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 B

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

E	Donor		Acceptor		Local Residues (within 3 Å of a cholesterol –OH group)
Corticotropin-releasing factor receptor 1 (CRF1R) with bound antagonist, Human  4k5y
-6.7	Chl	OH	Thr168 [2.63]	OG1	Leu164 [2.59]	Ala167 [2.62]	Thr168 [2.63]
-5.7	Chl	OH	Tyr197 [3.38]	OH	Tyr197 [3.38]	Trp236 [4.50]
Corticotropin-releasing factor receptor 1, (CRF1R) with bound antagonist, Human 4z9g
-5.9	Chl	OH	Thr168 [2.63]	OG1	Leu164 [2.59]	Thr168 [2.63]
-5.9	Chl	OH	Tyr197 [3.38]	OH	Tyr197 [3.38]	Trp236 [4.50]
-5.8	Chl	OH	Thr168 [2.63]	OG1	Leu164 [2.59]	Ala167 [2.62]	Thr168 [2.63]
Glucagon receptor, Human 4l6r
-8.9	Chl	OH	Ser189 [2.62]	OG	Leu186 [2.59]	Ser189 [2.62]	Ser190 [2.63]
	Chl	OH	Ser190 [2.63]	OG
-8.8	Chl	OH	Leu388 [7.45]	O	Leu388 [7.45]	Phe391 [7.48]	Gln392 [7.49]
	Chl	OH	Phe391 [7.48]	O
-7.4	Chl	OH	Leu388 [7.45]	O	His361 [6.52]	Leu388 [7.45]	Gln392 [7.49]
Glucagon receptor, Human 5xez
-6.4	Chl	OH	Ser189 [2.62]	OG	Leu186 [2.59]	Ser189 [2.62]	Ser190 [2.63]
	Ser189 [2.62]	OG	Chl	O
-5.9	Chl	OH	Gly359 [6.50]	O	Gly359 [6.50]	Val360 [6.51]
Glucagon receptor, Human 5xf1
-6.5	Chl	OH	Leu388 [7.45]	O	Leu388 [7.45]	Phe391 [7.48]	Gln392 [7.49]
Glucagon receptor,  with antagonist MK-0893, Human 5ee7
-5.6	Ser189 [2.62]	OG	Chl	O	Ser189 [2.62]
Glucagon-like peptide receptor (GLP-1R) complex with NNL0640, Human 5vex
-6.8	Chl	OH	Leu279 [4.55]	O	Leu279 [4.55]
-6.1	Chl	OH	Phe390 [7.45]	O	Phe390 [7.45]	Phe393 [7.48]	Gln394 [7.49]
Glucagon-like peptide receptor (GLP-1R) complex withPF-06372222, Human 5vew
-6.3	Chl	OH	Leu279 [4.55]	O	Leu279 [4.55]