Prokineticin Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
Prokineticins are multifunctional chemokine-like peptides that were found in the venom of the Black Mamba and the cutaneous secretions of yellow-bellied toads. A complex system made up of two ligands (PROK1 and PROK2) that bind to two GPCRs (PROKR1 and PROKR2) with similar ranges of affinities was discovered throughout the research on this family of peptides. There are prokineticins and their receptors in many different human tissues. They exhibit a wide spectrum of tissue-specific biological actions, and their regulation and cellular distribution differ significantly from tissue to tissue. Furthermore, they play a role in neuron migration and survival, angiogenesis, haematopoiesis, and inflammation in addition to being able to control complex behaviors including eating, drinking, circadian rhythm, and hyperalgesia.
Fig.1. The physiological functions of prokineticin family. (Monnier & Samson, 2010)
Creative Biolabs is a world-leading provider in membrane protein drug discovery. We can offer prokineticin family drug discovery tools with the best quality:
Overview of Prokineticin Family
The amino acid sequences of the two GPCRs for prokineticins, ROKR1 and PROKR2, have an overall similarity of 85%, with the majority of differences occurring at the N-terminal. PROKR2 has 384 amino acids compared to PROKR1's 393 amino acids. Both receptors can bind to and be activated by PROK1 and PROK2. Although PROKR1 marginally outperforms PROKR2 in terms of signal transduction efficiency. It has been demonstrated that PROKR activation results in inositol phosphate buildup and the mobilization of intracellular Ca2+ by Gq/11 proteins. Additionally, PROKRs can influence cAMP accumulation by activating or inhibiting Gi or Gs proteins, respectively. Additionally, it has been demonstrated that PROKRs release G protein βγ subunits and phospholipase Cβ as well as activate mitogen-activated protein kinase (MAPK) via Go protein-mediated signaling.
Fig.2. The diagram of PROKR2 mutations. (Zhao, 2019)
Platelet-activating Factor Family Drug Discovery
Prokineticin receptors are potential targets for drugs which block the nociceptive information before it reaches the brain. Prokineticins can actively take part in the carcinogenesis process by acting as an angiogenic and chemotactic factor for pro-inflammatory neutrophils, as well as a growth factor for cancer cells. Prokineticins may also play a role in other cancers that have not yet been fully characterized, including leukemias because monocytic/granulocytic lineage cells in the bone marrow express them at high levels and brain cancer because they are critical growth factors for the olfactory bulb's nerve cells.
References
- Monnier, J.; Samson, M. Prokineticins in angiogenesis and cancer. Cancer letters. 2010, 296(2), 144-149.
- Zhao, Y.; et al. Prokineticins and their G protein-coupled receptors in health and disease. Progress in Molecular Biology and Translational Science. 2019, 161, 149-179.