| ACE2-B0AT1 |
| 🎉 New Dataset Release: Novel Ligand Designs for ACE2-B0AT1 |
|
|
| I'm excited to share that a new dataset of novel ligand designs targeting the ACE2-B0AT1 complex has been uploaded and is now publicly available. This target is generating significant excitement in the research community, particularly after the recent positive Phase I clinical trial results from MAZE Therapeutics for their SLC6A19 (the gene for B0AT1) inhibitor, MZE782 |
|
|
| . |
|
|
| You can directly access and download the dataset here: |
| 👉 https://huggingface.co/datasets/Tc-43/ACE2-B0AT1 |
| Why the ACE2-B0AT1 Target Matters |
|
|
| The ACE2-B0AT1 complex is a critical heterodimer for neutral amino acid absorption in the intestines and kidneys |
| . It has gained attention not only for its role in metabolic disorders like Hartnup disease but also as a receptor for SARS-CoV-2 |
|
|
| . |
|
|
| The biology is fascinating: B0AT1 requires a partner—ACE2 in the gut and collectrin in the kidney—to reach the cell surface and function |
|
|
| . This tissue-specific partnership is key to understanding its mechanism and therapeutic potential. |
| The Clinical Connection: MAZE Therapeutics' Breakthrough |
|
|
| The buzz around this target is well-founded. In September 2025, Maze Therapeutics announced positive first-in-human results for MZE782, an oral SLC6A19 inhibitor |
|
|
| . |
|
|
| The Phase I data was compelling |
|
|
| : |
|
|
| Proof of Mechanism: The drug showed a dose-dependent, massive increase (up to a 42-fold rise) in urinary phenylalanine excretion, confirming potent target engagement. |
| |
| Therapeutic Potential: MZE782 is being developed as a potential best-in-class therapy for Phenylketonuria (PKU) and a first-in-class treatment for Chronic Kidney Disease (CKD). |
| |
| Safety: It demonstrated an excellent safety profile in healthy volunteers, supported by the generally benign nature of Hartnup disorder, which also involves reduced SLC6A19 function |
| |
| . |
| |
| About the Dataset |
|
|
| This resource provides computational chemists, structural biologists, and drug discovery researchers with a set of novel ligand designs to explore. Investigating these ligands could accelerate the development of new therapeutics for kidney and metabolic diseases by targeting this pivotal pathway. |
|
|
| Download, experiment, and let me know what you discover! I'd love to hear your thoughts and feedback. |
