Function and mechanism of action of the TRPV1 channel in the development of triple-negative breast cancer.

Transient receptor potential channel subfamily vanilloid 1 (TRPV1) is a member of the transient receptor potential family of nonselective cationic transmembrane channel proteins that are involved in the regulation of calcium homeostasis. It is expressed in various tumor types and has been implicated in the regulation of cancer growth, metastasis, apoptosis, and cancer-related pain. TRPV1 is highly expressed in triple-negative breast cancer (TNBC), and both its agonists and antagonists may exert anti-cancer effects. In this review, we provide an overview of the effect of TRPV1 on TNBC development and its influence on immunotherapy in an attempt to facilitate the development of future treatment strategies.

In situ stimulus-responsive self-assembled nanomaterials for drug delivery and disease treatment.

The individual motifs that respond to specific stimuli for the self-assembly of nanomaterials play important roles. In situ constructed nanomaterials are formed spontaneously without human intervention and have promising applications in bioscience. However, due to the complex physiological environment of the human body, designing stimulus-responsive self-assembled nanomaterials in vivo is a challenging problem for researchers. In this article, we discuss the self-assembly principles of various nanomaterials in response to the tissue microenvironment, cell membrane, and intracellular stimuli. We propose the applications and advantages of in situ self-assembly in drug delivery and disease diagnosis and treatment, with a focus on in situ self-assembly at the lesion site, especially in cancer. Additionally, we introduce the significance of introducing exogenous stimulation to construct self-assembly in vivo. Based on this foundation, we put forward the prospects and possible challenges in the field of in situ self-assembly. This review uncovers the relationship between the structure and properties of in situ self-assembled nanomaterials and provides new ideas for innovative drug molecular design and development to solve the problems in the targeted delivery and precision medicine.

Amphiphilic BODIPY dye aggregates in polymeric micelles for wavelength-dependent photo-induced cancer therapy.

Near-infrared (NIR) light-responsive nanoparticles of organic small-molecule dyes hold great promise as phototherapeutic dyes (PDs) for clinical translation due to their intrinsic merits, including well-defined structure, high purity, and good reproducibility. However, they have been explored with limited success in the development of photostable NIR PDs with extraordinary photoconversion for highly effective phototherapy. Herein, we have described amphiphilic BODIPY dye aggregates within the polymeric micelles (Micelles) as potent bifunctional PDs for dually cooperative phototherapy under NIR irradiation. Micelles possessed an intensive NIR absorption, high photostability, and favorable non-radiative transition, thereby exhibiting both remarkable singlet oxygen generation and photothermal effect under NIR light irradiation. Besides, Micelles had preferable cellular uptake, effective cytoplasmic drug translocation as well as enhanced tumor accumulation. Owing to the combined virtues, Micelles showed clinical potential as bifunctional PDs for photo-induced cancer therapy. This work thus provides a facile strategy to exploit advanced PDs for practical phototherapeutic applications.

Rational Design of Conjugated Photosensitizers with Controllable Photoconversion for Dually Cooperative Phototherapy.

High-performance photosensitizers are highly desired for achieving selective tumor photoablation in the field of precise cancer therapy. However, photosensitizers frequently suffer from limited tumor suppression or unavoidable tumor regrowth due to the presence of residual tumor cells surviving in phototherapy. A major challenge still remains in exploring an efficient approach to promote dramatic photoconversions of photosensitizers for maximizing the anticancer efficiency. Here, a rational design of boron dipyrromethene (BDP)-based conjugated photosensitizers (CPs) that can induce dually cooperative phototherapy upon light exposure is demonstrated. The conjugated coupling of BDP monomers into dimeric BDP (di-BDP) or trimeric BDP (tri-BDP) induces photoconversions from fluorescence to singlet-to-triplet or nonradiative transitions, together with distinctly redshifted absorption into the near-infrared region. In particular, tri-BDP within nanoparticles shows preferable conversions into both primary thermal effect and minor singlet oxygen upon near-infrared light exposure, dramatically achieving tumor photoablation without any regrowth through their cooperative anticancer efficiency caused by their dominant late apoptosis and moderate early apoptosis. This rational design of CPs can serve as a valuable paradigm for cooperative cancer phototherapy in precision medicine.