Market Intelligence, Clinical Progress, and High-Purity Reagents for Inflammation and Oncology Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for ADAM17 drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | ADAM17 ECD-Fc / Catalytic Domain Protein High purity (>95%), Endotoxin <1EU/ug, Sequence Verified, HEK293 Expressed (Native Glycosylation). |
View ADAM17 Products |
| Catalytic Mutant | ADAM17 E406A (Catalytic Dead) Mutant Protein For mechanism-of-action studies (binding vs. enzymatic). Sequence Verified. |
View ADAM17 Products |
| Gene Delivery | ADAM17 Promise-ORF / Lentivirus Full-length ORF for stable cell lines; preserves native membrane topology for shedding assays. |
View ADAM17 Products |
| Benchmark Ab | Anti-ADAM17 (Reference Sequence) Recombinant positive control for ELISA, SPR, blocking assays. Sequence Verified. |
View ADAM17 Products |
| Validator | ADAM17 siRNA Set For knockdown verification and background specificity controls. |
View ADAM17 Products |
| ADAM10 | ADAM10/CD156c – Closest homolog; essential for selectivity counter-screening (toxicity avoidance). | View ADAM10 Products |
| TNF-α | TNF-α / TNFSF2 – Primary substrate; for functional shedding assays. | View TNF-α Products |
| HER3 | HER3/ErbB3 – ADAM17 substrate; evaluates EGFR inhibitor resistance bypass mechanisms. | View HER3 Products |
| EGFR | EGFR – Downstream signaling partner for combination therapy research. | View EGFR Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| ADAM10/ADAM17 Selectivity | Human ADAM10 and ADAM17 ECD proteins with distinct disintegrin domains, verified by Mass Spec for precise counter-screening. |
| Catalytic vs. Allosteric Binding | Active WT and E406A Catalytic Dead mutant pair available for mechanism-of-action studies (differentiate active-site vs. allosteric). |
| Shedding Activity Quantification | Full-length Lentivirus for cell-based substrate cleavage assays (TNF-α release detection); native membrane topology ensures physiological relevance. |
| Cross-species Translation | Human / Cynomolgus / Mouse ADAM17 ortholog proteins with >95% purity for PK/PD modeling and toxicity studies. |
| False Positives / Off-target Binding | Validated siRNA included for target-specificity confirmation in cell-based formats. |
| Lack of Reliable Controls | Clinical Benchmark Antibodies (biosimilars) and inactive mutant controls provided. |
Live ADAM17 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for ADAM17 (TACE) therapeutics has shifted from broad-spectrum metalloproteinase inhibitors (associated with musculoskeletal toxicity due to ADAM10/MMP off-target effects) toward highly selective modalities. First-generation small molecules (e.g., from BMS, AstraZeneca, Novartis) failed in clinical trials because of unavoidable inhibition of closely related proteases. Current R&D focuses on allosteric sites, monoclonal antibodies targeting non-catalytic domains, conditionally active biologics (tumor-microenvironment-specific), and antibody-drug conjugates (ADCs). The next frontier involves combination strategies with EGFR inhibitors to overcome acquired resistance in solid tumors, as ADAM17-mediated shedding of TGF-α and amphiregulin drives bypass signaling. Additionally, host-directed antiviral applications (e.g., modulating ACE2 shedding in COVID-19) are emerging.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Selective Small Molecule (Allosteric) | AstraZeneca, iMetabolic Biopharma, Academic Consortia | Rheumatoid Arthritis, Inflammation, Solid Tumors | Selectivity Panel (ADAM10/ADAM17/MMPs) with purified proteins and mutant controls. |
| Allosteric Antibody / Biologic | Major Pharma, Emerging Biotechs | IBD, RA, Oncology | Epitope mapping & blocking assay using conformational ECD-Fc (HEK293, native glycosylation). |
| Conditionally Active Biologics | Emerging Biotechs | Tumor-microenvironment-specific Oncology | pH-dependent binding assay (pH 6.0 vs 7.4); need stable full-length cell lines. |
| Blocking Antibody | Emerging Biotechs | Solid Tumors | Internalization assay for ADC; high-purity ECD-Fc for affinity characterization. |
| ADC | Oncology-Focused Biotechs | Solid Tumors (e.g., NSCLC, CRC) | Shedding-dependent cytotoxicity assay (need stable full-length cell lines via Lentivirus). |
| Host-Directed Antiviral | Emerging Programs | Viral infections (e.g., COVID-19) | Shedding assay for ACE2; full-length Lentivirus cell lines. |
ADAM17 Molecular Biology & Key Mutations
ADAM17 (CD156b; UniProt P78536) is a type I transmembrane sheddase composed of several functional domains: a Peptidase M12B domain (catalytic) and a Disintegrin domain (critical for integrin interactions). Key naturally occurring mutations in the human population include dbSNP:rs34431503 and dbSNP:rs2230818, which may affect protein stability or substrate specificity. Researchers developing selective inhibitors or antibodies must account for these variants and ensure assays use recombinant proteins carrying the appropriate allele. TarMart's sequence-verified reagents (WT and E406A catalytic dead mutant) cover both common variants and enable precise mechanism-of-action studies.