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Peptides-Based Broad-spectrum antibiotics
Multidrug-resistant pathogens have become a major public health concern. There is a great need for the development of novel antibiotics with alternative mechanisms of action for the treatment of life-threatening bacterial infections. Antimicrobial peptides, a major class of antibacterial agents, share amphiphilicity and cationic structural properties with cell-penetrating peptides (CPPs). Herein, several amphiphilic cyclic CPPs and their analogues were synthesized and exhibited potent antibacterial activities against multidrug-resistant pathogens. Among all the peptides, cyclic peptide [R4W4] (1) showed the most potent antibacterial activity against methicillin-resistant Staphylococcus aureus [MRSA, exhibiting a minimal inhibitory concentration (MIC) of 2.67 μg/mL].
Amphiphilic peptides as a delivery tool
Antimicrobial peptides (AMPs) contain amphipathic structures and are derived from natural resources. AMPs have been found to be effective in treating the infections caused by antibiotic-resistant bacteria (ARB), and thus, are potential lead compounds against ARB. AMPs’ physicochemical properties, such as cationic nature, amphiphilicity, and their size, will provide the opportunity to interact with membrane bilayers leading to damage and death of microorganisms. Herein, AMP analogs of [R4W4] were designed and synthesized by changing the hydrophobicity and cationic nature of the lead compound with other amino acids to provide insights into a structure-activity relationship against selected model Gram-negative and Gram-positive pathogens.
InfeXtious Therapeutic using a proprietary Cyclic Peptide platform and novel small molecules. The primary focus of the company is on the clinical development of novel anti-infective therapeutic drugs with emphasis on developing antiviral peptides against SARS-COV2, herpes simplex (HSV) and human papilloma (HPV) viruses, broad-spectrum antimicrobial peptides with activity against multi-drug resistant bacteria, and antifungal peptides against Onychomycosis. InfeXtious therapeutics have developed active lead candidates for SAR-COV2, resistant Gram-positive and Gram-negative ESKAPE pathogens. Our developed cyclic peptide-based discovery platform offers a multitude of anti- infectious drug lead candidates with superior properties of selectivity, stability, and drug ability as compared to classically designed small molecules. Currently, the company collaborates with the faculty members and uses a research facility and office space at Chapman University School of Pharmacy and the University of California, Irvine, through mutual agreements. The company owns several national as well as international patents in developing antibacterial and antiviral agents.
The company’s mission is to develop tools for the delivery of oligonucleotide therapeutics. Although the delivery of oligonucleotides to the cytoplasm of the cells is significantly challenging, the company has developed a proprietary cyclic peptide platform technology that can be used for both in vitro and in vivo delivery systems. The delivery system is superior to existing delivery systems because of low toxicity, serum stability, and efficient delivery in various cells. The company has also developed a more stable, nontoxic, selective, and efficient transfecting agent as compared to commercially available transfecting agents. A number of academic laboratories are using the reagents for their particular purposes, such as the delivery of siRNA, DNA, CRISPR, and plasmid. More applications of our transfecting agents include the delivery of DNA and plasmid in the in vitro system. The cyclic peptides alone or in combination with gold nanoparticles are also used for oligonucleotide delivery in vivo.
ViImmune has a license to develop further discovered long-acting anti-HIV agents that are protected by multiple patents by our investigators. The compounds were designed as double-barreled antiviral agents to target two events in the HIV life cycle. Released parent compounds endow the conjugates with dual-action antiviral activity. The development of viral resistance to the parent drug would occur at a slower rate. This combination has resulted in the development of anti-HIV agents having enhanced efficacy, longer duration of action by the sustained intracellular release of active substrates at adequate concentrations, and higher uptake into infected cells.