Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Regulatory peptides represent the most diverse and versatile family of messenger molecules. They are produced by all living organisms from bacteria to mammals. They are involved in a wide variety of biological functions. Biologically active peptides and their receptors thus constitute an unlimited source of inspiration for the development of innovative drugs and cosmetics. The present eBook is a unique collection of research articles and reviews that provide a representative examplification of the latest progress in regulatory peptide research.

G protein-coupled receptors --- Cardiovascular peptides --- Antimicrobial peptides --- Peptides and cancer --- Neuropeptides --- Gliopeptides --- Biologically active peptides --- Gastrointestinal peptides --- G protein-coupled receptors --- Cardiovascular peptides --- Antimicrobial peptides --- Peptides and cancer --- Neuropeptides --- Gliopeptides --- Biologically active peptides --- Gastrointestinal peptides

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

G protein-coupled receptors (GPCRs) are the largest class of drug targets for human diseases. An important number of them remain devoid of confirmed ligands. GPR101 is one of these orphan receptors, which constitutively activates Gs, Gq/11 and G12/13, and is expressed notably in the hypothalamus, but also in other organs such as the pituitary gland. 
Here we studied the role of extracellular loop 2 (ECL2), the longest and most diverse of the rhodopsin-like GPCRs, which contains a highly conserved cysteine through which it binds to the top of the transmembrane domain 3 (TM3). To address the function of the GPR101 ECL2, we used site-directed mutagenesis. Three mutants were designed and made: a substitution of both the cysteine at position 182 and the tryptophan at position 186, as well as a complete deletion of the ECL2 sequence. 
Using computational approaches, the ECL2 structure of GPR101 was proposed to consist of a pair of antiparallel β-sheets, which could belong to so-called “group B” of the newly established classification system for ECL2. 
At this stage, questions surrounding the function of ECL2 in GPR101 remain unanswered. Consequently, efforts need to be directed towards understanding the function of this receptor.

GPR101 --- ECL2 --- Molecular Biology --- G protein-coupled receptors --- GPCR --- Pharmacology --- Sciences du vivant > Biochimie, biophysique & biologie moléculaire

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

The human genome encompasses ≈ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth, hydromineral homeostasis and stress response. GPCRs are also major drug targets and hence possess a strong potential for the development of innovative pharmaceuticals. The aim of this Research Topic is to assemble a series of review articles and original research papers on neuropeptide GPCRs and their ligands that will illustrate the different facets of the studies currently conducted in this domain.

Neuroendocrinology. --- Neuropharmacology. --- Endocrinology. --- Animal Biochemistry --- Human Anatomy & Physiology --- Health & Biological Sciences --- Transduction pathways --- G protein-coupled receptors --- Neuroendocrinology --- Heptahelical receptors --- Neuropeptides --- Signaling mechanisms --- Biologically active peptides --- seven-transmembrane domain receptors --- Transduction pathways --- G protein-coupled receptors --- Neuroendocrinology --- Heptahelical receptors --- Neuropeptides --- Signaling mechanisms --- Biologically active peptides --- seven-transmembrane domain receptors

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

H4 R is the newest member of the histamine receptor family, which was discovered about twelve years ago. It is considered a very promising drug target. The effort to improve the pharmacokinetic properties of the currently available H4 R ligands is reflected in a steadily growing number of scientific publications and patent applications. Preclinical data strongly confirms the need for novel potent H4 R ligands to explore their therapeutic value in allergy, inflammation, autoimmune disorders, and possibly, cancer. Readers will be provided with extensive knowledge on histamine metabolism, as well as cellular histamine transport, storage and release, effects of histamine and histamine receptor ligands, with particular attention to the H4 R, on inflammatory cells including mast cells, basophils, eosinophils, neutrophils, macrophages, dendritic cells, and T cells. The present knowledge on the regulatory role of histamine and the therapeutic exploitation of histamine receptor ligands in atopic diseases, with emphasis on human and animal models of asthma, allergic dermatitis and pruritus are discussed.

Histamine. --- G protein coupled receptors, H4R ligands, Inflammation, Autoimmune Disorders, Pruritus, Asthma, Allergy, Cancer, Drug Development, Drug Target, Clinical Candidates, Biogenic Amin. --- G protein coupled receptors, H4R ligands, Inflammation, Autoimmune Disorders, Pruritus, Asthma, Allergy, Cancer, Drug Development, Drug Target, Clinical Candidates, Biogenic Amin.

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Identification and development of cancer biomarkers and targets have greatly accelerated progress towards precision medicine in oncology. Studies of tumor biology have not only provided insights into the mechanisms underlying carcinogenesis, but also led to discovery of molecules that have been developed into cancer biomarkers and targets. Multi-platforms for molecular characterization of tumors using next-generation genomic sequencing, immunohistochemistry, in situ hybridization, and blood-based biopsies have greatly expanded the portfolio of potential biomarkers and targets. These cancer biomarkers have been developed for diagnosis, early detection, prognosis, and prediction of treatment response. The molecular targets have been exploited for anti-cancer therapy and delivery of therapeutic agents. This Special Issue of Biomedicines focuses on recent advances in the discovery, characterization, translation, and clinical application of cancer biomarkers and targets in malignant diseases of the digestive system. The goal is to stimulate basic and translational research and clinical collaboration in this exciting field with the hope of developing strategies for prevention and early detection/diagnosis of cancer in digestive organs, and improving therapeutic and psychosocial outcomes in patients with these malignant diseases.

n/a --- liver graft injury --- HFE --- neurokinin --- chemotherapy --- intestinal tumors --- therapeutic targets --- biliary tract carcinoma --- hepatocellular carcinoma --- clinical trial --- cell adhesion molecules --- colorectal cancer --- biomarkers --- phenotypic mosaics --- gastrointestinal oncology --- Asian Cancer Research Group (ACRG) --- biomarker --- psychosocial support --- precision therapy --- pancreatic carcinoma --- precision medicine --- Liver transplantation --- predictive biomarkers --- CD274 --- cholecystokinin --- The Cancer Genome Atlas (TCGA) --- gastrin --- pembrolizumab --- immunotherapy --- gastrin-releasing peptide --- stereotactic body radiation therapy --- immunohistochemistry --- gastric carcinoma --- liver transplant --- CAM invasion assay --- intragraft gene expression profiles --- molecular profiling --- targeted therapy --- neurotensin --- intestinal disorder --- ramucirumab --- next-generation sequencing --- colorectal carcinoma --- tumor progenitor --- circulating tumor cells --- gastrointestinal malignancies --- bombesin --- trastuzumab --- somatostatin --- zebrafish --- G protein–coupled receptors --- G protein-coupled receptors