Natural product–drug conjugates for modulation of TRPV1-expressing tumors

Baker, Charlotte; Rodrigues, Tiago; Almeida, Bernardo Pinto de; Barbosa‐Morais, Nuno L.; Bernardes, Gonçalo J. L.

doi:10.1016/j.bmc.2019.03.025

Cited by 7 publications

(7 citation statements)

References 30 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Looking forward, natural products and drug conjugates can be evaluated for the treatment of prostate cancers with TRPV1 overexpression. The stoichiometric combination of a TRPV1 agonist with a small, positively charged cytotoxic agent constitutes a promising avenue for prostate cancer treatment [146]. Another potential oncologic approach utilizes a gold nanorod-assisted NIR light-activated tool to open TRPV1 channels and thereby induce apoptosis [147].…”

Section: Recent Trends and Innovations In Oncologic Approaches Targeting Trpv1mentioning

confidence: 99%

Calcium Entry through TRPV1: A Potential Target for the Regulation of Proliferation and Apoptosis in Cancerous and Healthy Cells

Zhai

Líšková

Kubatka

et al. 2020

IJMS

View full text Add to dashboard Cite

Intracellular calcium (Ca2+) concentration ([Ca2+]i) is a key determinant of cell fate and is implicated in carcinogenesis. Membrane ion channels are structures through which ions enter or exit the cell, depending on the driving forces. The opening of transient receptor potential vanilloid 1 (TRPV1) ligand-gated ion channels facilitates transmembrane Ca2+ and Na+ entry, which modifies the delicate balance between apoptotic and proliferative signaling pathways. Proliferation is upregulated through two mechanisms: (1) ATP binding to the G-protein-coupled receptor P2Y2, commencing a kinase signaling cascade that activates the serine-threonine kinase Akt, and (2) the transactivation of the epidermal growth factor receptor (EGFR), leading to a series of protein signals that activate the extracellular signal-regulated kinases (ERK) 1/2. The TRPV1-apoptosis pathway involves Ca2+ influx and efflux between the cytosol, mitochondria, and endoplasmic reticulum (ER), the release of apoptosis-inducing factor (AIF) and cytochrome c from the mitochondria, caspase activation, and DNA fragmentation and condensation. While proliferative mechanisms are typically upregulated in cancerous tissues, shifting the balance to favor apoptosis could support anti-cancer therapies. TRPV1, through [Ca2+]i signaling, influences cancer cell fate; therefore, the modulation of the TRPV1-enforced proliferation–apoptosis balance is a promising avenue in developing anti-cancer therapies and overcoming cancer drug resistance. As such, this review characterizes and evaluates the role of TRPV1 in cell death and survival, in the interest of identifying mechanistic targets for drug discovery.

show abstract

Section: Recent Trends and Innovations In Oncologic Approaches Targeting Trpv1mentioning

confidence: 99%

Calcium Entry through TRPV1: A Potential Target for the Regulation of Proliferation and Apoptosis in Cancerous and Healthy Cells

Zhai

Líšková

Kubatka

et al. 2020

IJMS

View full text Add to dashboard Cite

show abstract

“…Unfortunately, changes in TRP expressions appear to be cancer-specific. For instance, TRPV1 expression is increased in HNSCC [ 3 ] and prostate cancer [ 132 ] but is markedly reduced or absent in renal cell carcinoma [ 102 ] or urothelial carcinoma [ 116 ]. Moreover, TRPV2 overexpression heralds poor prognosis in esophageal SCC [ 105 ], but identifies a subgroup of triple-negative breast cancer patients with favorable prognosis [ 114 ].…”

Section: Discussion and Future Research Directionsmentioning

confidence: 99%

“…TRPC3, TRPC4, and TRPC6 expression was described in the human breast carcinoma cell lines, TD7, MCF-7, and MDA-MB-231 [ 130 , 131 , 132 ] ( Table 1 , Table 2 ). In breast cancer, the level of TRPC1 and TRPC6 expression was similar in the noninvasive and invasive areas, regardless of the ER status.…”

Section: Trp Channels As Potential Diagnostic and Prognostic Toolsmentioning

confidence: 99%

Transient Receptor Potential (TRP) Channels in Head-and-Neck Squamous Cell Carcinomas: Diagnostic, Prognostic, and Therapeutic Potentials

Kiss

Pohóczky

Szállaśi

et al. 2020

IJMS

View full text Add to dashboard Cite

Head-and-neck squamous cell carcinomas (HNSCC) remain a leading cause of cancer morbidity and mortality worldwide. This is a largely preventable disease with smoking, alcohol abuse, and human papilloma virus (HPV) being the main risk factors. Yet, many patients are diagnosed with advanced disease, and no survival improvement has been seen for oral SCC in the past decade. Clearly, new diagnostic and prognostic markers are needed for early diagnosis and to guide therapy. Gene expression studies implied the involvement of transient receptor potential (TRP) channels in the pathogenesis of HNSCC. TRPs are expressed in normal epithelium where they play a key role in proliferation and differentiation. There is increasing evidence that the expression of TRP channels may change in HNSCC with important implications for diagnosis, prognosis, and therapy. In this review, we propose that TRP channel expression may afford a novel opportunity for early diagnosis of HNSCC and targeted molecular treatment.

show abstract

“…Library screening establishment, a systematic process for active substance identification, including sample purification and structural analysis, is essential for novel drug research. Additionally, the combination of reptile-derived anticancer components with various drug delivery system technologies such as medical implantable devices, small functional peptides, nanoparticles, liposomes, immunoliposomes, and antibody-drug conjugates (ADCs), might enable more safe and efficient pharmaceutical therapies [115][116][117][118][119][120][121]. If reptile-derived anticancer components and advanced technologies are actively fused and developed, an innovative cancer therapeutic drug platform could be organized based on a definite mechanism of action according to the individual components.…”

Section: Conclusion and Perspectives Regarding Reptile-derived Produc...mentioning

confidence: 99%

Reptiles as Promising Sources of Medicinal Natural Products for Cancer Therapeutic Drugs

2022

View full text Add to dashboard Cite

Natural products have historically played an important role as a source of therapeutic drugs for various diseases, and the development of medicinal natural products is still a field with high potential. Although diverse drugs have been developed for incurable diseases for several decades, discovering safe and efficient anticancer drugs remains a formidable challenge. Reptiles, as one source of Asian traditional medicines, are known to possess anticancer properties and have been used for a long time without a clarified scientific background. Recently, it has been reported that extracts, crude peptides, sera, and venom isolated from reptiles could effectively inhibit the survival and proliferation of various cancer cells. In this article, we summarize recent studies applying ingredients derived from reptiles in cancer therapy and discuss the difficulties and prospective development of natural product research.

show abstract

Natural product–drug conjugates for modulation of TRPV1-expressing tumors

Cited by 7 publications

References 30 publications

Calcium Entry through TRPV1: A Potential Target for the Regulation of Proliferation and Apoptosis in Cancerous and Healthy Cells

Calcium Entry through TRPV1: A Potential Target for the Regulation of Proliferation and Apoptosis in Cancerous and Healthy Cells

Transient Receptor Potential (TRP) Channels in Head-and-Neck Squamous Cell Carcinomas: Diagnostic, Prognostic, and Therapeutic Potentials

Reptiles as Promising Sources of Medicinal Natural Products for Cancer Therapeutic Drugs

Contact Info

Product

Resources

About