List of works - Kristian Strømgaard

A Heteromeric Snake Toxin and the Molecular Details of Pain Perception ⬇️

scholarly article by Kristian Strømgaard & Anders S Kristensen published 15 March 2012 in Angewandte Chemie International Edition

A fluorescence polarization based screening assay for identification of small molecule inhibitors of the PICK1 PDZ domain.

scientific article published in August 2011

A high-affinity, dimeric inhibitor of PSD-95 bivalently interacts with PDZ1-2 and protects against ischemic brain damage

scientific article

A parallel semisynthetic approach for structure-activity relationship studies of peptide YY.

scientific article

A sequential binding mechanism in a PDZ domain.

scientific article

AMPA receptor ligands: synthetic and pharmacological studies of polyamines and polyamine toxins

scientific article published in September 2004

Analogues of neuroactive polyamine wasp toxins that lack inner basic sites exhibit enhanced antagonism toward a muscle-type mammalian nicotinic acetylcholine receptor.

scientific article

Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: discovery of nanomolar, nonselective, and use-dependent antagonists

scientific article published on October 2010

Binding of ArgTX-636 in the NMDA receptor ion channel

scientific article published on 24 May 2014

Binding of the multimodal antidepressant drug vortioxetine to the human serotonin transporter.

scientific article published on 21 September 2015

Binding site residues control inhibitor selectivity in the human norepinephrine transporter but not in the human dopamine transporter

scientific article

Biophysical characterization of the complex between human papillomavirus E6 protein and synapse-associated protein 97.

scientific article published on 27 November 2010

Cell-permeable and plasma-stable peptidomimetic inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction.

scientific article

Characterization of intracellular regions in the human serotonin transporter for phosphorylation sites.

scientific article

Chemistry meets Biology: Chemical Approaches to the Study of Biology

scientific article published on 01 November 2004

Contrasting actions of philanthotoxin-343 and philanthotoxin-(12) on human muscle nicotinic acetylcholine receptors

scientific article published on October 2003

Controlling Ca2+ Permeable α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Photochromic Ion Channel Blockers

scholarly article by Niels G. Nørager et al published 20 August 2018 in Journal of Medicinal Chemistry

Deciphering the kinetic binding mechanism of dimeric ligands using a potent plasma-stable dimeric inhibitor of postsynaptic density protein-95 as an example.

scientific article

Design and Synthesis of Peptide YY Analogues with C-terminal Backbone Amide-to-Ester Modifications

scientific article

Design and synthesis of high-affinity dimeric inhibitors targeting the interactions between gephyrin and inhibitory neurotransmitter receptors

scientific article

Design and synthesis of highly potent and plasma-stable dimeric inhibitors of the PSD-95-NMDA receptor interaction

scientific article published in January 2009

Design and synthesis of labeled analogs of PhTX-56, a potent and selective AMPA receptor antagonist.

scientific article published on September 2005

Design, synthesis, and characterization of fatty acid derivatives of a dimeric peptide-based postsynaptic density-95 (PSD-95) inhibitor

scientific article published on 30 January 2015

Design, synthesis, and pharmacological characterization of polyamine toxin derivatives: potent ligands for the pore-forming region of AMPA receptors

scientific article published in April 2006

Designing Poly-agonists for Treatment of Metabolic Diseases: Challenges and Opportunities

scientific article published on 01 July 2019

Detecting protein-protein interactions in living cells: development of a bioluminescence resonance energy transfer assay to evaluate the PSD-95/NMDA receptor interaction

scientific article published on 4 June 2009

Development of potent fluorescent polyamine toxins and application in labeling of ionotropic glutamate receptors in hippocampal neurons.

scientific article published on 24 July 2013

Effects of Dimeric PSD-95 Inhibition on Excitotoxic Cell Death and Outcome After Controlled Cortical Impact in Rats.

scientific article published on 21 August 2017

Effects of the dimeric PSD-95 inhibitor UCCB01-144 in mouse models of pain, cognition and motor function

scientific article published on 28 March 2016

Effects of the dimeric PSD-95 inhibitor UCCB01-144 on functional recovery after fimbria-fornix transection in rats

scientific article

Energetic pathway sampling in a protein interaction domain.

scientific article

Evaluation of PhTX-74 as subtype-selective inhibitor of GluA2-containing AMPA receptors.

scientific article

From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: synthesis and structure-activity relationship studies.

scientific article

General Synthesis of β-Alanine-Containing Spider Polyamine Toxins and Discovery of Nephila Polyamine Toxins 1 and 8 as Highly Potent Inhibitors of Ionotropic Glutamate Receptors

scientific article published on 06 November 2012

Genetically encoded photocrosslinkers locate the high-affinity binding site of antidepressant drugs in the human serotonin transporter

scientific article published on 19 April 2016

Gephyrin-binding peptides visualize postsynaptic sites and modulate neurotransmission.

scientific article published on 28 November 2016

Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation

scientific article published in August 2002

Ginkgolides and glycine receptors: a structure-activity relationship study

scientific article published in March 2004

Ginkgolides: selective acetylations, translactonization, and biological evaluation

scientific article

Heterotrimeric G Proteins as Therapeutic Targets in Drug Discovery

scientific article published on 26 December 2019

Identification and characterization of a small-molecule inhibitor of death-associated protein kinase 1.

scientific article published on 7 November 2014

Identification of a small-molecule inhibitor of the PICK1 PDZ domain that inhibits hippocampal LTP and LTD.

scientific article

Importance of a Conserved Lys/Arg Residue for Ligand/PDZ Domain Interactions as Examined by Protein Semisynthesis.

scientific article published on 29 July 2016

Importance of the Extracellular Loop 4 in the Human Serotonin Transporter for Inhibitor Binding and Substrate Translocation

scientific article published on 22 April 2015

In vitro and in vivo effects of a novel dimeric inhibitor of PSD-95 on excitotoxicity and functional recovery after experimental traumatic brain injury

scientific article published on 17 November 2016

Inhibition of AMPA receptors by polyamine toxins is regulated by agonist efficacy and stargazin

scientific article published on 22 February 2014

Interaction of antidepressants with the serotonin and norepinephrine transporters: mutational studies of the S1 substrate binding pocket

scientific article published on 19 October 2012

Interaction partners of PSD-93 studied by X-ray crystallography and fluorescence polarization spectroscopy

scientific article

Interrogating the Molecular Basis for Substrate Recognition in Serotonin and Dopamine Transporters with High-Affinity Substrate-Based Bivalent Ligands

scientific article published on 18 July 2016

Knockin mouse with mutant Gα11 mimics human inherited hypocalcemia and is rescued by pharmacologic inhibitors

scientific article published on 09 February 2017

Ligand binding by PDZ domains.

scientific article published on 07 June 2012

Ligand binding to the PDZ domains of postsynaptic density protein 95.

scientific article

Location of the antidepressant binding site in the serotonin transporter: importance of Ser-438 in recognition of citalopram and tricyclic antidepressants.

scientific article

Mapping the Binding Site for Escitalopram and Paroxetine in the Human Serotonin Transporter Using Genetically Encoded Photo-Cross-Linkers.

scientific article

Mechanism and site of action of big dynorphin on ASIC1a

scientific article published on 12 March 2020

Mechanistic insight into benzenethiol catalyzed amide bond formations from thioesters and primary amines.

scientific article published on 26 June 2014

Modified peptides as potent inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction

scientific article published on 24 September 2008

Molecular Details of a Coupled Binding and Folding Reaction between the Amyloid Precursor Protein and a Folded Domain

scientific article published on 23 June 2021

Molecular basis for selective serotonin reuptake inhibition by the antidepressant agent fluoxetine (Prozac).

scientific article

Molecular basis of the alternative recruitment of GABA(A) versus glycine receptors through gephyrin

scientific article

Multisite NHERF1 phosphorylation controls GRK6A regulation of hormone-sensitive phosphate transport

scientific article published on 01 January 2021

Mutational mapping and modeling of the binding site for (S)-citalopram in the human serotonin transporter.

scientific article

PDZ Domains as Drug Targets

scientific article published on 24 April 2019

PDZ domain-mediated interactions of G protein-coupled receptors with postsynaptic density protein 95: quantitative characterization of interactions

scientific article

PSD-95 uncoupling from NMDA receptors by Tat- N-dimer ameliorates neuronal depolarization in cortical spreading depression

scientific article published on 22 April 2016

Plant Polyphenols Inhibit Functional Amyloid and Biofilm Formation in Pseudomonas Strains by Directing Monomers to Off-Pathway Oligomers

scientific article published on 26 October 2019

Polyamine toxins: development of selective ligands for ionotropic receptors.

scientific article

Precise Somatotopic Thalamocortical Axon Guidance Depends on LPA-Mediated PRG-2/Radixin Signaling.

scientific article published on 13 September 2016

Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists

scientific article

Preparation of a tritiated ginkgolide

scientific article published in November 2004

Probing Backbone Hydrogen Bonds in Proteins by Amide-to-Ester Mutations

scientific article published on 01 October 2018

Probing backbone hydrogen bonding in PDZ/ligand interactions by protein amide-to-ester mutations.

scientific article

Probing the Mint2 protein-protein interaction network with relevance for the pathophysiology of Alzheimer's disease

scientific article published on 26 March 2018

Probing the role of backbone hydrogen bonds in protein-peptide interactions by amide-to-ester mutations

scientific article published on 7 June 2013

Protein Engineering Reveals Mechanisms of Functional Amyloid Formation in Pseudomonas aeruginosa Biofilms

scholarly article by Alissa Bleem published in October 2018

Protolytic properties of polyamine wasp toxin analogues studied by 13C NMR spectroscopy

scientific article published in November 2006

Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity

scientific article published on 11 February 2019

Rational design of alpha-conotoxin analogues targeting alpha7 nicotinic acetylcholine receptors: improved antagonistic activity by incorporation of proline derivatives

scientific article

Recent achievements in developing selective Gq inhibitors

Recent advances in the understanding of the interaction of antidepressant drugs with serotonin and norepinephrine transporters.

scientific article

Recombinant production of peptide C-terminal α-amides using an engineered intein

scientific article

Rigidified clicked dimeric ligands for studying the dynamics of the PDZ1-2 supramodule of PSD-95.

scientific article

Selectivity, efficacy and toxicity studies of UCCB01-144, a dimeric neuroprotective PSD-95 inhibitor

scientific article published on 02 March 2019

Side-chain interactions form late and cooperatively in the binding reaction between disordered peptides and PDZ domains.

scientific article

Site-Specific Phosphorylation of PSD-95 PDZ Domains Reveals Fine-Tuned Regulation of Protein-Protein Interactions

scientific article published on 10 July 2017

Site-specific phosphorylation of PSD-95 dynamically regulates the postsynaptic density as observed by phase separation

scientific article published on 14 October 2021

Small molecules from spiders used as chemical probes.

scientific article published on 27 October 2011

Solid phase synthesis and biological evaluation of enantiomerically pure wasp toxin analogues PhTX-343 and PhTX-12.

scientific article published in February 2000

Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata.

scientific article published on 28 December 2010

Solid-phase synthesis and pharmacological evaluation of analogues of PhTX-12-A potent and selective nicotinic acetylcholine receptor antagonist.

scientific article

Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors

scientific article published in December 2002

Structure-Activity Relationship Studies of the Cyclic Depsipeptide Natural Product YM-254890, Targeting the Gq Protein

scientific article published on 16 May 2017

Structure-Activity Relationship Studies of the Natural Product Gq/11 Protein Inhibitor YM-254890

scientific article published on 21 March 2019

Structure-activity relationship studies of N-methylated and N-hydroxylated spider polyamine toxins as inhibitors of ionotropic glutamate receptors

scientific article published on 29 May 2014

Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors

scientific article

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

scientific article published on 23 December 2015

Structure-activity relationship study of spider polyamine toxins as inhibitors of ionotropic glutamate receptors.

scientific article published on 29 September 2014

Structure-activity relationships of a small-molecule inhibitor of the PDZ domain of PICK1

scientific article

Structure–activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359

scientific article published on 12 July 2018

Synthesis and biological activity of argiotoxin 636 and analogues: selective antagonists for ionotropic glutamate receptors

scientific article published in January 2009

Synthesis and biological activity of novel alpha-conotoxin analogues incorporating substituted proline derivatives.

scientific article published in January 2009

Synthesis of peptides using tert-butyloxycarbonyl (Boc) as the α-amino protection group

scientific article published in January 2013

Synthetic and mechanistic insight into nosylation of glycine residues.

scientific article published in April 2013

Targeting protein-protein interactions with trimeric ligands: high affinity inhibitors of the MAGUK protein family

scientific article

Targeting receptor complexes: a new dimension in drug discovery

scientific article published on 11 November 2020

Targeting the APP-Mint2 Protein-Protein Interaction with a Peptide-Based Inhibitor Reduces Amyloid-β Formation

scientific article published on 05 January 2021

Targeting the γ-Aminobutyric Acid Type B (GABAB) Receptor Complex: Development of Inhibitors Targeting the K+ Channel Tetramerization Domain (KCTD) Containing Proteins/GABAB Receptor Protein-Protein Interaction

scientific article published on 25 September 2019

Terpene trilactones from Ginkgo biloba are antagonists of cortical glycine and GABA(A) receptors

scientific article published on 22 September 2003

The role of backbone hydrogen bonds in the transition state for protein folding of a PDZ domain.

scientific article

Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors

scientific article published on 25 July 2016

UCCB01-125, a dimeric inhibitor of PSD-95, reduces inflammatory pain without disrupting cognitive or motor performance: comparison with the NMDA receptor antagonist MK-801.

scientific article

Uncompetitive antagonism of AMPA receptors: Mechanistic insights from studies of polyamine toxin derivatives

scientific article published in September 2006

List of works by Kristian Strømgaard

A Heteromeric Snake Toxin and the Molecular Details of Pain Perception ⬇️

A fluorescence polarization based screening assay for identification of small molecule inhibitors of the PICK1 PDZ domain.

A high-affinity, dimeric inhibitor of PSD-95 bivalently interacts with PDZ1-2 and protects against ischemic brain damage

A parallel semisynthetic approach for structure-activity relationship studies of peptide YY.

A sequential binding mechanism in a PDZ domain.

AMPA receptor ligands: synthetic and pharmacological studies of polyamines and polyamine toxins

Analogues of neuroactive polyamine wasp toxins that lack inner basic sites exhibit enhanced antagonism toward a muscle-type mammalian nicotinic acetylcholine receptor.

Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: discovery of nanomolar, nonselective, and use-dependent antagonists

Binding of ArgTX-636 in the NMDA receptor ion channel

Binding of the multimodal antidepressant drug vortioxetine to the human serotonin transporter.

Binding site residues control inhibitor selectivity in the human norepinephrine transporter but not in the human dopamine transporter

Biophysical characterization of the complex between human papillomavirus E6 protein and synapse-associated protein 97.

Cell-permeable and plasma-stable peptidomimetic inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction.

Characterization of intracellular regions in the human serotonin transporter for phosphorylation sites.

Chemistry meets Biology: Chemical Approaches to the Study of Biology

Contrasting actions of philanthotoxin-343 and philanthotoxin-(12) on human muscle nicotinic acetylcholine receptors

Controlling Ca2+ Permeable α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Photochromic Ion Channel Blockers

Deciphering the kinetic binding mechanism of dimeric ligands using a potent plasma-stable dimeric inhibitor of postsynaptic density protein-95 as an example.

Design and Synthesis of Peptide YY Analogues with C-terminal Backbone Amide-to-Ester Modifications

Design and synthesis of high-affinity dimeric inhibitors targeting the interactions between gephyrin and inhibitory neurotransmitter receptors

Design and synthesis of highly potent and plasma-stable dimeric inhibitors of the PSD-95-NMDA receptor interaction

Design and synthesis of labeled analogs of PhTX-56, a potent and selective AMPA receptor antagonist.

Design, synthesis, and characterization of fatty acid derivatives of a dimeric peptide-based postsynaptic density-95 (PSD-95) inhibitor

Design, synthesis, and pharmacological characterization of polyamine toxin derivatives: potent ligands for the pore-forming region of AMPA receptors

Designing Poly-agonists for Treatment of Metabolic Diseases: Challenges and Opportunities

Detecting protein-protein interactions in living cells: development of a bioluminescence resonance energy transfer assay to evaluate the PSD-95/NMDA receptor interaction

Development of potent fluorescent polyamine toxins and application in labeling of ionotropic glutamate receptors in hippocampal neurons.

Effects of Dimeric PSD-95 Inhibition on Excitotoxic Cell Death and Outcome After Controlled Cortical Impact in Rats.

Effects of the dimeric PSD-95 inhibitor UCCB01-144 in mouse models of pain, cognition and motor function

Effects of the dimeric PSD-95 inhibitor UCCB01-144 on functional recovery after fimbria-fornix transection in rats

Energetic pathway sampling in a protein interaction domain.

Evaluation of PhTX-74 as subtype-selective inhibitor of GluA2-containing AMPA receptors.

From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: synthesis and structure-activity relationship studies.

General Synthesis of β-Alanine-Containing Spider Polyamine Toxins and Discovery of Nephila Polyamine Toxins 1 and 8 as Highly Potent Inhibitors of Ionotropic Glutamate Receptors

Genetically encoded photocrosslinkers locate the high-affinity binding site of antidepressant drugs in the human serotonin transporter

Gephyrin-binding peptides visualize postsynaptic sites and modulate neurotransmission.

Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation

Ginkgolides and glycine receptors: a structure-activity relationship study

Ginkgolides: selective acetylations, translactonization, and biological evaluation

Heterotrimeric G Proteins as Therapeutic Targets in Drug Discovery

Identification and characterization of a small-molecule inhibitor of death-associated protein kinase 1.

Identification of a small-molecule inhibitor of the PICK1 PDZ domain that inhibits hippocampal LTP and LTD.

Importance of a Conserved Lys/Arg Residue for Ligand/PDZ Domain Interactions as Examined by Protein Semisynthesis.

Importance of the Extracellular Loop 4 in the Human Serotonin Transporter for Inhibitor Binding and Substrate Translocation

In vitro and in vivo effects of a novel dimeric inhibitor of PSD-95 on excitotoxicity and functional recovery after experimental traumatic brain injury

Inhibition of AMPA receptors by polyamine toxins is regulated by agonist efficacy and stargazin

Interaction of antidepressants with the serotonin and norepinephrine transporters: mutational studies of the S1 substrate binding pocket

Interaction partners of PSD-93 studied by X-ray crystallography and fluorescence polarization spectroscopy

Interrogating the Molecular Basis for Substrate Recognition in Serotonin and Dopamine Transporters with High-Affinity Substrate-Based Bivalent Ligands

Knockin mouse with mutant Gα11 mimics human inherited hypocalcemia and is rescued by pharmacologic inhibitors

Ligand binding by PDZ domains.

Ligand binding to the PDZ domains of postsynaptic density protein 95.

Location of the antidepressant binding site in the serotonin transporter: importance of Ser-438 in recognition of citalopram and tricyclic antidepressants.

Mapping the Binding Site for Escitalopram and Paroxetine in the Human Serotonin Transporter Using Genetically Encoded Photo-Cross-Linkers.

Mechanism and site of action of big dynorphin on ASIC1a

Mechanistic insight into benzenethiol catalyzed amide bond formations from thioesters and primary amines.

Modified peptides as potent inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction

Molecular Details of a Coupled Binding and Folding Reaction between the Amyloid Precursor Protein and a Folded Domain

Molecular basis for selective serotonin reuptake inhibition by the antidepressant agent fluoxetine (Prozac).

Molecular basis of the alternative recruitment of GABA(A) versus glycine receptors through gephyrin

Multisite NHERF1 phosphorylation controls GRK6A regulation of hormone-sensitive phosphate transport

Mutational mapping and modeling of the binding site for (S)-citalopram in the human serotonin transporter.

PDZ Domains as Drug Targets

PDZ domain-mediated interactions of G protein-coupled receptors with postsynaptic density protein 95: quantitative characterization of interactions

PSD-95 uncoupling from NMDA receptors by Tat- N-dimer ameliorates neuronal depolarization in cortical spreading depression

Plant Polyphenols Inhibit Functional Amyloid and Biofilm Formation in Pseudomonas Strains by Directing Monomers to Off-Pathway Oligomers

Polyamine toxins: development of selective ligands for ionotropic receptors.

Precise Somatotopic Thalamocortical Axon Guidance Depends on LPA-Mediated PRG-2/Radixin Signaling.

Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists

Preparation of a tritiated ginkgolide

Probing Backbone Hydrogen Bonds in Proteins by Amide-to-Ester Mutations

Probing backbone hydrogen bonding in PDZ/ligand interactions by protein amide-to-ester mutations.

Probing the Mint2 protein-protein interaction network with relevance for the pathophysiology of Alzheimer's disease

Probing the role of backbone hydrogen bonds in protein-peptide interactions by amide-to-ester mutations

Protein Engineering Reveals Mechanisms of Functional Amyloid Formation in Pseudomonas aeruginosa Biofilms

Protolytic properties of polyamine wasp toxin analogues studied by 13C NMR spectroscopy

Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity

Rational design of alpha-conotoxin analogues targeting alpha7 nicotinic acetylcholine receptors: improved antagonistic activity by incorporation of proline derivatives

Recent achievements in developing selective Gq inhibitors