X-ray structure based evaluation of analogs of citalopram: Compounds with increased affinity and selectivity compared with R-citalopram for the allosteric site (S2) on hSERT

Autor: Connie Sanchez, Krestian Larsen, Peter Bregnedal, Benny Bang-Andersen, Sid Topiol, Klaus Peter Bogeso, Claus J. Loland, Per Plenge, Karsten Juhl

Publikováno v: Topiol, S, Bang-Andersen, B, Sanchez, C, Plenge, P, Loland, C J, Juhl, K, Larsen, K, Bregnedal, P & Bogeso, K P 2017, ' X-ray structure based evaluation of analogs of citalopram : Compounds with increased affinity and selectivity compared with R-citalopram for the allosteric site (S2) on hSERT ', Bioorganic & Medicinal Chemistry Letters, vol. 27, no. 3, pp. 470-478 . https://doi.org/10.1016/j.bmcl.2016.12.037

The recent publication of X-ray structures of SERT includes structures with the potent antidepressant S-Citalopram (S-Cit). Earlier predictions of ligand binding at both a primary (S1) and an allosteric modulator site (S2), were confirmed. We provide

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eca2a6464758e5090d22cef076850aa6
https://doi.org/10.1016/j.bmcl.2016.12.037

Structure-activity relationship studies of citalopram derivatives: examining substituents conferring selectivity for the allosteric site in the 5-HT transporter

Autor: M. Andreas B. Larsen, Jonas N. N. Eildal, Benny Bang-Andersen, Jacob Andersen, Claus J. Loland, Per Plenge, Anders S. Kristensen, Klaus Peter Bogeso, Kristian Strømgaard, Ulrik Gether

Publikováno v: British Journal of Pharmacology. 173:925-936

Background and purpose The 5-HT transporter (SERT) is a target for antidepressant drugs. SERT possesses two binding sites: the orthosteric (S1) binding site, which is the presumed target for current SERT inhibitors, and an allosteric (S2) site for wh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fa723ecac7b2c3f5c415d683e5ab6882
https://doi.org/10.1111/bph.13411

Allosteric Binding in the Serotonin Transporter – Pharmacology, Structure, Function and Potential Use as a Novel Drug Target

Autor: Klaus Peter Bogeso, Claus J. Loland, Per Plenge, Benny Bang-Andersen, Connie Sanchez

Publikováno v: Allosterism in Drug Discovery ISBN: 9781782624592

The serotonin transporter (SERT) is an important drug target and the majority of currently used antidepressants are potent inhibitors of SERT, binding primarily to the substrate binding site. However, even though the existence of an allosteric modula

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::199157ad1f66050b1ab33b2d71d496e7
https://doi.org/10.1039/9781782629276-00360

Povl Krogsgaard-Larsen: A Giant in Medicinal Chemistry Research

Autor: Klaus Peter Bogeso

Publikováno v: Neurochemical Research. 39:1847-1849

Povl Krogsgaard-Larsen is a true giant in medicinal chemistry and without doubt the person that has had the greatest impact on this discipline in Denmark. I got to know Povl in the spring of 1970. After I had finished my chemical engineer education,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::beb577049315065a24b294f52c3fdd8b
https://doi.org/10.1007/s11064-014-1437-5

Synthesis and Positron Emission Tomography Evaluation of Three Norepinephrine Transporter Radioligands: [C-11]Desipramine, [C-11]Talopram and [C-11]Talsupram

Autor: Balázs Gulyás, Magnus Schou, Christer Halldin, Judit Sovago, Klaus Peter Bogeso, Lars Farde, Victor W. Pike

Publikováno v: Molecular Imaging and Biology. 8:1-8

Desipramine (DMI), talopram and talsupram, three of the most potent norepinephrine transporter (NET) inhibitors reported to date, were radiolabeled in high yields and at high specific radioactivity (58-75 GBq/micromol) by the methylation of nor-precu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9be6fbfd0c8ed89b380a2dc51fc815ed
https://doi.org/10.1007/s11307-005-0027-y