S6 kinase, a member of AGC family of protein kinases and a downstream effector of mTORC1 pathway has over the years found much relevance in maintaining a normal cellular state by virtue of its established role in regulation of cell growth and proliferation. S6 kinase activity has been linked to different cellular processes like glucose homeostasis, translational and transcriptional regulation. Hence any dysregulation in S6K1 leads to the emergence of various pathological conditions like diabetes, cancer and obesity. It is as such S6 kinase has emerged as a potential target for therapeutic interventions employed in curing such diseases. The Present Chapter reviews the regulation of S6K1, its structural organization and functions, besides highlighting its potential to act as an alternative therapeutic target for various cancerous situations exhibiting deranged mTOR signaling so as to overcome the possibility of relapses observed otherwise while using conventional drug