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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GPCRs Class F

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

E	Donor		Acceptor		Local Residues (within 3 Å of a cholesterol –OH group)
Smoothened (SMO) receptor with bound antagonist, LY2940680,  Human  4jkv
-5.9	Chl	OH	Ser366 [4.51]	OG	Leu362 [4.47]	Ser366 [4.51]
Smoothened (SMO) receptor with bound  SANT-1, Human  4n4w
-6.0	Chl	OH	Tyr323 [3.34]	OH	Tyr323 [3.34]
Smoothened (SMO) receptor with bound SAG1.5,  Human  4qin
-6.1	Tyr323 [3.34]	OH	Chl	O	Tyr323 3.34]
-5.8	Chl	OH	Ser366 [4.51]	OG	Ser366 [4.51]	Leu367 [4.52]
Smoothened (SMO) receptor with bound ANTA XV,  Human  4qim
None
Smoothened (SMO) receptor with bound cyclopamine, Human  4o9r
-5.6	Chl	OH	Ser468 [6.49]	OG	Leu464 [6.45]	Ile465 [6.46]	Ser468 [6.49]
Smoothened (SMO) receptor in complex with cholesterol,  Human  5l7d
-6.7	Ala324 [3.35]	N	Chl	O	Val319 [3.30]	Ile320 [3.31]	Tyr323 [3.34]	Ala324 [3.35]
	Chl	OH	Ile320 [3.31]	O
-6.0	Chl	OH	Leu458 [6.39]	O	Phe457 [6.38]	Leu458 [6.39]	Gly461 [ 6.42]
-5.8	Chl	OH	Tyr323 [3.34]	OH	Tyr323 [3.34]	Trp365 [4.50]
-5.8	Phe462 [6.43]	N	Chl	O	Leu458 [6.39]	Gly461 [ 6.42]	Phe462 [6.43]
Smoothened (SMO) receptor with bound vismodegib, Human  5l7i
-6.4	Ala324 [3.35]	N	Chl	O	Val319 [3.30]	Ile320 [3.31]	Tyr323 [3.34]	Ala324 [3.35]
	Chl	OH	Ile320 [3.31]	O