List of works - Jayvardhan Pandit

3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site

scientific article (publication date: 16 June 2003)

6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors

scientific article

A Novel Binding Mode Reveals Two Distinct Classes of NMDA Receptor GluN2B-selective Antagonists

scientific article published on 24 February 2016

A proposal for a specific double-helical structure in which the polynucleotide strands intercalate instead of forming base-pairs

scientific article published on 01 December 1983

Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks

scientific article published on January 2013

Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography

scientific article

Crystal structure of human squalene synthase. A key enzyme in cholesterol biosynthesis

scientific article published in September 2000

Cyclic nucleotide binding GAF domains from phosphodiesterases: structural and mechanistic insights

scientific article

Design of selective, ATP-competitive inhibitors of Akt

scientific article

Discovery and characterization of a novel dihydroisoxazole class of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiators

scientific article

Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design

scientific article

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.

scientific article

Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia

scientific article

Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics

scientific article (publication date: 10 February 2003)

Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors

scientific article

Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications

scientific article

Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: optimization studies and demonstration of in vivo efficacy

scientific article published on 29 March 2013

Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors

scientific article

Engineered stabilization and structural analysis of the autoinhibited conformation of PDE4

scientific article

High-resolution crystals and preliminary X-ray diffraction studies of a catalytic RNA

scientific article published on 01 May 1994

High-resolution structures of the ligand binding domain of the wild-type bacterial aspartate receptor

scientific article

Identification, characterization, and crystal structure of the Omega class glutathione transferases

scientific article

Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket

scientific article published on 01 January 1999

Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct

scientific article

PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency

scientific article

Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease

scientific article

Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.

scientific article

Potent, selective pyrimidinetrione-based inhibitors of MMP-13

scientific article published on 30 August 2006

Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13.

scientific article published on 29 September 2007

Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions

scientific article

Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors

scientific article published on May 2002

Synthesis and structure based optimization of novel Akt inhibitors

scientific article

The 2.0 Å crystal structure of the ERα ligand-binding domain complexed with lasofoxifene

scientific article

The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242)

scientific article

The three-dimensional structure of the ligand-binding domain of a wild-type bacterial chemotaxis receptor. Structural comparison to the cross-linked mutant forms and conformational changes upon ligand binding

scientific article

Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase

scientific article published in September 2005

Three-dimensional structure of dimeric human recombinant macrophage colony-stimulating factor

scientific article

Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia

scientific article

Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors

scientific article published on April 2015

List of works by Jayvardhan Pandit

3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site

6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors

A Novel Binding Mode Reveals Two Distinct Classes of NMDA Receptor GluN2B-selective Antagonists

A proposal for a specific double-helical structure in which the polynucleotide strands intercalate instead of forming base-pairs

Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks

Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography

Crystal structure of human squalene synthase. A key enzyme in cholesterol biosynthesis

Cyclic nucleotide binding GAF domains from phosphodiesterases: structural and mechanistic insights

Design of selective, ATP-competitive inhibitors of Akt

Discovery and characterization of a novel dihydroisoxazole class of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiators

Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.

Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia

Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics

Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors

Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications

Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: optimization studies and demonstration of in vivo efficacy

Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors

Engineered stabilization and structural analysis of the autoinhibited conformation of PDE4

High-resolution crystals and preliminary X-ray diffraction studies of a catalytic RNA

High-resolution structures of the ligand binding domain of the wild-type bacterial aspartate receptor

Identification, characterization, and crystal structure of the Omega class glutathione transferases

Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket

Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct

PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency

Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease

Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.

Potent, selective pyrimidinetrione-based inhibitors of MMP-13

Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13.

Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions

Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors

Synthesis and structure based optimization of novel Akt inhibitors

The 2.0 Å crystal structure of the ERα ligand-binding domain complexed with lasofoxifene

The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242)

The three-dimensional structure of the ligand-binding domain of a wild-type bacterial chemotaxis receptor. Structural comparison to the cross-linked mutant forms and conformational changes upon ligand binding

Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase

Three-dimensional structure of dimeric human recombinant macrophage colony-stimulating factor

Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia

Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors