Current Pharmaceutical Design - Volume 16, Issue 9, 2010

The production of new molecular entities endowed with salutary medicinal properties is a formidable challenge; synthetic molecules that can bind with high sequence specificity to a chosen target in a protein or gene sequence are of major interest in medicinal and biotechnological contexts. The general awareness of the importance of peptides in physiology and pathophysiology has markedly increased over the last few years Read More

Antimicrobial peptides are major components of the innate immune defence. They are well conserved along evolution, nontoxic and they ensure potent defences against a large number of pathogens. They act by direct killing of microorganisms and they possess additional roles in the regulation of adaptive immune responses, by recruting or stimulating immune cells. Skin and gut are positioned at the interface of inter Read More

Cancer has become the number one cause of death amongst Americans, killing approximately 1,600 people per day. Novel methods for early detection and the development of effective treatments are an eminent priority in medicine. For this reason, isolation of tumor-specific ligands is a growing area of research. Tumor-specific binding agents can be used to probe the tumor cell surface phenotype and customize treatme Read More

Membrane proteins account for approximately one third of all proteins in eukaryotic and prokaryotic cells. These proteins are critical in a diverse array of cellular functions. Despite their obvious importance, the effectiveness of research tools to study the structure and function of integral membrane proteins lags behind that of water-soluble proteins. This is due in part to the lack of probing agents that can specifically and s Read More

Toll-like receptors (TLRs) are a family of key proteins that permit mammals to detect microbes and endogenous molecules, which are present in body fluids, cell membranes and cytoplasm. They confer mechanisms to the host for maintaining homeostasis, activating innate immunity and inducing signals that lead to the activation of adaptive immunity. TLR signalling induces the expression of pro-inflammatory and anti-vira Read More

The function of the Toll-like receptor (TLR) family members has been extensively studied in the recent decades. The TLR family is generally involved in the defense against microbial infections. TLRs are expressed mainly on macrophages and dendritic cells (DCs) and activate these cells upon ligand binding. The activation of TLRs basically initiates innate immune response, but can also induce adaptive immune response. TLRs h Read More

The autonomous nervous system of the gut is increasingly recognized as an important regulatory factor in intestinal permeability and immune cell activation. Neuropeptides released by neurons -or inflammatory cells- have emerged as neuro-immune modulators that can relay, for instance, stress-induced neuronal activity to immune processes. Such peptides can participate in processes reducing inflammatory responses, or Read More

Androgen receptor (AR) is a steroid hormone receptor that is activated by endogenous androgens, mainly testosterone and 5α- dihydrotestosterone (5α-DHT). AR is also an important drug target, and AR antagonists (antiandrogens) have been widely used for prostate cancer therapy. Antiandrogens currently available on the market are all small molecules that antagonize AR function via binding to the ligand bi Read More

Cyclic nucleotide phosphodiesterase (PDE), that is a multigenic enzyme superfamily ubiquitously distributed in mammalians, mainly contributes to intracellular signaling regulation. Its various isozymes specifically control in a spatio-temporal manner intracellular levels of cAMP and cGMP downstream receptor activation and nearby functional proteins. The PDE superfamily is constituted by 11 gene families (PDE1-PDE11), c Read More

Opioid receptors and opioid peptides constitute the endogenous opioid system. The most relevant function of the opioid system seems to be the inhibitory modulation of nociceptive information at supraspinal, spinal and peripheral sites, although it is also implicated in the modulation of many other processes in the body. Centrally acting plant opiates, such as morphine, are the most frequently used analgesics for the relief of s Read More

Current pharmacologic treatments for inflammatory diseases are largely palliative rather than curative. Most of them result in nonspecific immunosuppression. This can be associated with disruption of natural and induced immunity with significant, sometimes dramatic, adverse effects. Among the novel strategies that are under development, tools that target specific molecular pathways and cells, and more precisely mo Read More

Viruses need to deliver their genomic information into the host cell lumen to establish productive infection. Enveloped viruses accomplish this task by fusing their membrane with a host cell membrane. Membrane fusion is facilitated by specialized viral membrane proteins, which mediate binding and entry into host cells. The architecture of the fusion machinery of envelope proteins can differ between viruses, and class I, II Read More

The heart is a sophisticated endocrine gland synthesizing a family of peptide hormones by three different genes. These cardiac hormones are stored as 3 prohormones, i.e. atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP) and C-type natriuretic peptide (CNP) prohormones. Within the ANP prohormones are 4 peptide hormones, i.e. atrial natriuretic peptide, vessel dilator, kaliuretic peptide and long-acting natr Read More

Peptides, polypeptides, and proteins have been extensively studied for their various structural and functional roles in living organisms. However, breakthrough discoveries in the last decades identified some peptide-based matrices that posses the ability to traverse biological membranes, and many peptides, polypeptides and even complete proteins have been shown to have such properties. Hence, these matrices have been s Read More