List of works - Umesh R Desai

1,2-dithiole-3-ones as potent inhibitors of the bacterial 3-ketoacyl acyl carrier protein synthase III (FabH)

scientific article

6-Hydroxyflavone and derivatives exhibit potent anti-inflammatory activity among mono-, di- and polyhydroxylated flavones in kidney mesangial cells

scientific article published on 19 March 2015

A Hexasaccharide Containing Rare 2-O-Sulfate-Glucuronic Acid Residues Selectively Activates Heparin Cofactor II.

scientific article

A Simple Method for Discovering Druggable, Specific Glycosaminoglycan-Protein Systems. Elucidation of Key Principles from Heparin/Heparan Sulfate-Binding Proteins

scientific article

A capillary electrophoretic method for fingerprinting low molecular weight heparins.

scientific article

A molecular dynamics-based algorithm for evaluating the glycosaminoglycan mimicking potential of synthetic, homogenous, sulfated small molecules

scientific article

A nanosensor for ultrasensitive detection of oversulfated chondroitin sulfate contaminant in heparin

scientific article published on 06 January 2014

A novel allosteric pathway of thrombin inhibition: Exosite II mediated potent inhibition of thrombin by chemo-enzymatic, sulfated dehydropolymers of 4-hydroxycinnamic acids

scientific article

A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.

scientific article

A synthetic glycosaminoglycan mimetic blocks HSV-1 infection in human iris stromal cells

scientific article published on 24 November 2018

A synthetic heparin mimetic that allosterically inhibits factor XIa and reduces thrombosis in vivo without enhanced risk of bleeding

scientific article published on 10 September 2019

Allosteric Inhibition of Factor XIIIa. Non-Saccharide Glycosaminoglycan Mimetics, but Not Glycosaminoglycans, Exhibit Promising Inhibition Profile.

scientific article

Allosteric inhibition of factor XIa. Sulfated non-saccharide glycosaminoglycan mimetics as promising anticoagulants

scientific article published on 22 April 2015

Allosteric inhibition of human factor XIa: discovery of monosulfated benzofurans as a class of promising inhibitors

scientific article

Allosterism-based simultaneous, dual anticoagulant and antiplatelet action: allosteric inhibitor targeting the glycoprotein Ibα-binding and heparin-binding site of thrombin.

scientific article published on 9 January 2016

An electrophoresis-based assay for glycosyltransferase activity

scientific article published on 01 August 1992

An update on recent patents on thrombin inhibitors (2010 - 2013)

scientific article

Application of molecular connectivity and electro-topological indices in quantitative structure-activity analysis of pyrazole derivatives as inhibitors of factor Xa and thrombin.

scientific article

Capillary electrophoretic study of small, highly sulfated, non-sugar molecules interacting with antithrombin.

scientific article published on May 2009

Characterization of the plasma and blood anticoagulant potential of structurally and mechanistically novel oligomers of 4-hydroxycinnamic acids

scientific article

Chemical sulfation of small molecules—advances and challenges ⬇️

scientific article published on April 17, 2010

Chemoenzymatically prepared heparan sulfate containing rare 2-O-sulfonated glucuronic acid residues.

scientific article published on 17 March 2015

Conformational analysis of sucrose octasulfate by high resolution nuclear magnetic resonance spectroscopy

scientific article published on 01 October 1995

Crystal structures of influenza A virus matrix protein M1: variations on a theme

scientific article

Designing "high-affinity, high-specificity" glycosaminoglycan sequences through computerized modeling

scientific article

Designing allosteric inhibitors of factor XIa. Lessons from the interactions of sulfated pentagalloylglucopyranosides

scientific article

Designing nonsaccharide, allosteric activators of antithrombin for accelerated inhibition of factor Xa.

scientific article

Designing small, nonsugar activators of antithrombin using hydropathic interaction analyses.

scientific article

Discovery methodology for the development of direct factor VIIa inhibitors.

scientific article

Discovery of Allosteric Modulators of Factor XIa by Targeting Hydrophobic Domains Adjacent to Its Heparin-Binding Site ⬇️

scientific article published on March 18, 2013

Discovery of Sulfated Small Molecule Inhibitors of Matrix Metalloproteinase-8

scientific article published on 09 August 2020

Discovery of novel sulfonated small molecules that inhibit vascular tube formation ⬇️

scientific article published on April 16, 2012

Dynamic affinity chromatography in the separation of sulfated lignins binding to thrombin.

scientific article

Electronically Rich N-Substituted Tetrahydroisoquinoline 3-Carboxylic Acid Esters: Concise Synthesis and Conformational Studies

scientific article

Enzyme immobilization offers a robust tool to scale up the production of longer, diverse, natural glycosaminoglycan oligosaccharides

scientific article published on 20 March 2020

Exploring new non-sugar sulfated molecules as activators of antithrombin.

scientific article published in February 2003

First steps in the direction of synthetic, allosteric, direct inhibitors of thrombin and factor Xa

scientific article published on 6 June 2009

Glycosaminoglycan-protein interaction studies using fluorescence spectroscopy.

scientific article

Heparin interaction with a receptor on hyperglycemic dividing cells prevents intracellular hyaluronan synthesis and autophagy responses in models of type 1 diabetes.

scientific article published on 16 April 2015

High dose acetaminophen inhibits STAT3 and has free radical independent anti-cancer stem cell activity

scientific article published on 26 February 2021

Identification of a new functional domain in angiopoietin-like 3 (ANGPTL3) and angiopoietin-like 4 (ANGPTL4) involved in binding and inhibition of lipoprotein lipase (LPL).

scientific article published on 23 March 2009

Identification of the site of binding of sulfated, low molecular weight lignins on thrombin

scientific article

Immobilization alters heparin cleaving properties of heparinase I.

scientific article published on 22 August 2017

Importance of lysine 125 for heparin binding and activation of antithrombin.

scientific article

Importance of tryptophan 49 of antithrombin in heparin binding and conformational activation.

scientific article

Inhibition of Herpes Simplex Virus-1 Entry into Human Cells by Nonsaccharide Glycosaminoglycan Mimetics

scientific article published on 16 July 2018

Inhibition of Human Cytomegalovirus Entry into Host Cells Through a Pleiotropic Small Molecule

scientific article published on 29 February 2020

Interaction of antithrombin with sulfated, low molecular weight lignins: opportunities for potent, selective modulation of antithrombin function.

scientific article

Interaction of designed sulfated flavanoids with antithrombin: lessons on the design of organic activators.

scientific article

Investigation of the heparin-thrombin interaction by dynamic force spectroscopy

scientific article

Linear polyalkylamines as fingerprinting agents in capillary electrophoresis of low-molecular-weight heparins and glycosaminoglycans.

scientific article

Lysines and Arginines play non-redundant roles in mediating chemokine-glycosaminoglycan interactions

scientific article published in Scientific Reports

Mechanism of Heparin Activation of Antithrombin: Evidence for an Induced-Fit Model of Allosteric Activation Involving Two Interaction Subsites ⬇️

scientific article published on September 15, 1998

Mechanism of heparin activation of antithrombin. Role of individual residues of the pentasaccharide activating sequence in the recognition of native and activated states of antithrombin.

scientific article

Mechanism of poly(acrylic acid) acceleration of antithrombin inhibition of thrombin: implications for the design of novel heparin mimics.

scientific article

Molecular Basis of Chemokine CXCL5-Glycosaminoglycan Interactions

scientific article

New approaches for the preparation of hydrophobic heparin derivatives

scientific article published on 01 July 1994

New steroid haptens for radioimmunoassay: synthesis of steroids substituted with thioether or ester linkages at the 2 alpha-position

scientific article published on 01 April 1991

Novel heparin mimetics reveal cooperativity between exosite 2 and sodium-binding site of thrombin

scientific article published on 17 March 2018

Novel low molecular weight lignins as potential anti-emphysema agents: In vitro triple inhibitory activity against elastase, oxidation and inflammation.

scientific article published on 29 December 2012

On designing non-saccharide, allosteric activators of antithrombin.

scientific article published on 09 October 2008

On scaffold hopping: Challenges in the discovery of sulfated small molecules as mimetics of glycosaminoglycans ⬇️

scientific article published on October 24, 2012

On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients

scientific article published on 28 May 2019

Perspective on computational simulations of glycosaminoglycans

scientific article published on 10 September 2018

Plasmin regulation through allosteric, sulfated, small molecules.

scientific article published on 5 January 2015

Polymeric fluorescent heparin as one-step FRET substrate of human heparanase

scientific article published on 28 October 2018

Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.

scientific article

Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.

scientific article published on 15 December 2016

Preface. Glycosaminoglycans

scientific article published on 01 January 2015

Preferential recognition and antagonism of SARS-CoV-2 spike glycoprotein binding to 3- O -sulfated heparan sulfate

scientific article published on 08 October 2020

Rapid and efficient microwave-assisted synthesis of highly sulfated organic scaffolds.

scientific article

Rational design of potent, small, synthetic allosteric inhibitors of thrombin

scientific article

Recent advances on plasmin inhibitors for the treatment of fibrinolysis-related disorders

scientific article published on 21 March 2014

Rigorous Analysis of Free Solution Glycosaminoglycan Dynamics Using Simple, New Tools

scientific article published on 20 February 2020

Role of arginine 129 in heparin binding and activation of antithrombin

scientific article published on 01 June 2000

Roles of N-terminal region residues Lys11, Arg13, and Arg24 of antithrombin in heparin recognition and in promotion and stabilization of the heparin-induced conformational change.

scientific article published on January 2004

Serpin-glycosaminoglycan interactions.

scientific article published on January 2011

Solution NMR characterization of chemokine CXCL8/IL-8 monomer and dimer binding to glycosaminoglycans: structural plasticity mediates differential binding interactions

scientific article

Strategy for the sequence analysis of heparin

scientific article published on 01 December 1995

Structural characterization of a serendipitously discovered bioactive macromolecule, lignin sulfate.

scientific article published in September 2005

Structure elucidation of a novel acidic tetrasaccharide and hexasaccharide derived from a chemically modified heparin

scientific article published on 01 March 1993

Studying glycosaminoglycan-protein interactions using capillary electrophoresis

scientific article published on 01 January 2015

Substantial non-electrostatic forces are needed to induce allosteric disruption of thrombin's active site through exosite 2.

scientific article

Substrate specificity of the heparin lyases from Flavobacterium heparinum

scientific article published on 01 November 1993

Sulfated caffeic acid dehydropolymer attenuates elastase and cigarette smoke extract-induced emphysema in rats: sustained activity and a need of pulmonary delivery.

scientific article

Sulfated low molecular weight lignins, allosteric inhibitors of coagulation proteinases via the heparin binding site, significantly alter the active site of thrombin and factor xa compared to heparin.

scientific article

Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa

scientific article

Sulfated, low molecular weight lignins inhibit a select group of heparin-binding serine proteases.

scientific article published on December 2011

Sulfation Patterns Determine Cellular Internalization of Heparin-Like Polysaccharides ⬇️

scientific article published on February 27, 2013

Synthesis of glycosaminoglycan mimetics through sulfation of polyphenols

scientific article

Synthesis of per-sulfated flavonoids using 2,2,2-trichloro ethyl protecting group and their factor Xa inhibition potential.

scientific article

Synthetic, non-saccharide, glycosaminoglycan mimetics selectively target colon cancer stem cells.

scientific article

Targeting the GPIbα binding site of thrombin to simultaneously induce dual anticoagulant and antiplatelet effects

scientific article (publication date: 10 April 2014)

The Compensatory G88R Change Is Essential in Restoring the Normal Functions of Influenza A/WSN/33 Virus Matrix Protein 1 with a Disrupted Nuclear Localization Signal ⬇️

scientific article published on October 17, 2012

The Promise of Sulfated Synthetic Small Molecules as Modulators of Glycosaminoglycan Function ⬇️

scientific article published on August 1, 2013

Toward a robust computational screening strategy for identifying glycosaminoglycan sequences that display high specificity for target proteins

scientific article

Training the next generation of biomedical investigators in glycosciences

scientific article published on February 2016

Transforming growth factor-β2 is sequestered in preterm human milk by chondroitin sulfate proteoglycans

scientific article

Understanding Dermatan Sulfate-Heparin Cofactor II Interaction through Virtual Library Screening

scientific article

Viral inhibition studies on sulfated lignin, a chemically modified biopolymer and a potential mimic of heparan sulfate.

scientific article published on 17 April 2007

Visualizing antithrombin-binding 3-O-sulfated heparan sulfate motifs on cell surfaces

scientific article published on 04 November 2020

List of works by Umesh R Desai

1,2-dithiole-3-ones as potent inhibitors of the bacterial 3-ketoacyl acyl carrier protein synthase III (FabH)

6-Hydroxyflavone and derivatives exhibit potent anti-inflammatory activity among mono-, di- and polyhydroxylated flavones in kidney mesangial cells

A Hexasaccharide Containing Rare 2-O-Sulfate-Glucuronic Acid Residues Selectively Activates Heparin Cofactor II.

A Simple Method for Discovering Druggable, Specific Glycosaminoglycan-Protein Systems. Elucidation of Key Principles from Heparin/Heparan Sulfate-Binding Proteins

A capillary electrophoretic method for fingerprinting low molecular weight heparins.

A molecular dynamics-based algorithm for evaluating the glycosaminoglycan mimicking potential of synthetic, homogenous, sulfated small molecules

A nanosensor for ultrasensitive detection of oversulfated chondroitin sulfate contaminant in heparin

A novel allosteric pathway of thrombin inhibition: Exosite II mediated potent inhibition of thrombin by chemo-enzymatic, sulfated dehydropolymers of 4-hydroxycinnamic acids

A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.

A synthetic glycosaminoglycan mimetic blocks HSV-1 infection in human iris stromal cells

A synthetic heparin mimetic that allosterically inhibits factor XIa and reduces thrombosis in vivo without enhanced risk of bleeding

Allosteric Inhibition of Factor XIIIa. Non-Saccharide Glycosaminoglycan Mimetics, but Not Glycosaminoglycans, Exhibit Promising Inhibition Profile.

Allosteric inhibition of factor XIa. Sulfated non-saccharide glycosaminoglycan mimetics as promising anticoagulants

Allosteric inhibition of human factor XIa: discovery of monosulfated benzofurans as a class of promising inhibitors

Allosterism-based simultaneous, dual anticoagulant and antiplatelet action: allosteric inhibitor targeting the glycoprotein Ibα-binding and heparin-binding site of thrombin.

An electrophoresis-based assay for glycosyltransferase activity

An update on recent patents on thrombin inhibitors (2010 - 2013)

Application of molecular connectivity and electro-topological indices in quantitative structure-activity analysis of pyrazole derivatives as inhibitors of factor Xa and thrombin.

Capillary electrophoretic study of small, highly sulfated, non-sugar molecules interacting with antithrombin.

Characterization of the plasma and blood anticoagulant potential of structurally and mechanistically novel oligomers of 4-hydroxycinnamic acids

Chemical sulfation of small molecules—advances and challenges ⬇️

Chemoenzymatically prepared heparan sulfate containing rare 2-O-sulfonated glucuronic acid residues.

Conformational analysis of sucrose octasulfate by high resolution nuclear magnetic resonance spectroscopy

Crystal structures of influenza A virus matrix protein M1: variations on a theme

Designing "high-affinity, high-specificity" glycosaminoglycan sequences through computerized modeling

Designing allosteric inhibitors of factor XIa. Lessons from the interactions of sulfated pentagalloylglucopyranosides

Designing nonsaccharide, allosteric activators of antithrombin for accelerated inhibition of factor Xa.

Designing small, nonsugar activators of antithrombin using hydropathic interaction analyses.

Discovery methodology for the development of direct factor VIIa inhibitors.

Discovery of Allosteric Modulators of Factor XIa by Targeting Hydrophobic Domains Adjacent to Its Heparin-Binding Site ⬇️

Discovery of Sulfated Small Molecule Inhibitors of Matrix Metalloproteinase-8

Discovery of novel sulfonated small molecules that inhibit vascular tube formation ⬇️

Dynamic affinity chromatography in the separation of sulfated lignins binding to thrombin.

Electronically Rich N-Substituted Tetrahydroisoquinoline 3-Carboxylic Acid Esters: Concise Synthesis and Conformational Studies

Enzyme immobilization offers a robust tool to scale up the production of longer, diverse, natural glycosaminoglycan oligosaccharides

Exploring new non-sugar sulfated molecules as activators of antithrombin.

First steps in the direction of synthetic, allosteric, direct inhibitors of thrombin and factor Xa

Glycosaminoglycan-protein interaction studies using fluorescence spectroscopy.

Heparin interaction with a receptor on hyperglycemic dividing cells prevents intracellular hyaluronan synthesis and autophagy responses in models of type 1 diabetes.

High dose acetaminophen inhibits STAT3 and has free radical independent anti-cancer stem cell activity

Identification of a new functional domain in angiopoietin-like 3 (ANGPTL3) and angiopoietin-like 4 (ANGPTL4) involved in binding and inhibition of lipoprotein lipase (LPL).

Identification of the site of binding of sulfated, low molecular weight lignins on thrombin

Immobilization alters heparin cleaving properties of heparinase I.

Importance of lysine 125 for heparin binding and activation of antithrombin.

Importance of tryptophan 49 of antithrombin in heparin binding and conformational activation.

Inhibition of Herpes Simplex Virus-1 Entry into Human Cells by Nonsaccharide Glycosaminoglycan Mimetics

Inhibition of Human Cytomegalovirus Entry into Host Cells Through a Pleiotropic Small Molecule

Interaction of antithrombin with sulfated, low molecular weight lignins: opportunities for potent, selective modulation of antithrombin function.

Interaction of designed sulfated flavanoids with antithrombin: lessons on the design of organic activators.

Investigation of the heparin-thrombin interaction by dynamic force spectroscopy

Linear polyalkylamines as fingerprinting agents in capillary electrophoresis of low-molecular-weight heparins and glycosaminoglycans.

Lysines and Arginines play non-redundant roles in mediating chemokine-glycosaminoglycan interactions

Mechanism of Heparin Activation of Antithrombin: Evidence for an Induced-Fit Model of Allosteric Activation Involving Two Interaction Subsites ⬇️

Mechanism of heparin activation of antithrombin. Role of individual residues of the pentasaccharide activating sequence in the recognition of native and activated states of antithrombin.

Mechanism of poly(acrylic acid) acceleration of antithrombin inhibition of thrombin: implications for the design of novel heparin mimics.

Molecular Basis of Chemokine CXCL5-Glycosaminoglycan Interactions

New approaches for the preparation of hydrophobic heparin derivatives

New steroid haptens for radioimmunoassay: synthesis of steroids substituted with thioether or ester linkages at the 2 alpha-position

Novel heparin mimetics reveal cooperativity between exosite 2 and sodium-binding site of thrombin

Novel low molecular weight lignins as potential anti-emphysema agents: In vitro triple inhibitory activity against elastase, oxidation and inflammation.

On designing non-saccharide, allosteric activators of antithrombin.

On scaffold hopping: Challenges in the discovery of sulfated small molecules as mimetics of glycosaminoglycans ⬇️

On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients

Perspective on computational simulations of glycosaminoglycans

Plasmin regulation through allosteric, sulfated, small molecules.

Polymeric fluorescent heparin as one-step FRET substrate of human heparanase

Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.

Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.

Preface. Glycosaminoglycans

Preferential recognition and antagonism of SARS-CoV-2 spike glycoprotein binding to 3- O -sulfated heparan sulfate

Rapid and efficient microwave-assisted synthesis of highly sulfated organic scaffolds.

Rational design of potent, small, synthetic allosteric inhibitors of thrombin

Recent advances on plasmin inhibitors for the treatment of fibrinolysis-related disorders

Rigorous Analysis of Free Solution Glycosaminoglycan Dynamics Using Simple, New Tools

Role of arginine 129 in heparin binding and activation of antithrombin

Roles of N-terminal region residues Lys11, Arg13, and Arg24 of antithrombin in heparin recognition and in promotion and stabilization of the heparin-induced conformational change.

Serpin-glycosaminoglycan interactions.

Solution NMR characterization of chemokine CXCL8/IL-8 monomer and dimer binding to glycosaminoglycans: structural plasticity mediates differential binding interactions

Strategy for the sequence analysis of heparin