Nitika Parmar,Fuyuhiko Tamanoi
Nitika Parmar
Rheb belongs to a unique family within the Ras superfamily of G-proteins. Although initially identified in rat brain, this G-protein is highly conserved from yeast to human. While only one Rheb is present in lower eukaryotes, two Rheb prote...
Fuyuhiko Tamanoi,Channing J Der
Fuyuhiko Tamanoi
Bing Yu,Ji Luo
Bing Yu
Mutations in the Ras family of small GTPases are among the most frequent oncogenic events in human cancer. Difficulties in targeting Ras itself and the limited efficacy in targeting its effector kinases have spurred the search for Ras synth...
Recent progress in developing small molecule inhibitors designed to interfere with ras membrane association: toward inhibiting K-Ras and N-Ras functions [0.03%]
靶向干扰RAS膜定位的的小分子抑制剂研究进展：特异性抑制K-Ras和N-Ras功能
Fuyuhiko Tamanoi,Jie Lu
Fuyuhiko Tamanoi
K-Ras and N-Ras are mutated in a wide range of human cancers, thus making these proteins attractive targets of anticancer drug development. However, no effective compounds have been obtained so far. One of the approaches taken to inhibit th...
Joachim Rudolph,James J Crawford,Klaus P Hoeflich et al.
Joachim Rudolph et al.
The p21-activated kinases (PAKs) are Ser/Thr kinases in the STE20 kinase family with important roles in regulating cytoskeletal organization, cell migration, and signaling. The PAK enzyme family comprises six members subdivided into two gro...
The RalGEF/Ral pathway: evaluating an intervention opportunity for Ras cancers [0.03%]
RalGEF/Ral通路：评估干预雷佐癌的机会
Jonathan M Cooper,Brian O Bodemann,Michael A White
Jonathan M Cooper
Recognition that Ral guanine nucleotide exchange factors (RalGEFs) are direct Ras effectors and that Ral G-protein activation is a direct consequence of Ras activation has spurred focused efforts to establish the contribution of RalGEF/Ral ...
Clare Sheridan,Julian Downward
Clare Sheridan
The PI3K pathway is over-activated in the majority of human cancers. This may occur through oncogenic activation of upstream RAS isoforms and tyrosine kinase receptors, or by mutational activation of components of the PI3K pathway themselve...
Inhibitors of the ERK mitogen-activated protein kinase cascade for targeting RAS mutant cancers [0.03%]
针对RAS突变癌症的ERK丝裂原活化蛋白激酶通路抑制剂
Leanna Gentry,Ahmed A Samatar,Channing J Der
Leanna Gentry
Although recent success in identifying direct inhibitors of mutant Ras has begun to challenge the perception that Ras is "undruggable," the successful transition of these hits to the clinic remains uncertain. Therefore, current efforts to d...
Xiaolun Wang,Kristin Schleicher
Xiaolun Wang
Since the discovery linking B-Raf mutations to human tumors in 2002, significant advances in the development of Raf inhibitors have been made, leading to the recent approval of two Raf inhibitor drugs. This chapter includes a brief introduc...
Seth Nickerson,Stephen T Joy,Paramjit S Arora et al.
Seth Nickerson et al.
Rat sarcoma (RAS) proteins are signaling nodes that transduce extracellular cues into precise alterations in cellular physiology by engaging effector pathways. RAS signaling thus regulates diverse cell processes including proliferation, mig...