Role of cholesterol in the function and organization of G-protein coupled receptors

Molecular rheology of neuronal membranes explored using a molecular rotor: Implications for receptor function

“…Membrane cholesterol has previously been shown to be a crucial modulator of the function of membrane receptors (Burger et al, 2000;Pucadyil and Chattopadhyay, 2006;Paila and Chattopadhyay, 2010;Oates and Watts, 2011;Jafurulla and Chattopadhyay, 2013).…”

“…In this context, cholesterol represents an important lipid since brain cholesterol has been implicated in a number of neurological disorders (Chattopadhyay and Paila, 2007;Martín et al, 2014), some of which share a common etiology of defective cholesterol 4 metabolism in the brain (Porter and Herman, 2011). More importantly, the function of neuronal receptors depends on cholesterol (Pucadyil and Chattopadhyay, 2006;Allen et al, 2007;Paila and Chattopadhyay, 2010;Jafurulla and Chattopadhyay, 2013), which affects neurotransmission, resulting in mood and anxiety disorders (Papakostas et al, 2004). In spite of these important functional correlates, the organization and dynamics of neuronal membranes as a consequence of alterations in membrane cholesterol is only beginning to be understood.…”

Distinct modes of molecular regulation of CCL3 induced calcium flux in monocytic cells

“…Previous reports by us and others highlighted the importance of cholesterol in the plasma membrane for effective CCR5 signalling [6,8,11,22]. Altogether there is a certain problematic with 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 65 13 specific, since it can be observed in CHO.CCR5 cells, but not in THP-1 cells [24].…”

“…Changing the cholesterol concentration in the plasma membrane of cells using MCD or similar agents generally decrease the signalling properties of the receptor [6,8,11], but it can also disrupt lipid rafts and modulate the activity of multiple signalling pathways, like activating the Ras-Erk pathways in T-lymphocytes [25]. Unlike other The question remains how MCD treatment increases the signal.…”

“…Furthermore it has been reported that chemokines bind preferentially to receptors which are associated with cholesterol and sphingolipid-rich 3 lipid raft microdomains in the plasma membrane [5]. It was shown that CCR5 requires membrane cholesterol to retain ligand binding and signalling functions [6][7][8].…”