Wenyi Li

Antimicrobial resistance (AMR) is one of the greatest threats to human health that, by 2050, will lead to more deaths from bacterial infections than cancer. New antimicrobial agents, both broad-spectrum and selective, that do not induce AMR are urgently required. Antimicrobial peptides (AMPs) are a novel class of alternatives that possess potent activity against a wide range of Gram-negative and positive bacteria with little or no capacity to induce AMR. This has stimulated substantial chemical development of novel peptide-based antibiotics possessing improved therapeutic index. This review summarises recent synthetic efforts and their impact on analogue design as well as their various applications in AMP development. It includes modifications that have been reported to enhance antimicrobial activity including lipidation, glycosylation and multimerization through to the broad application of novel bio-orthogonal chemistry, as well as perspectives on the direction of future research. The subject area is primarily the development of next-generation antimicrobial agents through selective, rational chemical modification of AMPs. The review further serves as a guide toward the most promising directions in this field to stimulate broad scientific attention, and will lead to new, effective and selective solutions for the several biomedical challenges to which antimicrobial peptidomimetics are being applied.

The tumor microenvironment (TME) is known to have a strong influence on tumorigenesis, with various components being involved in tumor suppression and tumor growth. A protumorigenic TME is characterized by an increased infiltration of tumor associated macrophages (TAMs), where their presence is strongly associated with tumor progression, therapy resistance, and poor survival rates. This association between the increased TAMs and poor therapeutic outcomes are stemming an increasing interest in investigating TAMs as a potential therapeutic target in cancer treatment. Prominent mechanisms in targeting TAMs include: blocking recruitment, stimulating repolarization, and depletion methods. For enhancing targeting specificity multiple nanomaterials are currently being explored for the precise delivery of chemotherapeutic cargo, including the conjugation with TAM-targeting peptides. In this paper, we provide a focused literature review of macrophage biology in relation to their role in tumorigenesis. First, we discuss the origin, recruitment mechanisms, and phenotypic diversity of TAMs based on recent investigations in the literature. Then the paper provides a detailed review on the current methods of targeting TAMs, including the use of nanomaterials as novel cancer therapeutics.

An efficient protocol for the selective synthesis of α-mono or α,α′-dihalo ketones <italic>via</italic> a water-controlled chemodivergent and regiospecific cascade reaction has been developed.

Abstract Dental implants are the most common therapeutic approach for resolving tooth loss and damage. Despite technical advances in treatment, implant failure rates can be as high as 23% with the major cause of peri‐implantitis: a multi‐species bacterial infection. With an annual growth rate in implant placements of 8.78% per annum, implant failure caused by bacterial infection is a significant oral and general health issue. The rise in antibiotic resistance in oral bacteria further adds pressure to implant failure; thus, there is a need for adjunctive therapy to improve implant outcomes. Due to the broad spectrum of activity and a low risk of inducing bacterial resistance, peptide antibiotics are emerging as a promising implant coating material to reduce/prevent peri‐implantitis and improve dental implant success rates. In this review, we summarised the current strategies of coating antimicrobial peptides (AMPs) onto dental implant material surfaces with multi‐functional properties to enhance osteoblast growth and prevent bacterial infections. This review compared the recent reported literature on dental implant coating with AMPs, which will provide an overview of the current dental implant coating strategies using AMPs and insights for future clinical applications.