2009 - AACR
The phosphatidylinositol 3-kinase/AKT signaling pathway plays a critical role in activating
survival and antiapoptotic pathways within cancer cells. Several studies have shown that …
survival and antiapoptotic pathways within cancer cells. Several studies have shown that …
Development of sulfonamide AKT PH domain inhibitors
AM Ahad, S Zuohe, L Du-Cuny, SA Moses… - Bioorganic & medicinal …, 2011 - Elsevier
Disruption of the phosphatidylinositol 3-kinase/AKT signaling pathway can lead to apoptosis
in cancer cells. Previously we identified a lead sulfonamide that selectively bound to the …
in cancer cells. Previously we identified a lead sulfonamide that selectively bound to the …