List of works - Shiva Malek

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

scientific article

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

scientific article published on 23 July 2013

A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade

scientific article

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

scientific article

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

scientific article published on 26 August 2016

Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900.

scientific article published on 19 July 2013

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

scientific article published on 11 March 2016

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

scientific article

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

scientific article

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

scientific article

Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1

scientific article

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

scientific article

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

scientific article

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

scientific article

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

scientific article

IκBα Functions through Direct Contacts with the Nuclear Localization Signals and the DNA Binding Sequences of NF-κB ⬇️

scientific article published on September 25, 1998

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

scientific article

Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1

scientific article

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

scientific article

Noncovalent wild-type-sparing inhibitors of EGFR T790M

scientific article published on 10 December 2012

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

scientific article

Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors

scientific article published on 01 October 2018

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

scientific article published on 15 April 2011

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

scientific article published on 12 December 2012

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

scientific article published on 17 December 2015

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

scientific article

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

scientific article

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling

scientific article

List of works by Shiva Malek

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900.

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

IκBα Functions through Direct Contacts with the Nuclear Localization Signals and the DNA Binding Sequences of NF-κB ⬇️

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Noncovalent wild-type-sparing inhibitors of EGFR T790M

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling