dTBP-3
dTBP-3 is a fully D-configured polypeptide competitive inhibitor that targets TIGIT. dTBP-3 can competitively occupy the binding interface between TIGIT and its ligand PVR, block TIGIT-mediated immunosuppressive signals, and reverse the immune exhaustion of NK cells and CD8+ T cells. dTBP-3 possesses anti-proteolytic activity and tumor tissue penetration ability, and can also enhance the tumor penetration capacity and cellular internalization efficiency of nanocarriers. dTBP-3 can be used in studies related to liver cancer, triple-negative breast cancer and non-small cell lung cancer.
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- 화학식: C70H93N21O16
- 분자량:1484.62
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
dTBP-3 can be completely released from DTBP-3NP-siANRIL within 6 h, while it remains tightly bound in the absence of GSH; in addition, dTBP-3-conjugated nanoparticles are taken up by Hep3B cells in a concentration-dependent manner, which inhibits Hep3B cell proliferation and induces apoptosis[1].
dTBP-3 conjugated with PLLD forms DTBP-PLLD, which can be liberated from PR-T@PLLD in a pH-dependent pattern and displays elevated release efficiency under acidic lysosomal and tumor microenvironment conditions[2].
dTBP-3-derived tracer [18F]TTDP binds to purified human TIGIT protein with a KD value of 40.14 nM, confirming its high-affinity targeting to human TIGIT[3].
dTBP-3 modification on PR-T@PLLD nanocarriers boosts cellular internalization and strengthens the cytotoxicity of co-loaded PTX and RC, with an IC50 value of 9.57 μg/mL at 48 h; it also facilitates efficient lysosomal escape in anti-PD-1 resistant 4T1 triple-negative breast cancer cells, and yields superior cellular uptake together with reduced lysosomal retention relative to unmodified nanocarriers[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
dTBP-3 (40 mg/kg, administered via tail vein base injection once every 3 days for a total of 5 doses) can enhance the in vivo anti-tumor effect against anti-PD-1-resistant triple-negative breast cancer via the PR-T@PLLD nanoplatform, strengthen the activity of CD8+ cytotoxic T cells, remodel the tumor immune microenvironment, and promote the secretion of pro-inflammatory cytokines; it can also induce the formation of immune memory in the body and effectively inhibit lung metastasis of triple-negative breast cancer[2].
dTBP-3 can be used to synthesize the intravenous tracer [18F]TTDP. This probe specifically targets TIGIT-positive tumor-infiltrating lymphocytes in mice and humans, shows significantly higher tumor uptake than all control groups, can quantitatively reflect the intratumoral TIGIT expression level, predict the intervention effect of combined immunotherapy, and shares the same urinary metabolic clearance pathway in rhesus monkeys as in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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분자량 1484.62
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화학식 C70H93N21O16
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Sequence
Gly-Gly-D-{Tyr-Thr-Phe-His-Trp-His-Arg-Leu-Asn-Pro}
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Sequence Shortening
GGytfhwhrlnp
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
dTBP-3 Related Classifications
HY-P11903 Related Classifications
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