Pharmacological analysis of four mutant receptors compared with wild-type GLP-1R: Lys-288–Ala4.64, Asn-300–AlaECL2, Trp-306–Ala5.36 or Arg-310–Ala5.40.

Slides:

Advertisements

Similar presentations

1.The trp repressor is made of: A)DNA B)RNA C)Protein D)None of the above.

Advertisements

Quantifying the drug-target binding affinity. Receptors as targets (Receptors are 45% of current drug targets) Receptors are areas of proteins found in.

Arginine, who are you? Why so important?. Release 2015_01 of 07-Jan-15 of UniProtKB/Swiss-Prot contains sequence entries, comprising

Selective inhibition of BCL10-induced NF-κB activation by Tat–Peptide VIII HEK-293 cells were transiently co-transfected with an expression vector encoding.

Control of Gene Expression

Transcriptional Regulation

Phosphorylation of serine 73 targets SREBP-1c for ubiquitination and proteasomal degradation Phosphorylation of serine 73 targets SREBP-1c for ubiquitination.

Modulation by aspirin of nuclear phospho–signal transducer and activator of transcription 6 expression: Possible role in therapeutic benefit associated.

Figure 3.14A–D Protein structure (layer 1)

Volume 125, Issue 3, Pages (September 2003)

Figure 5 In vitro characterization of the Y290F and T269M GNRHR mutations. A: Competitive binding curves for the Y290F and T269M GNRHR mutants compared.

Vemuri B. Reddy, PhD, Thomas A

Volume 25, Issue 8, Pages e4 (August 2017)

Young Kwon, Thomas Hofmann, Craig Montell Molecular Cell

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2 by Zil E. Huma, Julie Sanchez,

SP1 was a downstream target of miR-150-3p

AGL15 Interacts in a Sequence-Specific Manner with a Noncanonical CArG Motif Present in the Regulatory Region of AtGA2ox6.(A) Enrichment of the AtGA2ox6.

Approaches to signal transduction:

The Pattern Recognition Receptor NOD2 Mediates Staphylococcus aureus–Induced IL- 17C Expression in Keratinocytes Sarah A. Roth, Maren Simanski, Franziska.

Volume 22, Issue 6, Pages (June 2015)

Differentiation-induced changes in Tfam mRNA stability (A) The nt sequence corresponding to the 3′-UTR of mouse Tfam is illustrated. Differentiation-induced.

Amy R Mohn, Raul R Gainetdinov, Marc G Caron, Beverly H Koller Cell

Vemuri B. Reddy, PhD, Thomas A

Volume 19, Issue 5, Pages (March 2009)

RBPJ Mutations Identified in Two Families Affected by Adams-Oliver Syndrome Susan J. Hassed, Graham B. Wiley, Shaofeng Wang, Ji-Yun Lee, Shibo Li, Weihong.

Volume 6, Issue 5, Pages (May 1997)

Structure of the Human Transferrin Receptor-Transferrin Complex

Volume 25, Issue 3, Pages (February 2015)

Volume 6, Issue 5, Pages (May 1997)

A Cluster of Cytoplasmic Histidine Residues Specifies pH Dependence of the AE2 Plasma Membrane Anion Exchanger Israel Sekler, Sumire Kobayashi, Ron R.

Volume 25, Issue 8, Pages e4 (August 2017)

Yongsheng Ma, Eric Carter, Xiaomei Wang, Chang Shu

Signaling Cell Fate in Plant Meristems

Changes in transcript abundance of the TR-ACS gene family in white clover roots over 24 h in response to Pi supply Changes in transcript abundance of the.

XIST regulated miR-29c by directly targetting in TMZ-resistant glioma cells XIST regulated miR-29c by directly targetting in TMZ-resistant glioma cells.

Volume 19, Issue 9, Pages (September 2012)

Pharmacological Characterization of Loss of Function Mutations of the Human Melanocortin 1 Receptor That Are Associated with Red Hair Aneta Ringholm,

Overexpression of miR-340 inhibited osteoclast differentiation

Volume 22, Issue 11, Pages (November 2015)

Volume 21, Issue 3, Pages (March 2013)

Volume 17, Issue 10, Pages (October 2010)

Volume 18, Issue 5, Pages (May 2011)

Jillian G. Baker, Stephen J. Hill Trends in Pharmacological Sciences

M. Jonsson Fagerlund, J. Sjödin, J. Krupp, M.A. Dabrowski

Volume 59, Issue 5, Pages (May 2001)

Jiaxin Hu, Jing Liu, David R. Corey Chemistry & Biology

The Pro162 Variant is a Loss-of-Function Mutation of the Human Melanocortin 1 Receptor Gene Celia Jiménez-Cervantes, Concepción Olivares, Petra González,

Volume 58, Issue 2, Pages (August 2000)

Biochemical characterization of motif VI mutants—R592A and H594A

Figure 2 SORL1 mutants' overexpression increases β-amyloid secretion

Volume 21, Issue 10, Pages (October 2014)

Proposed model of signalling pathways involved in RBC shrinkage and vesiculation Inhibition of the depicted kinases induces shrinkage and vesiculation.

NFAT5 is transcriptionally active in skeletal muscle cells in vitro.

The recombinant Puf4 pumilio domain (Puf4-PD) binds to PUF consensus elements in HXL1 mRNA. The recombinant Puf4 pumilio domain (Puf4-PD) binds to PUF.

MiR-431-5p directly targets RAF1 and is negatively correlated to RAF1 expression (A) The predicted binding sites of miR-431-5p and RAF1 3′-UTR, and mutant.

FBXL19-AS1 acts as a sponge of miR-431-5p in lung cancer (A) The predicted binding sites of FBXL19-AS1 and miR-431-5p, and the mutant sites in mutant-type.

TSC1 knockdown enhances hypoxia-mediated lymphocyte death via mTORC1 activation TSC1 knockdown enhances hypoxia-mediated lymphocyte death via mTORC1 activation.

Thermostability of A2AR–SMALP and DDM-solubilized A2AR from P

Hypoxia decreases lipogenesis via mTORC1 signalling in lymphocytes

Volume 3, Issue 2, Pages (February 2006)

Figure 2. p62−/−MEF cells enhance the activation of NF-κB induced by TLR4. (A) Wild-type (WT) p62+/+MEF and p62−/−MEF cells were transfected with pBIIx-luc.

Hyperoxidation of ERp57 is intensified by removal of regulatory disulfide bonds in Ero1β (A–C) Where indicated, expression of Ero1β variants was induced.

Allosteric Regulation of NCLX by Mitochondrial Membrane Potential Links the Metabolic State and Ca2+ Signaling in Mitochondria Marko Kostic, Tomer Katoshevski,

Volume 89, Issue 3, Pages (May 1997)

Fig. 3 Organization of the active site of DHHC20.

FBXL19-AS1 knockdown inhibits proliferation, migration and invasion, and reduces the expression levels of angiogenesis related proteins in lung cancer.

Volume 15, Issue 11, Pages (November 2008)

Hcy decreases VEGFR1/2 and Angs (Ang1, Ang2) gene transcription

Fig. 2 Characterizing GLP1R signaling pathways and pharmacology activated by eGLP1-MALAT1-ASO (•) and eGLP1-FOXO1-ASO (▪) compared to eGLP1 peptide (○)

The cytotoxicity of Bacillus subtilis or surfactin in IPEC-J2 cells.

Presentation transcript:

Pharmacological analysis of four mutant receptors compared with wild-type GLP-1R: Lys-288–Ala4.64, Asn-300–AlaECL2, Trp-306–Ala5.36 or Arg-310–Ala5.40 Pharmacological analysis of four mutant receptors compared with wild-type GLP-1R: Lys-288–Ala4.64, Asn-300–AlaECL2, Trp-306–Ala5.36 or Arg-310–Ala5.40 (A) Concentration–response curves for GLP-1-induced cAMP accumulation in Flp-In HEK293 cells. US, unstimulated (no GLP-1 added). (B) Radioligand competition binding curves, using 75 pM 125I-EX4(9–39) and unlabelled GLP-1 as competitor, for membranes derived from Flp-In HEK293 cells expressing either wild-type GLP-1R or one of four single site mutant receptors. Replicates are in triplicate with errors representing S.E.M. Rachel L. Dods, and Dan Donnelly Biosci. Rep. 2016;36:e00285 ©2016 by Portland Press Ltd