Switching of Trp-214 intrinsic rotamer population in human serum albumin: An insight into the aftermath of embracing therapeutic bioorganic luminophore azapodophyllotoxin into sudlow site I.

摘要: Abstract Human serum albumin is perceived to be the most abundant protein in human blood plasma and functions as a major carrier of different enzymes drugs inside body. The present article puts an effort demonstrate attitude adopted by towards potential therapeutic luminophore 4-(2-Hydroxyethyl)-10-phenyl-3,4,6,7,8,10-hexahydro-1H-cyclopenta[g]furo[3,4-b]quinoline-1-one (HPFQ). HPFQ prodigy from azapodophyllotoxin class compounds, which have been synthesized perspective improved bioactivity than its prologue podophyllotoxins. While, has proved highly bioactive against cancer cell lines with best GI50 values K b = 0.74 × 105 M−1). time-resolve fluorescence studies reveal appreciable reduction HSA average radiative lifetime increase concentration provided evidence for Forster’s resonance energy transfer (FRET) being responsible dominant quenching mechanism, escorted minor structural deformations backbone structure. institutes itself near Trp-214 within matrix, subsequently “hydrophobic amino acids” dominated cybotactic environment experiences micropolarity. allosteric modulation triggered stronger association leads deformation secondary structure protein. Sudlow site I proficiently embraces favourable conformation like malleable dough furnish space arriving molecule. also believed administer conformational regulation domain affecting inter-conversion rotamers, may prove enlightening area decode preferable interaction between them. juxtaposed spectroscopic research described herein expected embolden design based anti-proliferative clinical agents efficient vivo bio-distribution employing HSA-centred drug delivery administration systems.