Phoenix Phamaceuticals/G-Protein Coupled Receptor (GPCR) Peptide Ligand Library/960 peptides/L-004
商品编号：
L-004
品牌：
phoenixpeptide
市场价：
¥483420.00
美元价：
241710.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
- Storage:
- Contents:
- List of Peptides:
| Store at 4°C | |
96 well plate(s), where each well contains 1.5 nmol of peptide packaged in 15µg of BSA.(Please inquire for larger peptide quantity) | |
| Download(PDF) |
GPCR Peptide Ligand Library
Updates coming soon
GPCR Network: a large-scale collaboration on GPCR structure and function
G protein-coupled receptors (GPCRs) are targeted by ~30–40% of marketed drugs, and their key roles in normal physiology and in disease demonstrate that an understanding of their structure and function is valuable to researchers in both basic science and drug discovery. However, until recently, detailed structural information on this protein family was limited by challenges in X-ray crystallographic analysis of such membrane proteins. The GPCR Network was created in 2010 with the goal of structurally characterizing 15–25 representative human GPCRs within 5 years, based on an active outreach programme addressing an interdisciplinary community of scientists interested in GPCR structure, chemistry and biology. Here, we provide an overview of how this collaborative effort has enabled the structural determination and characterization of eight human GPCRs so far, and discuss some of the challenges that remain in gaining more detailed insights into structure–function relationships in this receptor superfamily.Stevens RC, Cherezov V, Katritch V, et al. Nat Rev Drug Discov. 2013;12(1):25-34.
A collection of nature-inspired design of domain-specific peptides
This library is being continuously updated to include all new and current peptides including GnRH(1-5) (GPR101 and GPR173), SDF-1-alpha (CXCR4 receptor), Ela-32 and Ela-21 (APJ), SCNH2/Apelin-prepropeptide(42-57), TLQP-21 (C3a or C1q receptor), D-[Lys3]GHRP-6 (CCR5), Neuronostatin (GPR107), Pepcan-12 (CB1) Fractalkine peptides, cysteine-modified or C-terminally truncated INSLs and truncated GLP-1Peptide 34 (GPR54), Fertilization promoting peptide (TCP11), Head Activator Neuropeptide (GPR37), Obestatin( GPR39), Neuromedin S, Neuropeptide S, QRFP-43, PBAN, P518, NPB & NPW, INSL 3 & 7, Endokinin A/B, AF9, BK), receptors (FM-4/TGR-1, NPSR, GPR100, GPR135, GPR142, GPR103, GPR7 & 8, LGR7 & 8, CG6986, NPR-1, PBAN-R) and references.
It has been suggested that several different active conformations of the receptor may exist dependent on the properties of the agonist. Therefore, properly selection with modified peptide ligands for a biased signalling properties may allow the development of drugs that selectively modulate only the therapeutically relevant physiological functions, thereby decreasing the risk of side effects.
Three sub-families in “Class A GPCRs” contains being recognized when comparing their amino-acid sequences. Receptors to different families share no sequence similarity. Group 1a contains GPCRs for small ligands and the receptors of the retinal/odorants/opiates/enkephalins. Group 1b contains receptors for peptides whose binding site includees the N-terminal, the the extracellular loops and superior parts of transmembranes. Group 1c contains GPCRs for glycoprotein hormones. “Class B GPCRs” have a similar morphology to group 1c but they do not share any sequence homology. Additional Class includes the family of pheromone receptors(VNs0 and family of “frizzled” and “smoothened (Smo) receptors which involved in embryonic development. Finally, the cAMP receptors (cAR) have only seen found in D. discoideum but its possible expression in vertebrate has not yet been reported.
Figure and part of texts: “The EMBO Journal (1999) 18, 1723–1729”.
This gPeptide Library (L-004) contains more than 1000 peptides. Each of the peptide has a specific property to interact at least with a known subclass of GPCRs
A schematic representation of how the two-state receptor model relates to the action of drugs as strong agonists, partial agonists, neutral competitive antagonists, inverse agonists, and inverse partial agonists. The inactive and active receptor conformations (R and R*, respectively) are in constant equilibrium.
Figure: Raymond C. Stevens et al., GPCR Network: a large-scale collaboration on GPCR structure and function. Nat Rev Drug Discov. 2013 January; 12(1): 25–34.
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品牌介绍
美国Phoenix药物集团创建于1994年，被誉为在多肽领域的黄金招牌，是这个领域的先行者和权威。
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