JP2021036901A5 - - Google Patents
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- JP2021036901A5 JP2021036901A5 JP2020193343A JP2020193343A JP2021036901A5 JP 2021036901 A5 JP2021036901 A5 JP 2021036901A5 JP 2020193343 A JP2020193343 A JP 2020193343A JP 2020193343 A JP2020193343 A JP 2020193343A JP 2021036901 A5 JP2021036901 A5 JP 2021036901A5
- Authority
- JP
- Japan
- Prior art keywords
- gpcr
- receptor
- variant
- leu
- ala
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims 80
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims 80
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 30
- 102000005962 receptors Human genes 0.000 claims 27
- 108020003175 receptors Proteins 0.000 claims 27
- 239000003446 ligand Substances 0.000 claims 21
- 239000005557 antagonist Substances 0.000 claims 13
- 239000000556 agonist Substances 0.000 claims 11
- 150000001413 amino acids Chemical class 0.000 claims 10
- 238000003505 heat denaturation Methods 0.000 claims 5
- 102000004169 proteins and genes Human genes 0.000 claims 5
- 108090000623 proteins and genes Proteins 0.000 claims 5
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 4
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 claims 4
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 claims 4
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 claims 4
- 238000010438 heat treatment Methods 0.000 claims 4
- 230000014759 maintenance of location Effects 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 102000018208 Cannabinoid Receptor Human genes 0.000 claims 3
- 108050007331 Cannabinoid receptor Proteins 0.000 claims 3
- 101000887490 Homo sapiens Guanine nucleotide-binding protein G(z) subunit alpha Proteins 0.000 claims 3
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims 3
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims 3
- 238000004925 denaturation Methods 0.000 claims 3
- 230000036425 denaturation Effects 0.000 claims 3
- 102000052301 human GNAZ Human genes 0.000 claims 3
- 102000040430 polynucleotide Human genes 0.000 claims 3
- 108091033319 polynucleotide Proteins 0.000 claims 3
- 239000002157 polynucleotide Substances 0.000 claims 3
- GJLXVWOMRRWCIB-MERZOTPQSA-N (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanamide Chemical compound C([C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=CC=C(O)C=C1 GJLXVWOMRRWCIB-MERZOTPQSA-N 0.000 claims 2
- 102000009346 Adenosine receptors Human genes 0.000 claims 2
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- 239000002126 C01EB10 - Adenosine Substances 0.000 claims 2
- -1 His 103 Chemical compound 0.000 claims 2
- 102000017922 Neurotensin receptor Human genes 0.000 claims 2
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- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 claims 1
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- UCTWMZQNUQWSLP-UHFFFAOYSA-N Adrenaline Natural products CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 claims 1
- 108060003345 Adrenergic Receptor Proteins 0.000 claims 1
- 102000017910 Adrenergic receptor Human genes 0.000 claims 1
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 1
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 1
- 108070000005 Bile acid receptors Proteins 0.000 claims 1
- 102000017002 Bile acid receptors Human genes 0.000 claims 1
- 108010073466 Bombesin Receptors Proteins 0.000 claims 1
- 102000010183 Bradykinin receptor Human genes 0.000 claims 1
- 108050001736 Bradykinin receptor Proteins 0.000 claims 1
- 108010001789 Calcitonin Receptors Proteins 0.000 claims 1
- 102100038520 Calcitonin receptor Human genes 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 102000009410 Chemokine receptor Human genes 0.000 claims 1
- 108050000299 Chemokine receptor Proteins 0.000 claims 1
- 102000004859 Cholecystokinin Receptors Human genes 0.000 claims 1
- 108090001085 Cholecystokinin Receptors Proteins 0.000 claims 1
- 108010056643 Corticotropin-Releasing Hormone Receptors Proteins 0.000 claims 1
- 102100038018 Corticotropin-releasing factor receptor 1 Human genes 0.000 claims 1
- 102000015554 Dopamine receptor Human genes 0.000 claims 1
- 108050004812 Dopamine receptor Proteins 0.000 claims 1
- 108070000009 Free fatty acid receptors Proteins 0.000 claims 1
- 108010005551 GABA Receptors Proteins 0.000 claims 1
- 102000005915 GABA Receptors Human genes 0.000 claims 1
- 102000011392 Galanin receptor Human genes 0.000 claims 1
- 108050001605 Galanin receptor Proteins 0.000 claims 1
- 108010063919 Glucagon Receptors Proteins 0.000 claims 1
- 102100040890 Glucagon receptor Human genes 0.000 claims 1
- 102000017357 Glycoprotein hormone receptor Human genes 0.000 claims 1
- 108050005395 Glycoprotein hormone receptor Proteins 0.000 claims 1
- 102100033851 Gonadotropin-releasing hormone receptor Human genes 0.000 claims 1
- 108010002059 Histamine Receptors Proteins 0.000 claims 1
- 102000000543 Histamine Receptors Human genes 0.000 claims 1
- 101001060451 Homo sapiens Pyroglutamylated RF-amide peptide receptor Proteins 0.000 claims 1
- 102100030643 Hydroxycarboxylic acid receptor 2 Human genes 0.000 claims 1
- 101710125793 Hydroxycarboxylic acid receptor 2 Proteins 0.000 claims 1
- 101150020170 KISS1R gene Proteins 0.000 claims 1
- 108010021290 LHRH Receptors Proteins 0.000 claims 1
- 108070000013 Lysolipids receptors Proteins 0.000 claims 1
- 102000016994 Lysolipids receptors Human genes 0.000 claims 1
- 102000004378 Melanocortin Receptors Human genes 0.000 claims 1
- 108090000950 Melanocortin Receptors Proteins 0.000 claims 1
- 108050009605 Melatonin receptor Proteins 0.000 claims 1
- 102000001419 Melatonin receptor Human genes 0.000 claims 1
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 claims 1
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 claims 1
- 102100033818 Motilin receptor Human genes 0.000 claims 1
- 108700040483 Motilin receptors Proteins 0.000 claims 1
- 102100021126 N-formyl peptide receptor 2 Human genes 0.000 claims 1
- 101710091942 N-formyl peptide receptor 2 Proteins 0.000 claims 1
- 102000030937 Neuromedin U receptor Human genes 0.000 claims 1
- 108010002741 Neuromedin U receptor Proteins 0.000 claims 1
- 102000028517 Neuropeptide receptor Human genes 0.000 claims 1
- 108070000018 Neuropeptide receptor Proteins 0.000 claims 1
- 102000003840 Opioid Receptors Human genes 0.000 claims 1
- 108090000137 Opioid Receptors Proteins 0.000 claims 1
- 102100028139 Oxytocin receptor Human genes 0.000 claims 1
- 108090000876 Oxytocin receptors Proteins 0.000 claims 1
- 108010064032 Pituitary Adenylate Cyclase-Activating Polypeptide Receptors Proteins 0.000 claims 1
- 102000014743 Pituitary Adenylate Cyclase-Activating Polypeptide Receptors Human genes 0.000 claims 1
- 108070000023 Prokineticin receptors Proteins 0.000 claims 1
- 102000056271 Prolactin-releasing peptide receptors Human genes 0.000 claims 1
- 108700024163 Prolactin-releasing peptide receptors Proteins 0.000 claims 1
- 102000002020 Protease-activated receptors Human genes 0.000 claims 1
- 108050009310 Protease-activated receptors Proteins 0.000 claims 1
- 102000002298 Purinergic P2Y Receptors Human genes 0.000 claims 1
- 108010000818 Purinergic P2Y Receptors Proteins 0.000 claims 1
- 102100027888 Pyroglutamylated RF-amide peptide receptor Human genes 0.000 claims 1
- 101500028886 Rattus norvegicus Neurotensin Proteins 0.000 claims 1
- 102000004215 Relaxin receptors Human genes 0.000 claims 1
- 108090000728 Relaxin receptors Proteins 0.000 claims 1
- 108070000025 Releasing hormones receptors Proteins 0.000 claims 1
- 102000016983 Releasing hormones receptors Human genes 0.000 claims 1
- 108050001286 Somatostatin Receptor Proteins 0.000 claims 1
- 102000011096 Somatostatin receptor Human genes 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 238000011948 assay development Methods 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 230000003196 chaotropic effect Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 238000007876 drug discovery Methods 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
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- 229940125425 inverse agonist Drugs 0.000 claims 1
- 108010016743 leucine receptor Proteins 0.000 claims 1
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- 150000002617 leukotrienes Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000012986 modification Methods 0.000 claims 1
- 230000004048 modification Effects 0.000 claims 1
- 108091008880 orphan GPCRs Proteins 0.000 claims 1
- 239000004031 partial agonist Substances 0.000 claims 1
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- 238000012216 screening Methods 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
| JP2018135756A 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 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018135756A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021036901A JP2021036901A (ja) | 2021-03-11 |
| JP2021036901A5 true JP2021036901A5 (https=) | 2021-07-26 |
| JP7419217B2 JP7419217B2 (ja) | 2024-01-22 |
Family
ID=39386585
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Family Applications Before (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (14)
| Country | Link |
|---|---|
| US (7) | US8785135B2 (https=) |
| EP (4) | EP2386635A3 (https=) |
| JP (6) | JP4842400B2 (https=) |
| CN (2) | CN101688203B (https=) |
| AT (1) | ATE544854T1 (https=) |
| AU (1) | AU2008228085B2 (https=) |
| CA (1) | CA2681415C (https=) |
| DK (1) | DK2121919T3 (https=) |
| ES (2) | ES3008359T3 (https=) |
| GB (4) | GB2456236B8 (https=) |
| HR (1) | HRP20120336T1 (https=) |
| PL (1) | PL2121919T3 (https=) |
| PT (1) | PT2121919E (https=) |
| WO (1) | WO2008114020A2 (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2121919T3 (da) | 2007-03-22 | 2012-05-21 | Heptares Therapeutics Ltd | Mutante g-proteinkoblede receptorer og fremgangsmåder til udvælgelse heraf |
| GB0724051D0 (en) * | 2007-12-08 | 2008-01-16 | Medical Res Council | Mutant proteins and methods for producing them |
| GB0724860D0 (en) * | 2007-12-20 | 2008-01-30 | Heptares Therapeutics Ltd | Screening |
| GB0802474D0 (en) | 2008-02-11 | 2008-03-19 | Heptares Therapeutics Ltd | Mutant proteins and methods for selecting them |
| US20110112037A1 (en) * | 2008-03-05 | 2011-05-12 | Heptares Therapeutics Limited BioPark | Crystal structure |
| GB0910725D0 (en) | 2009-06-22 | 2009-08-05 | Heptares Therapeutics Ltd | Mutant proteins and methods for producing them |
| GB201014715D0 (en) | 2010-09-06 | 2010-10-20 | Vib Vzw | Nanobodies stabilizing functional conformational states of GPCRS |
| WO2012022928A2 (en) | 2010-08-20 | 2012-02-23 | Heptares Therapeutic Ltd | Biological materials and uses thereof |
| WO2012098413A1 (en) | 2011-01-21 | 2012-07-26 | Heptares Therapeutics Limited | Mutant g-protein coupled receptor proteins and methods for producing them |
| SG10201701547VA (en) | 2011-02-23 | 2017-03-30 | Massachusetts Inst Technology | Water soluble membrane proteins and methods for the preparation and use thereof |
| WO2012120315A2 (en) | 2011-03-10 | 2012-09-13 | Heptares Therapeutics Limited | Mutant proteins and methods for producing them |
| DK2742066T3 (en) | 2011-08-10 | 2018-03-05 | Heptares Therapeutics Ltd | STABLE PROTEINS |
| ES2676827T3 (es) * | 2012-06-01 | 2018-07-25 | Heptares Therapeutics Limited | Ensayos |
| WO2014118297A1 (en) | 2013-01-30 | 2014-08-07 | Vib Vzw | Novel chimeric polypeptides for screening and drug discovery purposes |
| EP2970425B1 (en) | 2013-03-15 | 2019-10-30 | United Kingdom Research and Innovation | Mutant membrane proteins and methods for their production |
| WO2014176544A1 (en) * | 2013-04-25 | 2014-10-30 | The Trustees Of The University Of Pennsylvania | Water soluble g-protein coupled receptor |
| WO2014176524A2 (en) | 2013-04-25 | 2014-10-30 | The Trustees Of The University Of Pennsylvania | Opioid detection based on high quality graphene transistor arrays and a synthetic mu receptor |
| CA2914831C (en) * | 2013-06-11 | 2022-10-11 | Paul Scherrer Institut | Method for determining mutateable ligand-gpcr binding at single amino acid resolution and pairs of mutated ligand and gpcr |
| US10373702B2 (en) | 2014-03-27 | 2019-08-06 | Massachusetts Institute Of Technology | Water-soluble trans-membrane proteins and methods for the preparation and use thereof |
| CN104151401A (zh) * | 2014-06-05 | 2014-11-19 | 维亚生物科技(上海)有限公司 | 融合表达离子通道蛋白及运输蛋白的方法及其使用的蛋白片断 |
| GB2527286A (en) * | 2014-06-11 | 2015-12-23 | Rsr Ltd | Glycoprotein hormone receptor mutations |
| WO2016070022A1 (en) | 2014-10-31 | 2016-05-06 | Abilita Bio, Inc. | Modified membrane spanning proteins and methods for the preparation and use thereof |
| US11618777B2 (en) | 2015-07-31 | 2023-04-04 | Shigeyuki Yokoyama | Method of manufacturing membrane protein and utilization thereof |
| GB201601690D0 (en) | 2016-01-29 | 2016-03-16 | Heptares Therapeutics Ltd | G proteins |
| EP3205450A1 (de) * | 2016-02-09 | 2017-08-16 | Hermes Schleifkörper GmbH | Verfahren zur herstellung eines keramischen formkörpers |
| EP3452516A4 (en) | 2016-05-04 | 2019-11-27 | Abilita Bio, Inc. | Methods and platform for preparing multispanning membrane proteins |
| CN113501881B (zh) * | 2017-09-27 | 2023-07-28 | 北京大学 | 融合蛋白 |
| US12123814B1 (en) * | 2019-06-14 | 2024-10-22 | Pierce Biotechnology, Inc. | G- protein coupled receptor extraction formulations |
| TW202242114A (zh) | 2020-12-23 | 2022-11-01 | 美商再生元醫藥公司 | 用於獲得結合至跨膜蛋白之抗體以及抗體生成細胞的方法 |
| CN114038498B (zh) * | 2022-01-06 | 2022-03-18 | 北京晶泰科技有限公司 | Gpcr的热稳定性突变预测方法、结构筛选方法及其装置 |
| CN120948816B (zh) * | 2025-10-20 | 2026-03-03 | 国科大杭州高等研究院 | 一种g蛋白偶联受体的热稳定性突变位点筛选方法及其用途 |
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