Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Kristian Kaufmann"'
Autor:
Gary A. Sulikowski, C. David Weaver, Darren W. Engers, Kristian Kaufmann, Craig W. Lindsley, Yu Du, Susan J. Ramos-Hunter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5195-5198
This Letter describes a novel series of GIRK activators identified through an HTS campaign. The HTS lead was a potent and efficacious dual GIRK1/2 and GIRK1/4 activator. Further chemical optimization through both iterative parallel synthesis and frag
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6de545745f9d1b33ed5215ec918d8ab6
https://doi.org/10.1016/j.bmcl.2013.07.002
https://doi.org/10.1016/j.bmcl.2013.07.002
Autor:
Yu Du, Wandong Wen, Wenjun Wu, Craig W. Lindsley, Kristian Kaufmann, Ian M. Romaine, Gary A. Sulikowski, C. David Weaver
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4562-4566
This letter describes a multi-dimensional SAR campaign based on a potent, efficacious and selective GIRK1/2 activator (~10-fold versus GIRK1/4 and inactive on nonGIRK 1-containing GIRKs, GIRK 2 or GIRK2/3). Further chemical optimization through an it
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d4b346e1f76e42ba0ccf72323640c14
https://doi.org/10.1016/j.bmcl.2013.06.023
https://doi.org/10.1016/j.bmcl.2013.06.023
Autor:
Gary A. Sulikowski, C. David Weaver, Bende Zou, Emily Days, Liya Yang, Jerod S. Denton, Greg Sliwoski, Conrado Pascual, Adam Malik, Colleen M. Niswender, Ian M. Romaine, Ryan D. Morrison, Craig W. Lindsley, Xinmin Simon Xie, Kristian Kaufmann, J. Scott Daniels, Yu Du
Publikováno v:
ACS Chemical Neuroscience. 4:1278-1286
The G-protein activated, inward-rectifying potassium (K(+)) channels, "GIRKs", are a family of ion channels (Kir3.1-Kir3.4) that has been the focus of intense research interest for nearly two decades. GIRKs are comprised of various homo- and heterote
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b25a0d66ba23e5b587a49405c0063928
https://doi.org/10.1021/cn400062a
https://doi.org/10.1021/cn400062a
Publikováno v:
Chemical Biology & Drug Design. 79:888-896
Predicting HIV-1 protease/inhibitor binding affinity as the difference between the free energy of the inhibitor bound and unbound state remains difficult as the unbound state exists as an ensemble of conformations with various degrees of flap opening
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e474a7b4816efa03cda59f45bbd89abd
https://doi.org/10.1111/j.1747-0285.2012.01356.x
https://doi.org/10.1111/j.1747-0285.2012.01356.x
Publikováno v:
Journal of Molecular Modeling
The PDZ domain is an interaction motif that recognizes and binds the C-terminal peptides of target proteins. PDZ domains are ubiquitous in nature and help assemble multiprotein complexes that control cellular organization and signaling cascades. We p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e074d90d462ad72a3d408d94e42f90f7
http://europepmc.org/articles/PMC3029681
http://europepmc.org/articles/PMC3029681
Autor:
Kristian Kaufmann, Gary A. Sulikowski, C. David Weaver, Kristopher K. Abney, Craig W. Lindsley, Yu Du, Emily Days, Shaun R. Stauffer, Ian M. Romaine
Publikováno v:
ACS chemical neuroscience. 6(6)
Ion channels are critical for life, and they are targets of numerous drugs. The sequencing of the human genome has revealed the existence of hundreds of different ion channel subunits capable of forming thousands of ion channels. In the face of this
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a27c707929b161c9a6f902b475b2307
https://pubmed.ncbi.nlm.nih.gov/25879403
https://pubmed.ncbi.nlm.nih.gov/25879403
Autor:
Xavier Pedragosa-Badia, Diana Lindner, Jens Meiler, Jan Stichel, Annette G. Beck-Sickinger, Gregory Sliwoski, Elizabeth Dong Nguyen, Kristian Kaufmann
Publikováno v:
The Journal of biological chemistry. 289(9)
Structural characterization of the human Y4 receptor (hY4R) interaction with human pancreatic polypeptide (hPP) is crucial, not only for understanding its biological function but also for testing treatment strategies for obesity that target this inte
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eff977f650542d1f72993bff104681ce
https://pubmed.ncbi.nlm.nih.gov/24375409
https://pubmed.ncbi.nlm.nih.gov/24375409
Publikováno v:
Journal of computer-aided molecular design. 27(12)
Interactions between protein domains and linear peptides underlie many biological processes. Among these interactions, the recognition of C-terminal peptides by PDZ domains is one of the most ubiquitous. In this work, we present a mathematical model
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e680650c0af2035ba70d9f6036a7b89e
https://pubmed.ncbi.nlm.nih.gov/24305904
https://pubmed.ncbi.nlm.nih.gov/24305904
Autor:
Annabelle Lejeune, André Matagne, Cécile Van de Weerdt, Nicolas Oliveira, Brent M. Dorr, Kristian Kaufmann, Jens Meiler, Joseph Martial, Maximiliano Figueroa
Publikováno v:
PLoS ONE
PLoS ONE, Vol 8, Iss 8, p e71858 (2013)
PLoS ONE, Vol 8, Iss 8, p e71858 (2013)
The computational protein design protocol Rosetta has been applied successfully to a wide variety of protein engineering problems. Here the aim was to test its ability to design de novo a protein adopting the TIM-barrel fold, whose formation requires
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ce414545c7017dcbe2cfcb0311435fb
http://europepmc.org/articles/PMC3747059
http://europepmc.org/articles/PMC3747059
Autor:
Kristian Kaufmann, Jens Meiler, Daniel Rathmann, Annette G. Beck-Sickinger, Stephanie H. DeLuca, Diana Lindner
Publikováno v:
The Journal of biological chemistry. 287(38)
The prolactin-releasing peptide receptor and its bioactive RF-amide peptide (PrRP20) have been investigated to explore the ligand binding mode of peptide G-protein-coupled receptors (GPCRs). By receptor mutagenesis, we identified the conserved aspart
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4679d089a93a4bcb81ddce2a45711158
https://pubmed.ncbi.nlm.nih.gov/22778259
https://pubmed.ncbi.nlm.nih.gov/22778259