Technologies– テクノロジー –

Creating the future of GPCR drug discovery based on the proprietary technologies specialized in GPCR-targeted antibodies

GPCR-Targeted Antibody – GPCRを標的とした抗体

GPCR-Targeted Drug Discovery – GPCRを標的とした創薬

GPCRs have been shown to be associated with a variety of diseases and are one of the attractive target molecules for drug development. Drugs targeting GPCRs have been applied to metabolic diseases, cardiovascular diseases, autoimmune diseases, respiratory diseases, central nervous system diseases, and others. They continue to account for a high percentage of new drug sales and numbers of products in the global market.

GPCR は様々な疾患との関連性が示されており、医薬品を開発する上で重要な標的分子群の1つです。GPCR を標的とした医薬品は、代謝性疾患、循環器疾患、自己免疫、呼吸器疾患、中枢性疾患などに応用され、グローバルマーケットにおいて新薬の売上高および売上品目数で依然として高い割合を占めています。

  • A membrane protein that controls various cell functions
  • There are about 800 types of GPCRs in the body
  • Structure and function of each GPCR are similar
  • Drug discovery targeting GPCRs is difficult due to their complex

  • 様々な細胞の機能をコントロールする膜タンパク質
  • からだの中には、約800種類のGPCRが存在している
  • それぞれのGPCRは構造や働き方が類似している
  • 複雑な構造のために、GPCRを標的とする創薬は難しい
  • Dysfunction of specific GPCRs causes specific diseases
  • Correlations between various GPCRs and diseases have been demonstrated
  • GPCRs are Involved in various diseases such as intractable rare diseases, lifestyle-related diseases, and cancer 
  • •GPCR drug discovery is mainstream  of new drug development

  • 特定のGPCRの機能異常が特定の病気の原因
  • 様々なGPCRと病気の関係が明らかになってきている
  • 難治性希少疾患、生活習慣病、ガンなど様々な疾患に関与
  • GPCR創薬は新薬開発の王道

However, in recent years, the probability of launching GPCR-targeted low molecular weight compounds has clearly continued to decline.


Difficulties in GPCR-Targeted Antibody Development – GPCR標的抗体開発の困難性

In addition to its high efficacy and safety, therapeutic monoclonal antibodies are steadily increasing their global sales due to the commoditization of commercial mass manufacturing technology.
On the other hand, the depletion of target molecules for new antibody drugs is becoming apparent.


GPCR-targeted antibodies have emerged as a growth market due to the declining probability of GPCR drug discovery using low molecular weight compound and the trend toward depletion of new target molecules in antibody drug development.
However, GPCR-targeted antibodies are said to be difficult to develop due to the high steep hurdles involved in drug discovery technology.

低分子化合物による GPCR 創薬の上市確率低下、抗体医薬開発における新規標的分子の枯渇傾向という状況から、GPCR標的抗体は成長市場として顕在化してきました。

Issues in GPCR-Targeted Antibody Development – GPCR標的抗体開発の課題

  1. Difficult to purify while maintaining the same 3D structure as natural GPCR
  2. Limited region of cell surface accessible to antibodies
  3. Low expression of target GPCRs per target cell
  4. Difficult to get the specific binder to target GPCR
  5. No standard method for efficient screening of antibodies has been established
  6. No Efficient humanization and optimization methods for antibody have been established
  1. 天然GPCRと同じ立体構造を保持した状態での精製困難
  2. 抗体がアクセスできる細胞表面の露出部分が限定的
  3. 細胞当たりの標的GPCRの発現が少ない
  4. 標的GPCRへの結合特異性を出すことが困難
  5. 抗体を効率的にスクリーニングする標準方法が未確立
  6. 効率的な抗体のヒト化、最適化手法が未確立

MoGRAA® Discovery Engine – MoGRAA® ディスカバリーエンジン

To overcome issues in GPCR-targeted antibody development,
we have developed a unique drug discovery exploration platform,
MGRAA® Discovery Engine.

What is MoGRAA® ?- MoGRAA®とは?

Controlling the function of the GPCR using antibodies
抗体を用いて GPCR の機能を制御する

Modification of G-protein coupled Receptor Activation with Monoclonal Antibody

MoGRAA® is an abbreviation for Modification of G-protein coupled Receptor Activation with monoclonal Antibody. It is representative of the concept of a new antibody drug that we propose as “regulating the function of GPCRs with monoclonal antibodies.”

MoGRAA®とは、Modification of G-protein-coupled receptor activation with monoclonal antibodyを意味する略語で、当社が提唱する新しい抗体医薬品のコンセプトである、『モノクローナル抗体によりGPCRの機能を調節する』ということを表しています。

MoGRAA® Discovery Engine – MoGRAA® ディスカバリーエンジン

Accumulating cutting-edge technology and know-how specialized in GPCR-targeted antibody

MoGRAA® Discovery Engine

MoGRAA® Discovery Engine is our drug discovery platform for GPCR-targeted antibody.
The MoGRAA® Discovery Engine enables the efficient acquisition of monoclonal antibodies that bind specifically to target GPCRs.

MoGRAA® ディスカバリーエンジンは、当社が開発したGPCR標的抗体取得のための創薬探索プラットフォームです。
MoGRAA® ディスカバリーエンジンにより、標的 GPCRに特異的に結合するモノクローナル抗体を効率的に取得することが可能です。

Features of MoGRAA® Discovery Engine – MoGRAA® ディスカバリーエンジンの特徴

  • Discovery of target GPCRs
  • Ingenuity of immunization method
  • Optimization of screening method
  • Efficiency of functionality evaluation
  • Antibody structure optimization technology
  • 標的GPCRの探索
  • 免疫方法の工夫
  • スクリーニング法の最適化
  • 機能性評価の効率化
  • 抗体構造の最適化技術

Advantages of MoGRAA® Discovery Engine – MoGRAA® ディスカバリーエンジンの優位性

  • Ability to obtain antibodies against various GPCR subtypes
  • Simultaneous development of multiple themes is possible with efficient lead antibody development technology
  • Strength in acquiring antagonist antibodies against low-molecular-weight ligands (lipid ligands)
  • Developable for useful antibodies against target GPCRs which have unknown structures and no surrogate antibodies
  • 様々なGPCRサブタイプに対し抗体取得が可能
  • リード抗体取得の省⼒化、効率化により、複数のテーマの同時開発が可能
  • 低分⼦リガンド(脂質リガンド)のアンタゴニスト抗体取得に強み
  • 構造未知、サロゲート抗体がない標的に対しても有⽤抗体開発が可能

NBHL is actively seeking collaboration opportunities.