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Recent advancements in the field of nanotechnology have enabled targeted delivery of drug agents in vivo with minimal side effects. The use of nanoparticles for bio-imaging has revolutionized the field of nanomedicine by enabling non-invasive targeting and selective delivery of active drug moieties in vivo. Various inorganic nanomaterials like mesoporous silica nanoparticles, gold nanoparticles, magnetite nanoparticles graphene-based nanomaterials etc., have been created for multimodal therapies with varied multi-imaging modalities. These nanomaterials enable us to overcome the disadvantages of conventional imaging contrast agents (organic dyes) such as lack of stability in vitro and in vivo, high reactivity, low-quantum yield and poor photo stability. Inorganic nanomaterials can be easily fabricated, functionalised and modified as per requirements. Recently, advancements in synthesis techniques, such as the ability to generate molecules and construct supramolecular structures for specific functionalities, have boosted the usage of engineered nanomaterials. Their intrinsic physicochemical properties are unique and they possess excellent biocompatibility. Inorganic nanomaterial research has developed as the most actively booming research fields in biotechnology and biomedicine. Inorganic nanomaterials like gold nanoparticles, magnetic nanoparticles, mesoporous silica nanoparticles, graphene-based nanomaterials and quantum dots have shown excellent use in bioimaging, targeted drug delivery and cancer therapies. Biocompatibility of nanomaterials is an important aspect for the evolution of nanomaterials in the bench to bedside transition. The conduction of thorough and meticulous study for safety and efficacy in well-designed clinical trials is absolutely necessary to determine the functional and structural relationship between the engineered nanomaterial and its toxicity. In this article an attempt is made to throw some light on the current scenario and developments made in the field of nanomaterials in bioimaging., Competing Interests: Declaration of Competing Interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: STALIN DHAS reports financial support was provided by Ministry of Earth Sciences, Govt of India. STALIN DHAS reports a relationship with Ministry of Earth Sciences, Govt of India that includes: funding grants., (Copyright © 2023 Elsevier Ltd. All rights reserved.)

The current challenges in cancer treatment using conventional therapies have made the emergence of nanotechnology with more advancements. The exponential growth of nanoscience has drawn to develop nanomaterials (NMs) with therapeutic activities. NMs have enormous potential in cancer treatment by altering the drug toxicity profile. Nanoparticles (NPs) with enhanced surface characteristics can diffuse more easily inside tumor cells, thus delivering an optimal concentration of drugs at tumor site while reducing the toxicity. Cancer cells can be targeted with greater affinity by utilizing NMs with tumor specific constituents. Furthermore, it bypasses the bottlenecks of indiscriminate biodistribution of the antitumor agent and high administration dosage. Here, we focus on the recent advances on the use of various nanomaterials for cancer treatment, including targeting cancer cell surfaces, tumor microenvironment (TME), organelles, and their mechanism of action. The paradigm shift in cancer management is achieved through the implementation of anticancer drug delivery using nano routes., Competing Interests: Conflict of interest The authors have no conflict of interest., (Copyright © 2022 Elsevier Inc. All rights reserved.)

Adaptor protein 2-associated kinase 1 (AAK1) is a serine/threonine kinase that was identified as a therapeutic target for the potential treatment of neuropathic pain. Inhibition of AAK1 in the central nervous system, particularly within the spinal cord, was found to be the relevant site for achieving an antinociceptive effect. We previously reported that compound 7 is a brain-penetrant, AAK1 inhibitor that showed efficacy in animal models for neuropathic pain. One approach we took to improve upon the potency of 7 involved tying the amide back into the neighboring phenyl ring to form a bicyclic heterocycle. Investigation of the structure-activity relationships (SARs) of substituents on the resultant quinazoline and quinoline ring systems led to the identification of ( S )-31 , a brain-penetrant, AAK1-selective inhibitor with improved enzyme and cellular potency compared to 7 . The synthesis, SAR, and in vivo evaluation of a series of quinazoline and quinoline-based AAK1 inhibitors are described herein.

Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an area of significant unmet medical need. A phenotypic screen of mouse gene knockouts led to the discovery that adaptor protein 2-associated kinase 1 (AAK1) is a potential therapeutic target for neuropathic pain. The synthesis and optimization of structure-activity relationships of a series of aryl amide-based AAK1 inhibitors led to the identification of 59 , a brain penetrant, AAK1-selective inhibitor that proved to be a valuable tool compound. Compound 59 was evaluated in mice for the inhibition of μ2 phosphorylation. Studies conducted with 59 in pain models demonstrated that this compound was efficacious in the phase II formalin model for persistent pain and the chronic-constriction-injury-induced model for neuropathic pain in rats. These results suggest that AAK1 inhibition is a promising approach for the treatment of neuropathic pain.