このページはRCSBの David S. Goodsell博士による「Molecule of the Month」2003年10月の記事を日本語に訳したものです。転載・引用については利用規約をご覧下さい。
「今月の分子」一覧に戻る / この記事のRCSBオリジナルサイト(英語)を見る
:翻訳 工藤高裕 (PDBj)
上:トリプシン(PDB:2ptn) 中:キモトリプシン(PDB:2cha) 下:エラスターゼ(PDB:3est)

我々の身体は成長と修復のため安定したアミノ酸の供給を必要とする。通常の大人は体重によって1日35〜90gのタンパク質が必要であるが、かなり驚くべきことにその多くは体内で得られる。通常の北米の食事には1日70〜100gのタンパク質※が含まれているが、一方で、我々の身体は消化を助け役目を終えると自分自身を消化するタンパク質を20〜30g分泌している。血管に漏れ出す死んだ腸細胞やタンパク質も消化され、アミノ酸となって再び吸収される。このことは我々の身体が再利用の達人であることを示している。

日本の場合1人1日当たりの供給量は82.3g(農林水産省食糧需給表2007年概算値)。

タンパク質のはさみ

タンパク質は丈夫なので、我々はタンパク質をその構成単位であるアミノ酸にまで消化するのにいくつもの酵素を使っている。タンパク質の消化は で始まる。ここでは 塩酸 (hydrochloric acid)がタンパク質を変性させ、それを酵素の ペプシン (pepsin)が大雑把に分解する。そして実質的な消化は (intestine)で始まる。 膵臓 (すい臓、pancreas)はタンパク質を切断する酵素の集まりを加える。ここではトリプシン(trypsin)が中心的な役割を果たし、タンパク質鎖を切り刻んで数個の長さのアミノ酸鎖にする。そしてその断片は、腸細胞の表面と内側にある酵素によって個々のアミノ酸にまで切断され、身体全体で使える状態になる。

タンパク質切断機械

トリプシンはタンパク質切断反応において特別な セリン (serine)アミノ酸を用いることから、 セリンプロテアーゼ (serine protease)として知られている。セリンプロテアーゼはさまざまな酵素が集まったファミリーで、どれも似た酵素の機械を使っている。消化では、 トリプシンキモトリプシン (chymotrypsin)、 エラスターゼ (elastase)は協同して働き、タンパク質を切断する。それぞれ特有のタンパク質鎖を対象とする。トリプシン(図上、PDBエントリー 2ptn )は リジン (lysine)と アルギニン (arginine)の隣を切断する。キモトリプシン(図中央、PDBエントリー 2cha )は フェニルアラニン (phenylalanine)などの大きなアミノ酸の隣を切断する。エラスターゼ(図下、PDBエントリー 3est )は アラニン (alanine)のように小さなアミノ酸でできたペプチド鎖がお好みである。各図では重要なセリンを中央に赤色で示す。これには ヒスチジン (histidine、白と青)と アスパラギン酸 (aspartate、赤で示した酸素1個だけが見えている)を伴っている。トリプシンに似た酵素は体内の他の場所でも見つかる。この中には高い特異性があり、特定に対象タンパク質だけを切断するものもある。例えば、今月の分子で2002年1月に紹介した [[mom:025|トロンビン (thronbin)は、 血栓 (blood clot)を作る フィブリノーゲン (fibrinogen)を特異的に切断するよう設計されている。

丈夫な酵素

セリンプロテアーゼは酵素の発見と研究において中心的な役割を果たしている。その理由の一つは、研究しやすいからである。消化液中に豊富に含まれていて大変溶けやすいので、集めて精製するのが比較的容易なのである。また機能を研究するのも簡単である。あるタンパク質を投げ込み、どれだけ速く消化されるかを見るだけでよいからである。キモトリプシンはX線結晶学で研究された最初のタンパク質の一つで、その研究によりこれが対象タンパク質をつかんで正確な原子変化を行う複雑な機械であることが明らかになった。今日、何百個ものセリンプロテアーゼの構造がPDBデータバンクに登録され、探索されるのを待っている。

タンパク質分解酵素の危険

左:トリプシノーゲン(PDB:1tgs、緑は不活性化のための追加配列、赤紫はそれが除去された後の末端) 右:トリプシンとトリプシン阻害剤(PDB:2ptc、赤が阻害剤)

体内にあるタンパク質の消化は細心の注意を要する仕事である、と思うかもしれない。タンパク質は各細胞において材料の5分の1を作り出している。そのため、タンパク質切断機械を作る時には注意しなければならない。消化酵素にとって、その方策とは酵素を不活性な型(これを酵素前駆体(zymogen、 チモーゲン )と呼ぶ)で作っておき、その後腸内で活性化するというものである。トリプシンは最初余分なタンパク質鎖をつけて作られる。それが上図左の構造(PDBエントリー 1tgs )中にある緑色の部分である。実際、この結晶構造ではこの余分な部分のうち2個のアミノ酸しか見えていないので、タンパク質から離れて辺りをばたばたしている残りの部分を想像しなくてはならない。この余分な部分がついた型のトリプシンは トリプシノーゲン (trypsinogen)と呼ばれる不活性型で、タンパク質鎖を切断することはできない。これが腸に入ると、 エンテロペプチダーゼ (enteropeptidase)酵素によって小さな尾部が切断される。これによって新たにできる鎖の末端(赤紫の部分)が折りたたまれたタンパク質の中にしまいこまれて安定化し、右側に示した活性型の酵素(PDBエントリー 2ptc )になる。更に保険として、膵臓も小さなタンパク質トリプシン阻害剤(図右の赤色部分)を作る。これは腸に分泌される前に存在するどんな微量の活性型トリプシンでも結合して活性を阻止する。これはトリプシンの活性部位に結合して、その活性を阻害するがこの阻害剤自体は小片へと切断されることはない。

構造をみる

トリプシンの電荷中継機構とトリプシン阻害剤(PDB:2ptc)

PDBデータベースを見ると、消化、ホルモン活性化、血液凝固、免疫機構活性化などさまざまな機能のために作られるセリンプロテアーゼの事例を見いだすことができるだろう。それらはタンパク質切断反応を補助するための独特なアミノ酸の集まりを共有している。これは進化によって繰り返し発見されてきたものである。機械の中心はヒスチジンとアルパラギン酸によって活性化されるセリンアミノ酸である。これら3つのアミノ酸をまとめて、 電荷中継機構 (charge relay system)と呼ばれている。ヒスチジンとアスパラギン酸はセリンの水素原子(白)を除去するのを助ける。これによって切断対象のタンパク質を攻撃する際の活性が更に上がる。右に示した図はPDBエントリー 2ptc の構造データを用いて作ったもので、阻害剤タンパク質(ピンク)がトリプシンの活性部位に結合している様子が描かれている。緑色で示した阻害剤の切断部位は、この位置ではほとんどのタンパク質は切断されないという十分離れた場所で捕まえられている。右下に伸びている長いリジンアミノ酸にも注目して欲しい。これはトリプシンの中にある別のアスパラギン酸と相互作用する(そのアスパラギン酸の酸素原子が図の右下の角に赤色で示されている)。トリプシンは、この反応によってリジンアミノ酸かアルギニンアミノ酸の隣を好んで切断する。

2003年10月時点でPDBに登録されている、トリプシンの構造全ての一覧をこちらのリストに掲載している。また、遺伝的視点から見たトリプシンに関する追加情報が、 欧州バイオインフォマティクス研究所 (EBI)の「 今月のタンパク質 」で提供されている。

2003年10月時点でPDBに登録されている、トリプシンの構造一覧
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1hja Crystal Structure of Lys18 Variant of Turkey Ovomucoid Inhibitor Third Domain Complexed with Alpha- Chymotrypsin at 2.3 A J.Ding,
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n/a To be Published n/a n/a n/a
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1j0q The Solution Structure of the Oxidized Bovine Microsomal Cytochrome B5 Mutant V61H C.Cao,
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1j8a Crystal Structure of Trypsin at Atomic Resolution Using Data from Laboratory Source J.A. Cuesta- Seijo,
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n/a To be Published n/a n/a n/a
1jbl Solution Structures by 1H NMR of the Novel Cyclic Trypsin Inhibitor Sfti-1 from Sunflower Seeds and an Acyclic Permutant M.L. J.Korsinczky,
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1jxc NMR Solution Structure of Attp, an Arabidopsis Thaliana Trypsin Inhibitor Q.Zhao,
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1lcn Crystal Structure of Lysozyme Complexed with Thiocyanate at 1.6 Angstroms C.Hamiaux,
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1ldt The three- dimensional structure of recombinant leech- derived tryptase inhibitor in complex with trypsin. Implications for the structure of human mast cell tryptase and its inhibition. M.T. Stubbs,
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n/a To be Published n/a n/a n/a
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R.G. Woodbury,
R.A. Reynolds,
B.W. Matthews,
H.Neurath
1988 Biochemistry 27 8097 3233198
3sga Structures of product and inhibitor complexes of Streptomyces griseus protease A at 1.8 A resolution. A model for serine protease catalysis. M.N. James,
A.R. Sielecki,
G.D. Brayer,
L.T. Delbaere,
C.A. Bauer
1980 J Mol Biol 144 43 6783761
4sga
5sga
3sgb Structure of the Complex of Streptomyces Griseus Protease B and the Third Domain of the Turkey Ovomucoid Inhibitor at 1.8 Angstroms Resolution R.J. Read,
M.Fujinaga,
A.R. Sielecki,
M.N. G.James
1983 Biochemistry 22 4420 n/a
3ssi Structural Modulation of the Protein Proteinase Inhibitor Ssi (Streptomyces Subtilisin Inhibitor) T.Suzuki n/a To be Published n/a n/a n/a
3tgi Comparison of Anionic and Cationic Trypsinogens: The Anionic Activation Domain is More Flexible in Solution and Differs in its Mode of Bpti Binding in the Crystal Structure A.Pasternak,
D.Ringe,
L.Hedstrom
n/a To be Published n/a n/a n/a
3tgj
4cha Structure of alpha- chymotrypsin refined at 1.68 A resolution. H.Tsukada,
D.M. Blow
1985 J Mol Biol 184 703 4046030
4est Crystallographic analysis of the inhibition of porcine pancreatic elastase by a peptidyl boronic acid: structure of a reaction intermediate. L.H. Takahashi,
R.Radhakrishnan,
R.E. Rosenfield Jr.,
E.F. Meyer Jr.
1989 Biochemistry 28 7610 2611205
5est
4gch Structure and activity of two photoreversible cinnamates bound to chymotrypsin. B.L. Stoddard,
J.Bruhnke,
N.Porter,
D.Ringe,
G.A. Petsko
1990 Biochemistry 29 4871 2364065
4htc The Refined Structure of the Hirudin- Thrombin Complex T.J. Rydel,
A.Tulinsky,
W.Bode,
R.Huber
1991 J.Mol.Biol. 221 583 n/a
4sgb Structure of the complex of Streptomyces griseus proteinase B and polypeptide chymotrypsin inhibitor-1 from Russet Burbank potato tubers at 2.1 A resolution. H.M. Greenblatt,
C.A. Ryan,
M.N. James
1989 J Mol Biol 205 201 2494344
4tpi The Refined 2.2- Angstroms (0.22-Nm) X-Ray Crystal Structure of the Ternary Complex Formed by Bovine Trypsinogen,
Valine- Valine and the Arg== 15== Analogue of Bovine Pancreatic Trypsin Inhibitor
W.Bode,
J.Walter,
R.Huber,
H.R. Wenzel,
H.Tschesche
1984 Eur. J. Biochem. 144 185 n/a
4wbc Cryocrystallography of a Serine Protease Inhibitor: The 90 K Structure of Winged Bean Chymotrypsin Inhibitor (Wci) at 2.13 A Resolution S.Ravichandran,
U.Sen,
C.Chakrabarti,
J.K. Dattagupta
1999 Acta Crystallogr., Sect.D 55 1814 n/a
5cha The refinement and the structure of the dimer of alpha- chymotrypsin at 1.67-A resolution. R.A. Blevins,
A.Tulinsky
1985 J Biol Chem 260 4264 3980476
5gch Chemistry of Caged Enzymes /II. Photoactivation of Inhibited Chymotrypsin B.L. Stoddard,
J.Bruhnke,
P.Koenig,
N.Porter,
D.Ringe,
G.A. Petsko
n/a To be Published n/a n/a n/a
5gds Hirunorms are true hirudin mimetics. The crystal structure of human alpha- thrombin- hirunorm V complex. G.De Simone,
A.Lombardi,
S.Galdiero,
F.Nastri,
R.Della Morte,
N.Staiano,
C.Pedone,
M.Bolognesi,
V.Pavone
1998 Protein Sci 7 243 9521099
5pti Structure of bovine pancreatic trypsin inhibitor. Results of joint neutron and X-ray refinement of crystal form II. A.Wlodawer,
J.Walter,
R.Huber,
L.Sjolin
1984 J Mol Biol 180 301 6210373
5ptp Solvent structure in crystals of trypsin determined by X-ray and neutron diffraction. J.S. Finer- Moore,
A.A. Kossiakoff,
J.H. Hurley,
T.Earnest,
R.M. Stroud
1992 Proteins 12 203 1557349
6cha Structure of a tetrahedral transition state complex of alpha- chymotrypsin dimer at 1.8-A resolution. A.Tulinsky,
R.A. Blevins
1987 J Biol Chem 262 7737 3584139
6est Interaction of the Peptide /Cf3- Leu- Ala- /Nh- C6H4- Cf3(/Tfla) with Porcine Pancreatic Elastase. X-Ray Studies at 1.8 Angstroms I.Li De La Sierra,
E.Papamichael,
C.Sakarelos,
J.-L.Dimicoli,
T.Prange
1990 J. Mol. Recog. 3 36 n/a
7est
6gch Structure of chymotrypsin- trifluoromethyl ketone inhibitor complexes: comparison of slowly and rapidly equilibrating inhibitors. K.Brady,
A.Z. Wei,
D.Ringe,
R.H. Abeles
1990 Biochemistry 29 7600 2271520
7gch
6pti Structure of form III crystals of bovine pancreatic trypsin inhibitor. A.Wlodawer,
J.Nachman,
G.L. Gilliland,
W.Gallagher,
C.Woodward
1987 J Mol Biol 198 469 2448484
7api The S variant of human alpha 1-antitrypsin, structure and implications for function and metabolism. R.Engh,
H.Lobermann,
M.Schneider,
G.Wiegand,
R.Huber,
C.B. Laurell
1989 Protein Eng 2 407 2785270
8api
9api
7pti Structural effects induced by removal of a disulfide- bridge: the X-ray structure of the C30A/C51A mutant of basic pancreatic trypsin inhibitor at 1.6 A. C.Eigenbrot,
M.Randal,
A.A. Kossiakoff
1990 Protein Eng 3 591 1699222
8est Reaction of porcine pancreatic elastase with 7-substituted 3-alkoxy- 4-chloroisocoumarins: design of potent inhibitors using the crystal structure of the complex formed with 4-chloro- 3-ethoxy- 7-guanidinoisocoumarin. J.C. Powers,
J.Oleksyszyn,
S.L. Narasimhan,
C.M. Kam
1990 Biochemistry 29 3108 2337582
8gch Gamma- chymotrypsin is a complex of alpha- chymotrypsin with its own autolysis products. M.Harel,
C.T. Su,
F.Frolow,
I.Silman,
J.L. Sussman
1991 Biochemistry 30 5217 2036388
8pti Crystal structure of a Y35G mutant of bovine pancreatic trypsin inhibitor. D.Housset,
K.S. Kim,
J.Fuchs,
C.Woodward,
A.Wlodawer
1991 J Mol Biol 220 757 1714504
9est Structural study of porcine pancreatic elastase complexed with 7-amino- 3-(2-bromoethoxy)- 4-chloroisocoumarin as a nonreactivatable doubly covalent enzyme- inhibitor complex. J.Vijayalakshmi,
E.F. Meyer Jr.,
C.M. Kam,
J.C. Powers
1991 Biochemistry 30 2175 1998677
9pti Crystal structure of a Y35G mutant of bovine pancreatic trypsin inhibitor C. Eigenbrot,
M. Randal,
A. A. Kossiakoff
n/a n/a n/a n/a n/a

トリプシンについてさらに知りたい方へ

以下の参考文献もご参照ください。

  • R.M. Stroud 1974 A family of protein-cutting proteins. Scientific American 231 74-88
  • R.H. Erickson and Y.S. Kim 1990 Digestion and absorption of dietary protein. Annual Review of Medicine 41 133-139



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