Uncovering molecular mechanisms involved in activation of G protein-coupled receptors

Endocrine Reviews

Volumn 21, Issue 1, 2000, Pages 90-113

  Gether, Ulrik ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

BETA 2 ADRENERGIC RECEPTOR; CALCITONIN RECEPTOR; CALCIUM; G PROTEIN COUPLED RECEPTOR; GLUCAGON; HORMONE; METABOTROPIC RECEPTOR; NEUROTRANSMITTER; RHODOPSIN; SUBSTANCE P; TACHYKININ RECEPTOR ANTAGONIST; VASOACTIVE INTESTINAL POLYPEPTIDE;

BINDING AFFINITY; BINDING SITE; BIOPHYSICS; CONFORMATIONAL TRANSITION; CRYSTALLIZATION; DIMERIZATION; HUMAN; LIGAND BINDING; MODEL; MOLECULAR INTERACTION; MOLECULAR MODEL; NEUROTRANSMISSION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DOMAIN; PROTEIN FAMILY; PROTEIN STABILITY; PROTEIN TERTIARY STRUCTURE; PROTON TRANSPORT; RECEPTOR BINDING; REVIEW; SIGNAL TRANSDUCTION;

EID: 0034464742     PISSN: 0163769X     EISSN: None     Source Type: Journal    
DOI: 10.1210/edrv.21.1.0390     Document Type: Review

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81. Identification of critical extracellular loop residues involved in α1-adrenergic receptor subtype-selective antagonist binding
82. Tachykinin receptors and tachykinin receptor antagonists
83. 3H]senktide and [125I-MePhe7]neurokinin B, and is responsive to tachykinin peptide agonists
84. Delineation of structural domains involved in subtype specificity of tachykinin receptors through chimeric formation of substance P/substance K receptors
85. Chimeric NK-1 (substance P)/NK-3 (Neurokinin-B) receptors: Identification of domains determining the binding specificity of tachykinin agonists
86. The extracellular domain of the neurokinin-1 receptor is required for high-affinity binding of peptides
87. Localization of agonist and antagonist binding domains of the human neurokinin-1 receptor
88. Interaction of substance P with the second and seventh transmembrane domains of the neurokinin-1 receptor
89. The peptide binding site of the substance P (NK-1) receptor localized by a photoreactive analogue of substance P: Presence of a disulfide bond
90. Identification of methionine as the site of covalent attachment of a p-benzoyl-phenylalanine-containing analogue of substance P on the substance P (NK-1) receptor
91. Steric hindrance mutagenesis vs. alanine scan in mapping of ligand binding sites in the tachykinin NK1 receptor
92. Identification of residues involved in ligand binding to the neurokinin-2 receptor
93. The ligand binding site of the neurokinin 2 receptor. Site-directed mutagenesis and identification of neurokinin A binding residues in the human neurokinin 2 receptor
94. Mutations along transmembrane segment II of the NK-1 receptor affect substance P competition with non-peptide antagonists but not substance P binding
95. Radioligand-dependent discrepancy in agonist affinities enhanced by mutations in the kappa-opioid receptor
96. Point mutation increases a form of the NK1 receptor with high affinity for neurokinin A and B and septide
97. Identification of peptide binding residues in the extracellular domains of the AT1 receptor
98. The docking of Arg2 of angiotensin II with Asp281 of AT1 receptor is essential for full agonism
99. Mutational analysis of the angiotensin II type 2 receptor: Contribution of conserved extracellular amino acids
100. Acidic residues in extracellular loops of the human-y1 neuropeptide-y receptor are essential for ligand binding
101. Complete mutagenesis of the extracellular domain of interleukin-8 (IL-8) type A receptor identifies charged residues mediating IL-8 binding and signal transduction
102. Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor
103. Irreversible activation of the gonadotropin-releasing hormone receptor by photoaffinity cross-linking: Localization of attachment site to Cys residue in N-terminal segment
104. Importance of extracellular domains for ligand binding in the thyrotropin-releasing hormone receptor
105. Identification of Asn289 as a ligand binding site in the rat thyrotropin-releasing hormone (THR) receptor as determined by complementary modifications in the ligand and receptor: A new model for THR binding
106. Role of the extracellular loops of the thyrotropin-releasing hormone receptor: Evidence for an initial interaction with thyrotropin-releasing hormone
107. Two-site binding of C5a by its receptor: An alternative binding paradigm for G protein-coupled receptors
108. Residues 21-30 within the extracellular N-terminal region of the C5a receptor represent a binding domain for the C5a anaphylatoxin
109. Human formyl peptide receptor ligand binding domain(s). Studies using an improved mutagenesis/expression vector reveal a novel mechanism for the regulation of receptor occupancy
110. Identification of ligand binding determinants in the somatostatin receptor subtypes 1 and 2
111. The third extracellular loop of the mu opioid receptor is important for agonist selectivity
112. Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors
113. Involvement of Trp-284, Val-296, and Val-297 of the human δ-opioid receptor in binding of δ-selective ligands
114. The third extracellular loop of the human δ-opioid receptor determines the selectivity of delta-opioid agonists
115. Novel "restoration of function" mutagenesis strategy to identify amino acids of the δ-opioid receptor involved in ligand binding
116. The N-terminal amino group of [Tyr8]bradykinin is bound adjacent to analogous amino acids of the human and rat B2 receptor
117. Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin
118. Direct identification of a distinct site of interaction between the carboxyl-terminal residue of cholecystokinin and the type A cholecystokinin receptor using photoaffinity labeling
119. Role of the extracellular domains of the cholecystokinin receptor in agonist binding
120. Met-195 of the cholecystokinin-A receptor interacts with the sulfated tyrosine of cholecystokinin and is crucial for receptor transition to high affinity state
121. Direct identification of a second distinct site of contact between cholecystokinin and its receptor
122. 3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: Characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor
123. A model of the thyrotropin-releasing hormone (TRH) receptor binding pocket. Evidence for a second direct interaction between transmembrane helix 3 and TRH
124. Hydrogen bonding interaction of thyrotropin-releasing hormone (TRH) with transmembrane tyrosine 106 of the TRH receptor
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126. 1)
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128. Lysine 182 of endothelin B receptor modulates agonist selectivity and antagonist affinity: Evidence for the overlap of peptide and non-peptide ligand binding sites
129. Tyr-129 is important to the peptide ligand affinity and selectivity of human endothelin type A receptor
130. Mutational analysis of the endothelin type A receptor (ETA): Interactions and model of selective ETA antagonist BMS-182874 with putative ETA receptor binding cavity
131. Identification of a critical aspartate residue in transmembrane domain three necessary for the binding of somatostatin to the somatostatin receptor SSTR2
132. Two amino acids, located in transmembrane domains VI and VII, determine the selectivity of the peptide agonist SMS 201-995 for the SSTR2 somatostatin receptor
133. A single amino acid substitution in somatostatin receptor subtype 5 increases affinity for somatostatin-14
134. Role of aromatic transmembrane residues of the δ-opioid receptor in ligand recognition
135. A single position in the third transmembrane domains of the human B1 and B2 bradykinin receptors is adjacent to and discriminates between the C-terminal residues of subtype-selective ligands
136. Identification of two related pentapeptides from the brain with potent opiate agonist activity
137. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry
138. Different binding epitopes on the NK1 receptor for substance-P and a non-peptide antagonist
139. Evidence for a common molecular mode of action for chemically distinct nonpeptide antagonists at the neurokinin-1 (Substance-P) receptor
140. Two nonpeptide tachykinin antagonists act through epitopes on corresponding segments of the NK-1 and NK-2 receptors
141. Characterization of non-peptide antagonist and peptide agonist binding sites of the NK1 receptor with fluorescent ligands
142. Amino aromatic interaction between histidine-197 of the neurokinin-1 receptor and CP-96345
143. Conserved His(VI-17) of the NK-1 receptor is involved in binding of non-peptide antagonists but not substance P
144. The role of histidine-265 in antagonist binding to the neurokinin-1 receptor
145. Specific residues at the top of transmembrane segment V and VI of the neurokinin-1 (NK-1) receptor involved in binding of the nonpeptide antagonist CP 96,345
146. Tachykinin non-peptide antagonists: Binding domain and molecular mode of action
147. Interaction of glutamine 165 in the fourth transmembrane segment of the human neurokinin-1 receptor with quinuclidine antagonists
148. The species selectivity of chemically distinct tachykinin nonpeptide antagonists is dependent on common divergent residues of the rat and human neurokinin-1 receptors
149. Molecular basis for the species selectivity of the neurokinin-1 receptor antagonist-CP-96,345 and antagonist-RP67580
150. Molecular basis for the species selectivity of the substance-P antagonist, CP-96,345
151. Differentiation between binding sites for angiotensin II and nonpeptide antagonists on the angiotensin II type 1 receptors
152. Genetic transfer of a nonpeptide antagonist binding site to a previously unresponsive angiotensin receptor
153. Agonists and antagonists bind to different domains of the cloned κ opioid receptor
154. Differential binding domains of peptide and non-peptide ligands in the cloned rat κ opioid receptor
155. A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists
156. A segment of five amino acids in the second extracellular loop of the cholecystokinin-B receptor is essential for selectivity of the peptide agonist gastrin
157. Mutations within the cholecystokinin-B/gastrin receptor ligand 'pocket' interconvert the functions of nonpeptide agonists and antagonists
158. Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist
159. Separable binding sites for the natural agonist endothelin-1 and the non-peptide antagonist bosentan on human endothelin-A receptors
160. Neuropeptide Y and the nonpeptide antagonist BIBP 3226 share an overlapping binding site at the human Y1 receptor
161. Non-peptide angiotensin agonist. Functional and molecular interaction with the AT1 receptor
162. Eleven amino acids (Lys-201 to Lys-211) and 9 amino acids (Gly-222 to Leu-230) in the human thyrotropin receptor are involved in ligand binding
163. Thyrotropin-luteinizing hormone/chorionic gonadotropin receptor extracellular domain chimeras as probes for thyrotropin receptor function
164. Leutropin/beta-adrenergic receptor chimeras bind choriogonadotropin and adrenergic ligands but are not expressed at the cell surface
165. Mutational analyses of the extracellular domain of the full-length lutropin/choriogonadotropin receptor suggest leucine-rich repeats 1-6 are involved in hormone binding
166. Derivation of functional antagonists using N-terminal extracellular domain of gonadotropin and thyrotropin receptors
167. The luteinizing hormone receptor
168. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation
169. Protease-activated receptor 3 is a second thrombin receptor in humans
170. Specificity of the thrombin receptor for agonist peptide is defined by its extracellular surface
171. Mechanisms of thrombin receptor agonist specificity. Chimeric receptors and complementary mutations identify an agonist recognition site
172. Highly conserved aspartate 68, tryptophane 73 and glycine 109 in the N-terminal extracellular domain of the human VIP receptor are essential for its ability to bind VIP
173. Glucagon.glucagon-like peptide I receptor chimeras reveal domains that determine specificity of glucagon binding
174. Multiple extracellular loop domains contribute critical determinants for agonist binding and activation of the secretin receptor
175. Determinants for calcitonin analog interaction with the calcitonin receptor N-terminus and transmembrane-loop regions
176. Antibodies against specific extracellular epitopes of the glucagon receptor block glucagon binding
177. Five out of six tryptophan residues in the N-terminal extracellular domain of the rat GLP-1 receptor are essential for its ability to bind GLP-1
178. Vasoactive intestinal polypeptide and pituitary adenylate cyclase-activating polypeptide receptor chimeras reveal domains that determine specificity of vasoactive intestinalpolypeptide binding and activation
179. Mapping of the ligand-selective domain of the Xenopus laevis corticotropin-releasing factor receptor 1: Implications for the ligand- binding site
180. Multiple regions of ligand discrimination revealed by analysis of chimeric parathyroid hormone 2 (PTH2) and PTH/PTH-related peptide (PTHrP) receptors
181. Evidence for a ligand interaction site at the amino-terminus of the parathyroid hormone (PTH)/PTH-related protein receptor from cross-linking and mutational studies
182. Arginine 186 in the extracellular N-terminal region of the human parathyroid hormone 1 receptor is essential for contact with position 13 of the hormone
183. Vasoactive intestinal peptide (VIP)1 receptor. Three nonadjacent amino acids are responsible for species selectivity with respect to recognition of peptide histidine isoleucineamide
184. Residues in the membrane-spanning and extracellular loop regions of the parathyroid hormone (PTH)-2 receptor determine signaling selectivity for PTH and PTH-related peptide
185. Localization of agonist- and antagonist-binding domains of human corticotropin-releasing factor receptors
186. Aspartate 196 in the first extracellular loop of the human VIP1 receptor is essential for VIP binding and VIP-stimulated cAMP production
187. Parathyroid hormone-receptor interactions identified directly by photocross-linking and molecular modeling studies
188. CP-154,526: A potent and selective nonpeptide antagonist of corticotropin releasing factor receptors
189. Role of the large extracellular domain of metabotropic glutamate receptors in agonist selectivity determination
190. The agonist selectivity of a class III metabotropic glutamate receptor, human mGluR4a, is determined by the N-terminal extracellular domain
191. The extracellular calcium-sensing receptor: Its role in health and disease
192. Structure of a glutamate-receptor ligand-binding core in complex with kainate
193. Is there a 'lock' for all agonist 'keys' in 7TM receptors?
194. Functional autoimmune epitope on alpha 1-adrenergic receptors in patients with malignant hypertension
195. Autoimmunity in idiopathic dilated cardiomyopathy. Characterization of antibodies against the β1-adrenoceptor with positive chronotropic effect
196. Monoclonal antibodies to purified muscarinic receptor display agonist-like activity
197. Extracellular domains of the bradykinin B2 receptor involved in ligand binding and agonist sensing defined by anti-peptide antibodies
198. Binding domains of stimulatory and inhibitory thyrotropin (TSH) receptor autoantibodies determined with chimeric TSH-lutropin/chorionic gonadotropin receptors
199. Antagonists with negative intrinsic activity at delta-opioid receptors coupled to GTP-binding proteins
200. Negative antagonists promote an inactive conformation of the β(2)-adrenergic receptor
201. Inverse agonist activity of β-adrenergic antagonists
202. G-protein-coupled receptor genes as protooncogenes: Constitutively activating mutation of the α 1B-adrenergic receptor enhances mitogenesis and tumorigenicity
203. Constitutive activation of the alpha 1B-adrenergic receptor by all amino acid substitutions at a single site. Evidence for a region which constrains receptor activation
204. Constitutive activity of receptors coupled to guanine nucelotide regulatory proteins
205. A mutation-induced activated state of the β2-adrenergic receptor: Extending the ternary complex model
206. Constitutively active mutants of rhodopsin
207. Pigmentation phenotypes of variant extension locus alleles result from point mutations that alter MSH receptor function
208. Somatic mutations in the thyrotropin receptor gene cause hyperfunctioning thyroid adenomas
209. A constitutively activating mutation of the lutenizing hormone receptor in familial male precocious puberty
210. Rhodopsin mutation G90D and a molecular mechanism for congenital night blindness
211. Somatic mutations causing constitutive activity of the thyrotropin receptor are the major cause of hyperfunctioning thyroid adenomas: Identification of additional mutations activating both the cyclic adenosine 3′,5′-monophosphate and inositol phosphate-Ca2+ cascades
212. Activation of the α1b-adrenergic receptor is initiated by disruption of an interhelical salt bridge constraint
213. Thrombin receptor activating mutations. Alteration of an extracellular agonist recognition domain causes constitutive signaling
214. Constitutive activation of the TSH receptor by spontaneous mutations affecting the N-terminal extracellular domain
215. The second intracellular loop of the m5 muscarinic receptor is the switch which enables G-protein coupling
216. Constitutive activation of the human vasoactive intestinal peptide 1 receptor, a member of the new class II family of G protein-coupled receptors
217. Constitutive activity of glucagon receptor mutants
218. Mutation of a highly conserved aspartic acid in the β2 adrenergic receptor: Constitutive activation, structural instability, and conformational rearrangement of transmembrane segment 6
219. The third extracellular loop of the beta2-adrenergic receptor can modulate receptor/G protein affinity
220. Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility
221. Transmembrane regions V and VI of the human luteinizing hormone receptor are required for constitutive activation by a mutation in the third intracellular loop
222. Identification of a ligand-dependent switch within a muscarinic receptor
223. Identification of a polar region in transmembrane domain 6 that regulates the function of the G protein-coupled α-factor receptor
224. A model of the lutropin/choriogonadotropin receptor: Insights into the structural and functional effects of constitutively activating mutations
225. Constitutive activation of opsin by mutation of methionine 257 on transmembrane helix 6
226. Mutation of Asn111 in the third transmembrane domain of the AT1A angiotensin II receptor induces its constitutive activation
227. A conserved carboxylic acid group mediates light-dependent proton uptake and signaling by rhodopsin
228. The activation process of the alpha1B-adrenergic receptor: Potential role of protonation and hydrophobicity of a highly conserved aspartate
229. Functional microdomains in G-protein-coupled receptors. The conserved arginine-cage motif in the gonadotropin-releasing hormone receptor
230. The role of the aspartate-arginine-tyrosine triad in the m1 muscarinic receptor: Mutations of aspartate 122 and tyrosine 124 decrease receptor expression but do not abolish signaling
231. Constitutive activation of opsin: Influence of charge at position 134 and size at position 296
232. Conserved aspartic acid residues 79 and 113 of the β-adrenergic receptor have different roles in receptor function
233. Site-directed mutagenesis and continuous expression of human beta-adrenergic receptors. Identification of a conserved aspartate residue involved in agonist binding and receptor activation
234. Pivotal role for aspartate-80 in the regulation of dopamine D2 receptor affinity for drugs and inhibition of adenylyl cyclase
235. A point mutation of the α2-adrenoceptor that blocks coupling to potassium but not calcium currents
236. Mutation of Asp(74) of the rat angiotensin-II receptor confers changes in antagonist affinities and abolishes G-protein coupling
237. Fourier transform infrared difference spectroscopy of rhodopsin mutants: Light activation of rhodopsin causes hydrogen-bonding change in residue aspartic acid-83 during meta II formation
238. Rhodopsin activation blocked by metal-ion-binding sites linking transmembrane helices C and F
239. Similar structures and shared switch mechanisms of the β2-adrenoceptor and the parathyroid hormone receptor. Zn(II) bridges between helices III and VI block activation
240. Constitutive activation of the beta2 adrenergic receptor alters the orientation of its sixth membrane-spanning segment
241. Fourier transform infrared difference spectra of intermediates in rhodopsin bleaching
242. Fourier transform infrared spectroscopy indicates a major conformational rearrangement in the activation of rhodopsin
243. Conformational changes in rhodopsin probed by surface plasmon resonance spectroscopy
244. Specific tryptophan UV-absorbance changes are probes of the transition of rhodopsin to its active state
245. Structure and function in rhodopsin: Rhodopsin mutants with a neutral amino acid at E134 have a partially activated conformation in the dark state
246. Single-cysteine substitution mutants at amino acid positions 55-75, the sequence connecting the cytoplasmic ends of helices I and II in rhodopsin: Reactivity of the sulfhydryl groups and their derivatives identifies a tertiary structure that changes upon light-activation
247. Conformational changes in rhodopsin. Movement of helix f detected by site-specific chemical labeling and fluorescence spectroscopy
248. Fluorescent labeling of purified beta2-adrenergic receptor: Evidence for ligand-specific conformational changes
249. Agonists induce conformational changes in transmembrane domains III and VI of the β2 adrenoceptor
250. Exchange of agonist site with metal-ion chelator site in the β2 adrenergic receptor
251. Model systems for the study of seven-transmembrane-segment receptors
252. Structure and function of G protein-coupled receptors
253. Molecular basis of receptor/G-protein-coupling selectivity
254. Identification of an intracellular tyrosine residue critical for muscarinic receptor-mediated stimulation of phosphatidylinositol hydrolysis
255. Functional role of a cytoplasmic aromatic amino acid in muscarinic receptor-mediated activation of phospholipase-C
256. Structure of a G-protein-coupling domain of a muscarinic receptor predicted by random saturation mutagenesis
257. Amino acid side chains that define muscarinic receptor/G-protein coupling. Studies of the third intracellular loop
258. Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins
259. Identification of a receptor/G-protein contact site critical for signaling specificity and G-protein activation
260. Molecular mechanisms involved in muscarinic aetylcholine receptor-mediated G protein activation studied by insertion mutagenesis
261. The structure of the G protein heterotrimer Gi α1 β1 γ2
262. The 2.0 A crystal structure of a heterotrimeric G protein
263. G-protein diseases furnish a model for the turn-on switch
264. A peptide derived from a β2-adrenergic receptor transmembrane domain inhibits both receptor dimerization and activation
265. Dimerization of the delta opioid receptor: Implication for a role in receptor internalization
266. Dopamine D2 receptor dimers and receptor-blocking peptides
267. Expression of dopamine D3 receptor dimers and tetramers in brain and in transfected cells
268. A transmembrane domain-derived peptide inhibits D1 dopamine receptor function without affecting receptor oligomerization
269. Similarities and differences in RANTES- and (AOP)-RANTES-triggered signals: Implications for chemotaxis
270. The chemokine monocyte chemoattractant protein-1 induces functional responses through dimerizalion of its receptor CCR2
271. Dimerization of the extracellular calcium-sensing receptor (CaR) on the cell surface of CaR-transfected HEK293 cells
272. Disulfide bonds in the extracellular calcium-polyvalent cation-sensing receptor correlate with dimer formation and its response to divalent cations in vitro
273. Metabotropic glutamate receptor 5 is a disulfide-linked dimer
274. Coexpression studies with mutant muscarinic/adrenergic receptors provide evidence for intermolecular "cross-talk" between G-protein-linked receptors
275. Dimerization of the calcium-sensing receptor occurs within the extracellular domain and is eliminated by Cys → Ser mutations at Cys101 and Cys236
276. Heterodimerization is required for the formation of a functional GABA(B) receptor
277. GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2
278. GABA(B)-receptor subtypes assemble into functional heteromeric complexes
279. Role of heteromer formation in GABAB receptor function
280. G-protein-coupled receptor heterodimerization modulates receptor function
281. Mechanism of transdominant inhibition of CCR5-mediated HIV-1 infection by CCR5δ32
282. RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor
283. Physiological effects of inverse agonists in transgenic mice with myocardial expression of the β2-adrenergic receptor
284. The two-state model of receptor activation
285. A mutation changes ligand selectivity and transmembrane signaling preference of the neurokinin-1 receptor
286. Agonist-specific coupling of a cloned Drosophila melanogaster D1-like dopamine receptor to multiple second messenger pathways by synthetic agonists
287. Contribution of serine residues to constitutive and agonist-induced signaling via the D2S dopamine receptor: Evidence for multiple, agonist-specific active conformations
288. Constitutively active α-1b adrenergic receptor mutants display different phosphorylation and internalization features
289. A three-state receptor model: Predictions of multiple agonist pharmacology for the same receptor type
290. Photoactivated conformational changes in rhodopsin: A time-resolved spin label study
291. Structure and function in rhodopsin. Measurement of the rate of metarhodopsin II decay by fluorescence spectroscopy
292. Functional interaction of transmembrane helices 3 and 6 in rhodopsin. Replacement of phenylalanine 261 by alanine causes reversion of phenotype of a glycine 121 replacement mutant