List of works - Amarnath Natarajan

2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: a structure-activity relationship study

scientific article

3,3-diaryl-1,3-dihydroindol-2-ones as antiproliferatives mediated by translation initiation inhibition.

scientific article published on April 2004

A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells.

scientific article

A mitotic CDK5-PP4 phospho-signaling cascade primes 53BP1 for DNA repair in G1

scientific article published on 18 September 2019

A quinoxaline urea analog uncouples inflammatory and pro-survival functions of IKKβ

scientific article

A simple fluorescent assay for the discovery of protein-protein interaction inhibitors

scientific article published on 30 January 2019

Anticancer activity of Celastrol in combination with ErbB2-targeted therapeutics for treatment of ErbB2-overexpressing breast cancers

scientific article

Beyond the frog: the evolution of homology models of human IKKβ.

scientific article

CDK5 Inhibitor Downregulates Mcl-1 and Sensitizes Pancreatic Cancer Cell Lines to Navitoclax

scientific article published on 01 October 2019

Catalytically inactive Dnmt3b rescues mouse embryonic development by accessory and repressive functions

scientific article published on 26 September 2019

Characterization of CDK(5) inhibitor, 20-223 (aka CP668863) for colorectal cancer therapy.

scientific article published on 28 December 2017

Characterization of Promiscuous Binding of Phosphor Ligands to Breast-Cancer-Gene 1 (BRCA1) C-Terminal (BRCT): Molecular Dynamics, Free Energy, Entropy and Inhibitor Design

scientific article

Chemical Genetic Screens Identify Kinase Inhibitor Combinations that Target Anti-Apoptotic Proteins for Cancer Therapy.

scientific article published on 5 April 2018

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC).

scientific article published on 21 June 2017

Computational and experimental studies of the interaction between phospho-peptides and the C-terminal domain of BRCA1.

scientific article

Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy

scientific article

Development of 1-((1,4-trans)-4-Aryloxycyclohexyl)-3-arylurea Activators of Heme-Regulated Inhibitor as Selective Activators of the Eukaryotic Initiation Factor 2 Alpha (eIF2α) Phosphorylation Arm of the Integrated Endoplasmic Reticulum Stress Respo

scientific article published on 19 June 2017

Discovery and characterization of small molecule Rac1 inhibitors

scientific article published on 29 March 2017

Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction

scientific article

Erratum to: Inhibition of BRCT(BRCA1)-phosphoprotein interaction enhances the cytotoxic effect of olaparib in breast cancer cells: a proof of concept study for synthetic lethal therapeutic option

scientific article published on 01 February 2016

Exploiting the P-1 pocket of BRCT domains toward a structure guided inhibitor design

scientific article

Explorations of substituted urea functionality for the discovery of new activators of the heme-regulated inhibitor kinase

scientific article

Face selective reduction of the exocyclic double bond in isatin derived spirocyclic lactones.

scientific article published on 19 November 2012

Fbxo7 promotes Cdk6 activity to inhibit PFKP and glycolysis in T cells

scientific article published in 2022

Ferulic acid dimer as a non-opioid therapeutic for acute pain.

scientific article

High-throughput compatible fluorescence resonance energy transfer-based assay to identify small molecule inhibitors of AMSH deubiquitinase activity

scientific article published on 5 June 2013

High-throughput fluorescence polarization assay to identify inhibitors of Cbl(TKB)-protein tyrosine kinase interactions

scientific article

High-throughput fluorescence polarization assay to identify small molecule inhibitors of BRCT domains of breast cancer gene 1.

scientific article published on 3 February 2006

Human Apurinic/Apyrimidinic Endonuclease (APE1) Is Acetylated at DNA Damage Sites in Chromatin, and Acetylation Modulates Its DNA Repair Activity

scientific article published on 19 December 2016

Identification of the DNA-Binding Domains of Human Replication Protein A That Recognize G-Quadruplex DNA

scientific article

Impact of structurally modifying hyaluronic acid on CD44 interaction.

scientific article published on 20 September 2017

Inhibition of BRCT(BRCA1)-phosphoprotein interaction enhances the cytotoxic effect of olaparib in breast cancer cells: a proof of concept study for synthetic lethal therapeutic option

scientific article

Irreversible binding of an anticancer compound (BI-94) to plasma proteins

scientific article

Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study

scientific article published on 14 April 2016

Micellar formulation of indocyanine green for phototherapy of melanoma

scientific article published on 16 October 2015

Mouse Pancreatic Tumor Model Independent of Tumor Suppressor Gene Inactivation

scientific article published on 01 May 2018

Mutant Cbl proteins as oncogenic drivers in myeloproliferative disorders

scientific article

Novel arylsulfoanilide-oxindole hybrid as an anticancer agent that inhibits translation initiation.

scientific article published on October 2004

Novel treatment for mantle cell lymphoma including therapy-resistant tumor by NF-κB and mTOR dual-targeting approach.

scientific article published on 20 August 2013

Peptide truncation leads to a twist and an unusual increase in affinity for casitas B-lineage lymphoma tyrosine kinase binding domain

scientific article

Perturbing pro-survival proteins using quinoxaline derivatives: A structure–activity relationship study ⬇️

scientific article published on February 16, 2012

Pharmacokinetics, protein binding and metabolism of a quinoxaline urea analog as an NF-κB inhibitor in mice and rats by LC-MS/MS.

scientific article

Poly-L-proline type II peptide mimics as probes of the active site occupancy requirements of cGMP-dependent protein kinase

scientific article published on 01 October 2005

Poly-L-proline type II peptide mimics based on the 3-azabicyclo[3.1.0]hexane system

scientific article

Protein tyrosine kinase regulation by ubiquitination: critical roles of Cbl-family ubiquitin ligases

scientific article

Protein-protein interactions as therapeutic targets in neuropsychopharmacology

scientific article published on January 2009

Pulse design for broadband correlation NMR spectroscopy by multi-rotating frames.

scientific article

RAC1 GTPase promotes the survival of breast cancer cells in response to hyper-fractionated radiation treatment

scientific article

Recent Advances in Cancer Drug Development: Targeting Induced Myeloid Cell Leukemia-1 (Mcl-1) Differentiation Protein

scientific article published on 11 September 2017

Recent Advances in EPAC-Targeted Therapies: A Biophysical Perspective

scientific article published on 19 November 2019

Selective degradation of CDK6 by a palbociclib based PROTAC

scientific article published on 26 March 2019

Small molecule adenosine 5'-monophosphate activated protein kinase (AMPK) modulators and human diseases

scientific article

Structural characterization of BRCT-tetrapeptide binding interactions.

scientific article

Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors.

scientific article published on 2 October 2017

Structure-activity relationship studies to probe the phosphoprotein binding site on the carboxy terminal domains of the breast cancer susceptibility gene 1.

scientific article published on 26 May 2011

Symbiotic Prodrugs (SymProDs) Dual Targeting of NFkappaB and CDK

scientific article published on 31 March 2020

Synthesis and biological evaluation of thiazolidine-2,4-dione and 2,4-thione derivatives as inhibitors of translation initiation.

scientific article published on November 2004

Synthesis and evaluation of macrocyclic diarylether heptanoid natural products and their analogs

scientific article

Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides

scientific article (publication date: November 2007)

Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy

scientific article published on 15 October 2018

Synthesis of conformationally constrained lysine analogues

scientific article published on 01 June 2006

Synthesis of fluorescein labeled 7-methylguanosinemonophosphate

scientific article published in May 2004

Synthesis of unnatural amino acid derivatives via palladium catalyzed 1,4 addition of boronic acids.

scientific article published on May 2010

Targeting the NF-κB and mTOR pathways with a quinoxaline urea analog that inhibits IKKβ for pancreas cancer therapy

scientific article published on 26 February 2013

The paradox of conformational constraint in the design of Cbl(TKB)-binding peptides

scientific article

Thermodynamics of phosphopeptide tethering to BRCT: the structural minima for inhibitor design

scientific article published on 09 August 2007

List of works by Amarnath Natarajan

2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: a structure-activity relationship study

3,3-diaryl-1,3-dihydroindol-2-ones as antiproliferatives mediated by translation initiation inhibition.

A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells.

A mitotic CDK5-PP4 phospho-signaling cascade primes 53BP1 for DNA repair in G1

A quinoxaline urea analog uncouples inflammatory and pro-survival functions of IKKβ

A simple fluorescent assay for the discovery of protein-protein interaction inhibitors

Anticancer activity of Celastrol in combination with ErbB2-targeted therapeutics for treatment of ErbB2-overexpressing breast cancers

Beyond the frog: the evolution of homology models of human IKKβ.

CDK5 Inhibitor Downregulates Mcl-1 and Sensitizes Pancreatic Cancer Cell Lines to Navitoclax

Catalytically inactive Dnmt3b rescues mouse embryonic development by accessory and repressive functions

Characterization of CDK(5) inhibitor, 20-223 (aka CP668863) for colorectal cancer therapy.

Characterization of Promiscuous Binding of Phosphor Ligands to Breast-Cancer-Gene 1 (BRCA1) C-Terminal (BRCT): Molecular Dynamics, Free Energy, Entropy and Inhibitor Design

Chemical Genetic Screens Identify Kinase Inhibitor Combinations that Target Anti-Apoptotic Proteins for Cancer Therapy.

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC).

Computational and experimental studies of the interaction between phospho-peptides and the C-terminal domain of BRCA1.

Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy

Development of 1-((1,4-trans)-4-Aryloxycyclohexyl)-3-arylurea Activators of Heme-Regulated Inhibitor as Selective Activators of the Eukaryotic Initiation Factor 2 Alpha (eIF2α) Phosphorylation Arm of the Integrated Endoplasmic Reticulum Stress Respo

Discovery and characterization of small molecule Rac1 inhibitors

Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction

Erratum to: Inhibition of BRCT(BRCA1)-phosphoprotein interaction enhances the cytotoxic effect of olaparib in breast cancer cells: a proof of concept study for synthetic lethal therapeutic option

Exploiting the P-1 pocket of BRCT domains toward a structure guided inhibitor design

Explorations of substituted urea functionality for the discovery of new activators of the heme-regulated inhibitor kinase

Face selective reduction of the exocyclic double bond in isatin derived spirocyclic lactones.

Fbxo7 promotes Cdk6 activity to inhibit PFKP and glycolysis in T cells

Ferulic acid dimer as a non-opioid therapeutic for acute pain.

High-throughput compatible fluorescence resonance energy transfer-based assay to identify small molecule inhibitors of AMSH deubiquitinase activity

High-throughput fluorescence polarization assay to identify inhibitors of Cbl(TKB)-protein tyrosine kinase interactions

High-throughput fluorescence polarization assay to identify small molecule inhibitors of BRCT domains of breast cancer gene 1.

Human Apurinic/Apyrimidinic Endonuclease (APE1) Is Acetylated at DNA Damage Sites in Chromatin, and Acetylation Modulates Its DNA Repair Activity

Identification of the DNA-Binding Domains of Human Replication Protein A That Recognize G-Quadruplex DNA

Impact of structurally modifying hyaluronic acid on CD44 interaction.

Inhibition of BRCT(BRCA1)-phosphoprotein interaction enhances the cytotoxic effect of olaparib in breast cancer cells: a proof of concept study for synthetic lethal therapeutic option

Irreversible binding of an anticancer compound (BI-94) to plasma proteins

Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study

Micellar formulation of indocyanine green for phototherapy of melanoma

Mouse Pancreatic Tumor Model Independent of Tumor Suppressor Gene Inactivation

Mutant Cbl proteins as oncogenic drivers in myeloproliferative disorders

Novel arylsulfoanilide-oxindole hybrid as an anticancer agent that inhibits translation initiation.

Novel treatment for mantle cell lymphoma including therapy-resistant tumor by NF-κB and mTOR dual-targeting approach.

Peptide truncation leads to a twist and an unusual increase in affinity for casitas B-lineage lymphoma tyrosine kinase binding domain

Perturbing pro-survival proteins using quinoxaline derivatives: A structure–activity relationship study ⬇️

Pharmacokinetics, protein binding and metabolism of a quinoxaline urea analog as an NF-κB inhibitor in mice and rats by LC-MS/MS.

Poly-L-proline type II peptide mimics as probes of the active site occupancy requirements of cGMP-dependent protein kinase

Poly-L-proline type II peptide mimics based on the 3-azabicyclo[3.1.0]hexane system

Protein tyrosine kinase regulation by ubiquitination: critical roles of Cbl-family ubiquitin ligases

Protein-protein interactions as therapeutic targets in neuropsychopharmacology

Pulse design for broadband correlation NMR spectroscopy by multi-rotating frames.

RAC1 GTPase promotes the survival of breast cancer cells in response to hyper-fractionated radiation treatment

Recent Advances in Cancer Drug Development: Targeting Induced Myeloid Cell Leukemia-1 (Mcl-1) Differentiation Protein

Recent Advances in EPAC-Targeted Therapies: A Biophysical Perspective

Selective degradation of CDK6 by a palbociclib based PROTAC

Small molecule adenosine 5'-monophosphate activated protein kinase (AMPK) modulators and human diseases

Structural characterization of BRCT-tetrapeptide binding interactions.

Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors.

Structure-activity relationship studies to probe the phosphoprotein binding site on the carboxy terminal domains of the breast cancer susceptibility gene 1.

Symbiotic Prodrugs (SymProDs) Dual Targeting of NFkappaB and CDK

Synthesis and biological evaluation of thiazolidine-2,4-dione and 2,4-thione derivatives as inhibitors of translation initiation.

Synthesis and evaluation of macrocyclic diarylether heptanoid natural products and their analogs

Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides

Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy

Synthesis of conformationally constrained lysine analogues

Synthesis of fluorescein labeled 7-methylguanosinemonophosphate

Synthesis of unnatural amino acid derivatives via palladium catalyzed 1,4 addition of boronic acids.

Targeting the NF-κB and mTOR pathways with a quinoxaline urea analog that inhibits IKKβ for pancreas cancer therapy

The paradox of conformational constraint in the design of Cbl(TKB)-binding peptides

Thermodynamics of phosphopeptide tethering to BRCT: the structural minima for inhibitor design