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Found 2 translations.
| Name | Current message text |
|---|---|
| h English (en) | [[File:The inhibitor ligand and the DPP-4 binding site.png|thumb|600px|'''Fig.3:''' The key interactions between the ligand and DPP-4 complex. The ligand's basic amine forms a hydrogen bonding network. The nitrile reacts with the catalytic active serine and forms an imidate adduct]] [[DPP-4 inhibitors]] usually have an electrophilic group that can interact with the [[hydroxyl]] of the catalytic serine in the active binding site (''Figure 3''). Frequently that group is a [[nitrile]] group but can also be [[boronic acid]] or diphenyl [[phosphonate]]. This electrophilic group can bind to the [[imidate]] [[Multiprotein complex|complex]] with [[covalent bonds]] and slow, tight-binding kinetics but this group is also responsible for stability issues due to [[Chemical reaction|reaction]]s with the free amino group of the P2-amino acid. Therefore, inhibitors without the electrophilic group have also been developed, but these [[molecule]]s have shown [[toxicity]] due to affinity to other dipeptidyl peptidases, e.g. DPP-2, [[DPP8|DPP-8]] and [[DPP9|DPP-9]]. |
| h Japanese (ja) | [[File:The inhibitor ligand and the DPP-4 binding site.png|thumb|600px|'''図3:'''リガンドとDPP-4複合体の主な相互作用。リガンドの塩基性アミンは水素結合ネットワークを形成する。ニトリルは触媒活性を持つセリンと反応し、イミデート付加物を形成する。]] [[DPP-4 inhibitors/ja|DPP-4阻害剤]]は通常、活性結合部位の触媒セリンの[[hydroxyl/ja|水酸基]]と相互作用できる親電子基を持つ（''図3''）。この基はしばしば[[nitrile/ja|ニトリル]]基であるが、[[boronic acid/ja|ボロン酸]]やジフェニル[[phosphonate/ja|ホスホネート]]でもよい。この親電子基は[[imidate/ja|イミデート]]に結合することができる。[[Multiprotein complex/ja|複合体]]と[[covalent bonds/ja|共有結合]]し、ゆっくりとしたタイトな結合速度で結合できるが、この基はP2-アミノ酸の遊離アミノ基との[[chemical reaction/ja|反応]]による安定性の問題も引き起こす。そのため、親電子基を持たない阻害剤も開発されているが、これらの[[molecule/ja|分子]]は他のジペプチジルペプチダーゼ、例えばDPP-2、[[DPP8/ja|DPP-8]]、[[DPP9/ja|DPP-9]]との親和性のために[[toxicity/ja|毒性]]を示す。 |