Deep Cholesterol Binding Sites    Anthony Lee - University of Southampton

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Deep Cholesterol Binding Sites

• Introduction
• GPCR Class A
• Rhodopsin and Opsin
• GPCR Class B
• GPCR Class C
• GPCR Class F
• Adiponectin Receptor
• Ion Channels
• Porins Etc.
• Transporters
• Other Membrane Proteins

Interfacial Cholesterol Binding Sites

• GPCR Class A [Part 1]
• GPCR Class A [Part 2]
• GPCR Class B
• GPCR Class C
• GPCR Class F
• Adiponectin Receptor
• TRPA-TRPN channels
• TRPP-TRPV channels

Deep Cholesterol Binding Sites on Mammalian Membrane Proteins

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Rhodopsin and Opsin

[With residue numbers in the Ballesteros-Weinstein numbering system; Units of E, kcals/mol with molar concentration units]

E	Donor		Acceptor		Local Residues (within 3 Å of a cholesterol –OH group)
Rhodopsin,  Bovine 1f88
None
Rhodopsin,  Bovine 1l9h
None
Rhodopsin,  Bovine 1gzm
None
Rhodopsin,  Bovine 1hzx
None
Rhodopsin,  Bovine 3c9l
None
Rhodopsin,  Bovine 1u19
None
Rhodopsin, with beta-ionone, Bovine 3oax
None
Rhodopsin, active (meta-II), without transducin peptide, Bovine 3pxo
None
Rhodopsin, active (meta-II), with C-terminal fragment of G-alpha, Bovine 3pqr
None
Rhodopsin,consititutionally active (meta-II), with C-terminal fragment of G-alpha,  Bovine 4a4m
None
Rhodopsin, in agonist-induced active state, Bovine 2x72
None
Rhodopsin, complex with arrestin, Human 4zwj
None
Rhodopsin, complex with arrestin, Human, 5w0p
None
Opsin retinal-free state,  Bovine, 5te3
None
Opsin,  Bovine 5wkt
None
Opsin retinal-free state, Bovine 3cap
-6.0	Thr297 [7.43]	OG1	Chl	O	Thr297 [7.43]	Val300 [7.47]	Tyr301 [7.48]
-6.0	Chl	OH	Thr297 [7.43]	OG1	Thr297 [7.43]	Tyr301 [7.48]
	Thr297 [7.43]	OG1	Chl	O
Opsin retinal-free state with bound G-alpha peptide,  Bovine 4j4q
None
Opsin retinal-free state with bound G-alpha peptide,  Bovine 4x1h
None
Opsin retinal-free state with bound ArrFL-1,  Bovine 4pxf
None
Opsin activated state with bound G-alpha peptide,  Bovine 3dqb
None
Squid rhodopsin, complex with 11-cis retinal, dimer, Japanese flying squid 2z73
-8.4	Chl	OH	Leu85 [2.55]	O	Gly45 [1.43]	Ser84 [2.54]	Leu85 [2.55]	Phe89 [2.59]
	Chl	OH	Ser84 [2.54]	O
	Phe89 [2.59]	N	Chl	O
-5.8	Chl	OH	Ser275 [6.49]	OG	Leu271 [6.45]	Ser275 [6.49]
-5.7	Ser273 [6.47]	OG	Chl	O	Gln269 [6.43]	Leu272 [6.46]	Ser273 [6.47]
Squid rhodopsin, complex with 9-cis isorhodopsin, Japanese flying squid 3ayn
-7.3	Chl	OH	Leu85 [2.55]	O	Ser84 [2.54]	Leu85 [2.55]	Phe89 [2.59]