List of works - Matthias P Wymann

(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase

scientific article published on 20 June 2019

4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders

scientific article published on 09 November 2020

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.

scientific article published on 22 August 2017

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

scientific article published on 11 September 2019

A central role for DOCK2 during interstitial lymphocyte motility and sphingosine-1-phosphate-mediated egress

scientific article

A class of highly selective inhibitors bind to an active state of PI3Kγ

scientific article published on 04 February 2019

Ablation of phosphoinositide 3-kinase-gamma reduces the severity of acute pancreatitis

scientific article

Activation loop sequences confer substrate specificity to phosphoinositide 3-kinase alpha (PI3Kalpha ). Functions of lipid kinase-deficient PI3Kalpha in signaling.

scientific article published on 13 February 2001

Activation of PI3-kinase is required for AMPA receptor insertion during LTP of mEPSCs in cultured hippocampal neurons

scientific article (publication date: 22 May 2003)

Activation of the respiratory burst in eosinophil leucocytes--a transduction sequence decoupled from cytosolic Ca2+ rise

scientific article published on 01 January 1995

Airway inflammation: chemokine-induced neutrophilia and the class I phosphoinositide 3-kinases

scientific article published in April 2005

Bifurcation of lipid and protein kinase signals of PI3Kgamma to the protein kinases PKB and MAPK

scientific article published on 01 October 1998

Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.

scientific article published on 28 August 2005

Brain-penetrant PQR620 mTOR and PQR530 PI3K/mTOR inhibitor reduce huntingtin levels in cell models of HD

scientific article published on 14 October 2019

C-C motif chemokine CCL3 and canonical neutrophil attractants promote neutrophil extravasation through common and distinct mechanisms

scientific article published on 6 June 2012

Cell-permeant and photocleavable chemical inducer of dimerization

scientific article published on 26 March 2014

Central role for G protein-coupled phosphoinositide 3-kinase gamma in inflammation.

scientific article

Chemical development of intracellular protein heterodimerizers

scientific article

Chemiluminescence detection of H2O2 produced by human neutrophils during the respiratory burst

scientific article published on 01 September 1987

Class IB-phosphatidylinositol 3-kinase (PI3K) deficiency ameliorates IA-PI3K-induced systemic lupus but not T cell invasion

scientific article published in January 2006

Corresponding oscillations in neutrophil shape and filamentous actin content.

scientific article published on January 1990

Cutting edge: T cell development requires the combined activities of the p110gamma and p110delta catalytic isoforms of phosphatidylinositol 3-kinase.

scientific article published in September 2005

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

scientific article

Defective dendritic cell migration and activation of adaptive immunity in PI3Kgamma-deficient mice

scientific article

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

scientific article published on 14 November 2018

Elastin-derived peptides potentiate atherosclerosis through the immune Neu1-PI3Kγ pathway.

scientific article

Essential role of phosphoinositide 3-kinase gamma in eosinophil chemotaxis within acute pulmonary inflammation.

scientific article

Essential role of the p110beta subunit of phosphoinositide 3-OH kinase in male fertility.

scientific article

European workshop on the cell biology of phagocytes

scientific article published on 01 January 1997

Fluid-phase pinocytosis of native low density lipoprotein promotes murine M-CSF differentiated macrophage foam cell formation

scientific article

GABAA receptor-associated phosphoinositide 3-kinase is required for insulin-induced recruitment of postsynaptic GABAA receptors

scientific journal article

GTPgammaS-induced actin polymerisation in vitro: ATP- and phosphoinositide-independent signalling via Rho-family proteins and a plasma membrane-associated guanine nucleotide exchange factor

scientific article published on 01 June 1998

Genetic ablation of PI3Kγ results in defective IL-17RA signalling in T lymphocytes and increased IL-17 levels

scientific article published in October 2012

Genetic and pharmacological targeting of phosphoinositide 3-kinase-gamma reduces atherosclerosis and favors plaque stability by modulating inflammatory processes

scientific article published on 11 February 2008

Human PI3Kγ deficiency and its microbiota-dependent mouse model reveal immunodeficiency and tissue immunopathology

scientific article published on 25 September 2019

Human neutrophil migration into skin chambers is associated with production of NAP-1/IL8 and C5a

scientific article published on 01 July 1991

Inactivation of PI3Kgamma and PI3Kdelta distorts T-cell development and causes multiple organ inflammation.

scientific article published on 12 July 2007

Inhibition of phosphoinositide 3-kinase γ attenuates inflammation, obesity, and cardiovascular risk factors.

scientific article published in March 2013

Integrating cardiac PIP3 and cAMP signaling through a PKA anchoring function of p110γ.

scientific article published on April 2011

Lack of phosphoinositide 3-kinase-gamma attenuates ventilator-induced lung injury

scientific article

Leukocyte transmigration is modulated by chemokine-mediated PI3Kgamma-dependent phosphorylation of vimentin

scientific article published in April 2009

Lipid kinase and protein kinase activities of G-protein-coupled phosphoinositide 3-kinase gamma: structure-activity analysis and interactions with wortmannin.

scientific article published on June 1997

Lipid signalling in disease.

scientific article published on February 2008

Lipids on the move: phosphoinositide 3-kinases in leukocyte function

scientific article

Living with lethal PIP3 levels: viability of flies lacking PTEN restored by a PH domain mutation in Akt/PKB.

scientific article published on 28 February 2002

Loss of phosphatase activity in myotubularin-related protein 2 is associated with Charcot-Marie-Tooth disease type 4B1.

scientific article

Luminal decoration of blood vessels by activated perivasal mast cells in allergic rhinitis

scientific article

Mal connects TLR2 to PI3Kinase activation and phagocyte polarization

scientific article

Membrane dynamics in physiology and disease

scientific article published on 3 June 2013

Membrane transport in Caenorhabditis elegans: an essential role for VPS34 at the nuclear membrane

scientific article

Microquantification of cellular and in vitro F-actin by rhodamine phalloidin fluorescence enhancement.

scientific article published in November 1998

Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL.

scientific article published on 4 November 2011

Negative feedback regulation of Rac in leukocytes from mice expressing a constitutively active phosphatidylinositol 3-kinase gamma

scholarly article

Neutral not a loss: phosphoinositides beyond the head group

scientific article published on 01 March 2011

New molecular and therapeutic insights into canine diffuse large B-cell lymphoma elucidates the role of the dog as a model for human disease

scientific article published on 13 December 2018

PI(3)Kγ has an important context-dependent role in neutrophil chemokinesis

article

PI3K p110γ deletion attenuates murine atherosclerosis by reducing macrophage proliferation but not polarization or apoptosis in lesions.

scientific article

PI3Kgamma adaptor subunits define coupling to degranulation and cell motility by distinct PtdIns(3,4,5)P3 pools in mast cells.

scientific article

PI3Ks-drug targets in inflammation and cancer.

scientific article published on January 2012

PI3Kγ Modulates the Cardiac Response to Chronic Pressure Overload by Distinct Kinase-Dependent and -Independent Effects

article

PI3Kγ activity in leukocytes promotes adipose tissue inflammation and early-onset insulin resistance during obesity

scientific article published on 18 July 2017

PI3Kγ within a nonhematopoietic cell type negatively regulates diet-induced thermogenesis and promotes obesity and insulin resistance

scientific article

PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control

scientific article (publication date: 2013)

PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy.

scientific article

Phosphatidylinositol 3-kinase regulates the CD4/CD8 T cell differentiation ratio

scientific journal article

Phosphoinositide 3-kinase gamma controls autonomic regulation of the mouse heart through Gi-independent downregulation of cAMP level.

scientific article published in January 2005

Phosphoinositide 3-kinase gamma is an essential amplifier of mast cell function

scientific article published in March 2002

Phosphoinositide 3-kinase gamma mediates Jun kinase activation via its lipid-kinase activity

scientific article published on 01 January 2004

Phosphoinositide 3-kinase gamma participates in T cell receptor-induced T cell activation.

scientific article

Phosphoinositide 3-kinase gamma-deficient hearts are protected from the PAF-dependent depression of cardiac contractility

scientific article published in November 2003

Phosphoinositide 3-kinase gamma: a key modulator in inflammation and allergy

scientific article

Phosphoinositide 3-kinase signalling--which way to target?

scientific article

Phosphoinositide 3-kinase signalling: no lipids.

scientific article

Phosphoinositide 3-kinase γ mediates microglial phagocytosis via lipid kinase-independent control of cAMP.

scientific article published on 29 December 2012

Plasmin inhibitors prevent leukocyte accumulation and remodeling events in the postischemic microvasculature.

scientific article

Properties and activation mechanism of neutrophilic leukocytes

scientific article published in January 1989

Ras is an indispensable coregulator of the class IB phosphoinositide 3-kinase p87/p110gamma

scientific journal article

Regulation of myocardial contractility and cell size by distinct PI3K-PTEN signaling pathways

scientific article

Requirement for PI 3-kinase gamma in macrophage migration to MCP-1 and CSF-1.

scientific article published in October 2003

Resistance to thromboembolism in PI3Kgamma-deficient mice.

scientific article published on 9 July 2001

Respiratory burst oscillations in human neutrophils and their correlation with fluctuations in apparent cell shape

scientific article published on 01 September 1989

Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils

scientific article

Shape changes, exocytosis, and cytosolic free calcium changes in stimulated human eosinophils

scientific article

Staurosporine inhibits the respiratory burst and induces exocytosis in human neutrophils.

scientific article published on December 1989

Structural Determinants of Phosphoinositide 3-Kinase Inhibition by Wortmannin, LY294002, Quercetin, Myricetin, and Staurosporine

scientific article

Structure and function of phosphoinositide 3-kinases.

scientific article published in December 1998

Susi, a negative regulator of Drosophila PI3-kinase

scientific article published in June 2005

Targeting PI3K in neuroblastoma.

scientific article published on 12 March 2010

Targeting PI3Kγ activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response.

scientific article

Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors.

scientific article published in April 2009

Targeting phosphoinositide 3-kinase: moving towards therapy

scientific article

The Drosophila insulin/IGF receptor controls growth and size by modulating PtdInsP(3) levels

scientific article published in September 2002

The Novel TORC1/2 Kinase Inhibitor PQR620 Has Anti-Tumor Activity in Lymphomas as a Single Agent and in Combination with Venetoclax

scientific article published on 04 June 2019

The Ras/Rac1/Cdc42/SEK/JNK/c-Jun cascade is a key pathway by which agonists stimulate DNA synthesis in primary cultures of rat hepatocytes

scientific journal article

The direct effect of leptin on skeletal muscle thermogenesis is mediated by substrate cycling between de novo lipogenesis and lipid oxidation.

scientific article published in November 2004

The forkhead transcription factor FOXO3a increases phosphoinositide-3 kinase/Akt activity in drug-resistant leukemic cells through induction of PIK3CA expression

scientific article published on 21 July 2008

The mitogen-activated protein (MAP) kinase cascade can either stimulate or inhibit DNA synthesis in primary cultures of rat hepatocytes depending upon whether its activation is acute/phasic or chronic.

scientific article published on March 1998

The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy

scientific article published on 03 August 2018

The onset of the respiratory burst in human neutrophils. Real-time studies of H2O2 formation reveal a rapid agonist-induced transduction process.

scientific article published in September 1987

Transient targeting of phosphoinositide 3-kinase acts as a roadblock in mast cells' route to allergy

scientific article

Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction

scientific article

Wortmannin is a potent phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses.

scientific article published on December 1993

List of works by Matthias P Wymann

(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase

4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

A central role for DOCK2 during interstitial lymphocyte motility and sphingosine-1-phosphate-mediated egress

A class of highly selective inhibitors bind to an active state of PI3Kγ

Ablation of phosphoinositide 3-kinase-gamma reduces the severity of acute pancreatitis

Activation loop sequences confer substrate specificity to phosphoinositide 3-kinase alpha (PI3Kalpha ). Functions of lipid kinase-deficient PI3Kalpha in signaling.

Activation of PI3-kinase is required for AMPA receptor insertion during LTP of mEPSCs in cultured hippocampal neurons

Activation of the respiratory burst in eosinophil leucocytes--a transduction sequence decoupled from cytosolic Ca2+ rise

Airway inflammation: chemokine-induced neutrophilia and the class I phosphoinositide 3-kinases

Bifurcation of lipid and protein kinase signals of PI3Kgamma to the protein kinases PKB and MAPK

Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.

Brain-penetrant PQR620 mTOR and PQR530 PI3K/mTOR inhibitor reduce huntingtin levels in cell models of HD

C-C motif chemokine CCL3 and canonical neutrophil attractants promote neutrophil extravasation through common and distinct mechanisms

Cell-permeant and photocleavable chemical inducer of dimerization

Central role for G protein-coupled phosphoinositide 3-kinase gamma in inflammation.

Chemical development of intracellular protein heterodimerizers

Chemiluminescence detection of H2O2 produced by human neutrophils during the respiratory burst

Class IB-phosphatidylinositol 3-kinase (PI3K) deficiency ameliorates IA-PI3K-induced systemic lupus but not T cell invasion

Corresponding oscillations in neutrophil shape and filamentous actin content.

Cutting edge: T cell development requires the combined activities of the p110gamma and p110delta catalytic isoforms of phosphatidylinositol 3-kinase.

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

Defective dendritic cell migration and activation of adaptive immunity in PI3Kgamma-deficient mice

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

Elastin-derived peptides potentiate atherosclerosis through the immune Neu1-PI3Kγ pathway.

Essential role of phosphoinositide 3-kinase gamma in eosinophil chemotaxis within acute pulmonary inflammation.

Essential role of the p110beta subunit of phosphoinositide 3-OH kinase in male fertility.

European workshop on the cell biology of phagocytes

Fluid-phase pinocytosis of native low density lipoprotein promotes murine M-CSF differentiated macrophage foam cell formation

GABAA receptor-associated phosphoinositide 3-kinase is required for insulin-induced recruitment of postsynaptic GABAA receptors

GTPgammaS-induced actin polymerisation in vitro: ATP- and phosphoinositide-independent signalling via Rho-family proteins and a plasma membrane-associated guanine nucleotide exchange factor

Genetic ablation of PI3Kγ results in defective IL-17RA signalling in T lymphocytes and increased IL-17 levels

Genetic and pharmacological targeting of phosphoinositide 3-kinase-gamma reduces atherosclerosis and favors plaque stability by modulating inflammatory processes

Human PI3Kγ deficiency and its microbiota-dependent mouse model reveal immunodeficiency and tissue immunopathology

Human neutrophil migration into skin chambers is associated with production of NAP-1/IL8 and C5a

Inactivation of PI3Kgamma and PI3Kdelta distorts T-cell development and causes multiple organ inflammation.

Inhibition of phosphoinositide 3-kinase γ attenuates inflammation, obesity, and cardiovascular risk factors.

Integrating cardiac PIP3 and cAMP signaling through a PKA anchoring function of p110γ.

Lack of phosphoinositide 3-kinase-gamma attenuates ventilator-induced lung injury

Leukocyte transmigration is modulated by chemokine-mediated PI3Kgamma-dependent phosphorylation of vimentin

Lipid kinase and protein kinase activities of G-protein-coupled phosphoinositide 3-kinase gamma: structure-activity analysis and interactions with wortmannin.

Lipid signalling in disease.

Lipids on the move: phosphoinositide 3-kinases in leukocyte function

Living with lethal PIP3 levels: viability of flies lacking PTEN restored by a PH domain mutation in Akt/PKB.

Loss of phosphatase activity in myotubularin-related protein 2 is associated with Charcot-Marie-Tooth disease type 4B1.

Luminal decoration of blood vessels by activated perivasal mast cells in allergic rhinitis

Mal connects TLR2 to PI3Kinase activation and phagocyte polarization

Membrane dynamics in physiology and disease

Membrane transport in Caenorhabditis elegans: an essential role for VPS34 at the nuclear membrane

Microquantification of cellular and in vitro F-actin by rhodamine phalloidin fluorescence enhancement.

Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL.

Negative feedback regulation of Rac in leukocytes from mice expressing a constitutively active phosphatidylinositol 3-kinase gamma

Neutral not a loss: phosphoinositides beyond the head group

New molecular and therapeutic insights into canine diffuse large B-cell lymphoma elucidates the role of the dog as a model for human disease

PI(3)Kγ has an important context-dependent role in neutrophil chemokinesis

PI3K p110γ deletion attenuates murine atherosclerosis by reducing macrophage proliferation but not polarization or apoptosis in lesions.

PI3Kgamma adaptor subunits define coupling to degranulation and cell motility by distinct PtdIns(3,4,5)P3 pools in mast cells.

PI3Ks-drug targets in inflammation and cancer.

PI3Kγ Modulates the Cardiac Response to Chronic Pressure Overload by Distinct Kinase-Dependent and -Independent Effects

PI3Kγ activity in leukocytes promotes adipose tissue inflammation and early-onset insulin resistance during obesity

PI3Kγ within a nonhematopoietic cell type negatively regulates diet-induced thermogenesis and promotes obesity and insulin resistance

PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control

PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy.

Phosphatidylinositol 3-kinase regulates the CD4/CD8 T cell differentiation ratio

Phosphoinositide 3-kinase gamma controls autonomic regulation of the mouse heart through Gi-independent downregulation of cAMP level.

Phosphoinositide 3-kinase gamma is an essential amplifier of mast cell function

Phosphoinositide 3-kinase gamma mediates Jun kinase activation via its lipid-kinase activity

Phosphoinositide 3-kinase gamma participates in T cell receptor-induced T cell activation.

Phosphoinositide 3-kinase gamma-deficient hearts are protected from the PAF-dependent depression of cardiac contractility

Phosphoinositide 3-kinase gamma: a key modulator in inflammation and allergy

Phosphoinositide 3-kinase signalling--which way to target?

Phosphoinositide 3-kinase signalling: no lipids.

Phosphoinositide 3-kinase γ mediates microglial phagocytosis via lipid kinase-independent control of cAMP.

Plasmin inhibitors prevent leukocyte accumulation and remodeling events in the postischemic microvasculature.

Properties and activation mechanism of neutrophilic leukocytes

Ras is an indispensable coregulator of the class IB phosphoinositide 3-kinase p87/p110gamma

Regulation of myocardial contractility and cell size by distinct PI3K-PTEN signaling pathways

Requirement for PI 3-kinase gamma in macrophage migration to MCP-1 and CSF-1.