JP2011224018A5 - - Google Patents
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- JP2011224018A5 JP2011224018A5 JP2011171887A JP2011171887A JP2011224018A5 JP 2011224018 A5 JP2011224018 A5 JP 2011224018A5 JP 2011171887 A JP2011171887 A JP 2011171887A JP 2011171887 A JP2011171887 A JP 2011171887A JP 2011224018 A5 JP2011224018 A5 JP 2011224018A5
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Claims (15)
- 親GPCRと比較して増大した立体構造の安定性を有するGタンパク質共役型受容体(GPCR)変異体。
- 変性条件下において、親GPCRの特定の立体構造と比較して、同じ特定の立体構造の寿命が延長している、請求項1に記載のGPCR変異体。
- 熱、界面活性剤、カオトロピック剤、及び極端なpHのいずれか1つ又は複数に対する増大した立体構造の安定性を有する、請求項1又は2に記載のGPCR変異体。
- 増大した立体構造の熱安定性を有し、例えば、親よりも少なくとも1℃安定なものである、請求項1から3のいずれか一項に記載のGPCR変異体。
- アゴニスト又はアンタゴニスト立体構造の増大した立体構造の安定性を有する、請求項1から4のいずれか一項に記載のGPCR変異体。
- それらに対するリガンド、例えば、アンタゴニスト、完全なアゴニスト、部分的なアゴニスト、又は逆アゴニストのいずれかの存在下において、親と比較して増大した立体構造の安定性を有する、請求項1から5のいずれか一項に記載のGPCR変異体であって、場合によって、前記リガンドがGPCRに結合するポリペプチド、例えば、抗体、アンキリン、RGSタンパク質、アレスチン、GPCRキナーゼ、受容体チロシンキナーゼ、RAMP、NSF、GPCR、NMDA受容体サブユニットNR1若しくはNR2a、又はカルシオン、フィブロネクチンドメインフレームワーク、或いはGPCRに結合するそれらの断片若しくは誘導体のいずれかである、請求項1から5のいずれか一項に記載のGPCR変異体。
- 前記GPCR変異体が、アデノシン受容体変異体、β−アドレナリン受容体変異体、ニューロテンシン受容体変異体、ムスカリン酸受容体変異体、5−ヒドロキシトリプタミン受容体変異体、アドレナリン受容体変異体、アナフィラトキシン受容体変異体、アンジオテンシン受容体変異体、アペリン受容体変異体、ボンベシン受容体変異体、ブラディキニン受容体変異体、カンナビノイド受容体変異体、ケモカイン受容体変異体、コレシストキニン受容体変異体、ドーパミン受容体変異体、エンドセリン受容体変異体、遊離脂肪酸受容体変異体、胆汁酸受容体変異体、ガラニン受容体変異体、モチリン受容体変異体、グレリン受容体変異体、糖タンパク質ホルモン受容体変異体、GnRH受容体変異体、ヒスタミン受容体変異体、KiSS1−由来ペプチド受容体変異体、ロイコトリエン及びリポキシン受容体変異体、リゾリン脂質受容体変異体、メラニン濃縮ホルモン受容体変異体、メラノコルチン受容体変異体、メラトニン受容体変異体、ニューロメジンU受容体変異体、神経ペプチド受容体変異体、N−ホルミルペプチドファミリー受容体変異体、ニコチン酸受容体変異体、オピオイド受容体変異体、オプシン様受容体変異体、オレキシン受容体変異体、P2Y受容体変異体、ペプチドP518受容体変異体、血小板活性化因子受容体変異体、プロキネチシン受容体変異体、プロラクチン放出ペプチド受容体変異体、プロスタノイド受容体変異体、プロテアーゼ活性化受容体変異体、リラキシン受容体変異体、ソマトスタチン受容体変異体、SPC/LPC受容体変異体、タチキニン受容体変異体、トレースアミン受容体変異体、チロトロピン放出ホルモン受容体変異体、ユーロテンシン受容体変異体、バソプレッシン/オキシトシン受容体変異体、オーファンGPCR変異体、カルシトニン受容体変異体、コルチコトロピン放出因子受容体変異体、グルカゴン受容体変異体、パラチロイド受容体変異体、VIP/PACAP受容体変異体、LNB7TM受容体変異体、GABA受容体変異体、メタボトロピックグルタミン酸受容体変異体、及びカルシウムセンサー受容体変異体のいずれかである、請求項1から6のいずれか一項に記載のGPCR変異体。
- 親受容体と比較して、以下の位置:
(i)図9に記載のシチメンチョウβ−アドレナリン受容体の番号付けした以下の位置:
Ile 55, Gly 67, Arg 68, Val 89, Met 90, Gly 98, Ile 129, Ser 151, Val 160, Gln 194, Gly 197, Leu 221, Tyr 227, Arg 229, Val 230, Ala 234, Ala 282, Asp 322, Phe 327, Ala 334, 及びPhe 338;
(ii)図10に記載のヒトアデノシンA2a受容体の番号付けした以下の位置:Gly 114, Gly 118, Leu 167, Ala 184, Arg 199, Ala 203, Leu 208, Gln 210, Ser 213, Glu 219, Arg 220, Ser 223, Thr 224, Gln 226, Lys 227, His 230, Leu 241, Pro 260, Ser 263, Leu 267, Leu 272, Thr 279, Asn 284, Gln 311, Pro 313, 及びLys 315;
(iii)図11に記載のラットニューロテンシン受容体の番号付けした以下の位置:Ala 69, Leu 72, Ala 73, Ala 86, Ala 90, Ser 100, His 103, Ser 108, Leu 109, Leu 111, Asp 113, Ile 116, Ala 120, Asp 139, Phe 147, Ala 155, Val 165, Glu 166, Lys 176, Ala 177, Thr 179, Met 181, Ser 182, Arg 183, Phe 189, Leu 205, Thr 207, Gly 209, Gly 215, Val 229, Met 250, Ile 253, Leu 256, Ile 260, Asn 262, Val 268, Asn 270, Thr 279, Met 293, Thr 294, Gly 306, Leu 308, Val 309, Leu 310, Val 313, Phe 342, Asp 345, Tyr 349, Tyr 351, Ala 356, Phe 358, Val 360, Ser 362, Asn 370, Ser 373, Phe 380, Ala 385, Cys 386, Pro 389, Gly 390, Trp 391, Arg 392, His 393, Arg 395, Lys 397, 及びPro 399;並びに
(iv)図17に記載のムスカリン受容体の番号付けした以下の位置:Leu 65, Met 145, Leu 399, Ile 383、及びMet 384のいずれか1つ又は複数に対応する位置に少なくとも1つの異なるアミノ酸を有する、請求項1から7のいずれか一項に記載のGPCR変異体。 - (i)対応する野生型アドレナリン受容体と比較して、図9に記載のシチメンチョウβ−アドレナリン受容体の番号付けした以下の位置:Ile 55, Gly 67, Arg 68, Val 89, Met 90, Gly 98, Ile 129, Ser 151, Val 160, Gln 194, Gly 197, Leu 221, Tyr 227, Arg 229, Val 230, Ala 234, Ala 282, Asp 322, Phe 327, Ala 334, 及びPhe 338のいずれか1つ又は複数に対応する位置に異なるアミノ酸を有するβ−アドレナリン受容体変異体であるか;
(ii)対応する野生型アデノシン受容体と比較して、図10に記載のヒトアデノシンA2a受容体の番号付けした以下の位置:Gly 114, Gly 118, Leu 167, Ala 184, Arg 199, Ala 203, Leu 208, Gln 210, Ser 213, Glu 219, Arg 220, Ser 223, Thr 224, Gln 226, Lys 227, His 230, Leu 241, Pro 260, Ser 263, Leu 267, Leu 272, Thr 279, Asn 284, Gln 311, Pro 313, 及びLys 315のいずれか1つ又は複数に対応する位置に異なるアミノ酸を有するアデノシン受容体変異体であるか;
(iii)対応する野生型ニューロテンシン受容体と比較して、図11に記載のラットニューロテンシン受容体の番号付けした以下の位置:Ala 69, Leu 72, Ala 73, Ala 86, Ala 90, Ser 100, His 103, Ser 108, Leu 109, Leu 111, Asp 113, Ile 116, Ala 120, Asp 139, Phe 147, Ala 155, Val 165, Glu 166, Lys 176, Ala 177, Thr 179, Met 181, Ser 182, Arg 183, Phe 189, Leu 205, Thr 207, Gly 209, Gly 215, Val 229, Met 250, Ile 253, Leu 256, Ile 260, Asn 262, Val 268, Asn 270, Thr 279, Met 293, Thr 294, Gly 306, Leu 308, Val 309, Leu 310, Val 313, Phe 342, Asp 345, Tyr 349, Tyr 351, Ala 356, Phe 358, Val 360, Ser 362, Asn 370, Ser 373, Phe 380, Ala 385, Cys 386, Pro 389, Gly 390, Trp 391, Arg 392, His 393, Arg 395, Lys 397, 及びPro 399のいずれか1つ又は複数に対応する位置に異なるアミノ酸を有するニューロテンシン受容体変異体であるか;
(iv)対応する野生型ムスカリン受容体と比較して、図17に記載のヒトムスカリン受容体の番号付けした以下の位置:Leu 65, Met 145, Leu 399, Ile 383、及びMet 384のいずれか1つ又は複数に対応する位置に異なるアミノ酸を有するムスカリン受容体変異体である、請求項1から6のいずれか一項に記載のGPCR変異体。 - 請求項1から9のいずれか一項に記載のGPCR変異体をコードするポリヌクレオチド。
- 請求項10に記載のポリヌクレオチドを含む宿主細胞。
- 可溶化された形態であるか、他のタンパク質を実質的に含まないか、又は固体支持体に固定化されている、請求項1から9のいずれか一項に記載のGPCR変異体。
- 結晶化のための、又は創薬のため、例えば、リガンド結合スクリーニング又はアッセイ開発における、又はバイオセンサーとしての、請求項1から9のいずれか一項に記載のGPCR変異体の使用。
- 前記GPCR変異体がヒトカンナビノイド受容体ではない、請求項1から9及び12のいずれか一項に記載のGPCR変異体、請求項10に記載のポリヌクレオチド、請求項11に記載の宿主細胞、又は請求項13に記載の使用。
- 請求項1から9、12、及び14のいずれか一項に記載のGPCR変異体の結晶化形態。
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GB0705450A GB0705450D0 (en) | 2007-03-22 | 2007-03-22 | Mutant proteins and method for selecting them |
GB0705450.5 | 2007-03-22 | ||
GB0724052.6 | 2007-12-08 | ||
GB0724052A GB0724052D0 (en) | 2007-12-08 | 2007-12-08 | Mutant proteins and methods for selecting them |
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JP2010500347A Division JP4842400B2 (ja) | 2007-03-22 | 2008-03-20 | Gタンパク質共役型受容体変異体及びその選択方法 |
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JP2011224018A JP2011224018A (ja) | 2011-11-10 |
JP2011224018A5 true JP2011224018A5 (ja) | 2012-11-01 |
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JP2010500347A Active JP4842400B2 (ja) | 2007-03-22 | 2008-03-20 | Gタンパク質共役型受容体変異体及びその選択方法 |
JP2011171887A Pending JP2011224018A (ja) | 2007-03-22 | 2011-08-05 | Gタンパク質共役型受容体変異体及びその選択方法 |
JP2014100213A Pending JP2014155502A (ja) | 2007-03-22 | 2014-05-14 | Gタンパク質共役型受容体変異体及びその選択方法 |
JP2016129938A Active JP6426661B2 (ja) | 2007-03-22 | 2016-06-30 | Gタンパク質共役型受容体変異体及びその選択方法 |
JP2018135756A Pending JP2018164456A (ja) | 2007-03-22 | 2018-07-19 | Gタンパク質共役型受容体変異体及びその選択方法 |
JP2020193343A Active JP7419217B2 (ja) | 2007-03-22 | 2020-11-20 | Gタンパク質共役型受容体変異体及びその選択方法 |
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JP2016129938A Active JP6426661B2 (ja) | 2007-03-22 | 2016-06-30 | Gタンパク質共役型受容体変異体及びその選択方法 |
JP2018135756A Pending JP2018164456A (ja) | 2007-03-22 | 2018-07-19 | Gタンパク質共役型受容体変異体及びその選択方法 |
JP2020193343A Active JP7419217B2 (ja) | 2007-03-22 | 2020-11-20 | Gタンパク質共役型受容体変異体及びその選択方法 |
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US (7) | US8785135B2 (ja) |
EP (4) | EP2121919B1 (ja) |
JP (6) | JP4842400B2 (ja) |
CN (2) | CN101688203B (ja) |
AT (1) | ATE544854T1 (ja) |
AU (1) | AU2008228085B2 (ja) |
CA (1) | CA2681415C (ja) |
DK (1) | DK2121919T3 (ja) |
ES (1) | ES2381780T3 (ja) |
GB (4) | GB2456237B8 (ja) |
HR (1) | HRP20120336T1 (ja) |
PL (1) | PL2121919T3 (ja) |
PT (1) | PT2121919E (ja) |
WO (1) | WO2008114020A2 (ja) |
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