K. Andrews

发表

Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.

Kristin L. Andrews, B. Herberich, Matthew R. Lee, 2016, Bioorganic & medicinal chemistry letters.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Kristin L. Andrews, Jiandong Zhang, S. Chmait, 2015, Journal of medicinal chemistry.

The discovery and optimization of aminooxadiazoles as potent Pim kinase inhibitors.

Kristin L. Andrews, B. Herberich, Matthew R. Lee, 2015, Bioorganic & medicinal chemistry letters.

Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.

Daniel J. Freeman, R. Wahl, J. McCarter, 2011, Journal of medicinal chemistry.

Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).

E. Hu, S. Chmait, J. Treanor, 2014, ACS medicinal chemistry letters.

The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.

Matthew R. Lee, Xin Huang, A. Tasker, 2015, Bioorganic & medicinal chemistry letters.

Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.

Daniel J. Freeman, J. McCarter, Nancy Zhang, 2012, Journal of medicinal chemistry.

Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.

Daniel J. Freeman, J. McCarter, Nancy Zhang, 2011, Journal of medicinal chemistry.

Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.

Xiaolin Hao, Ben Fisher, Andreas Reichelt, 2015, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.

Daniel J. Freeman, J. McCarter, Nancy Zhang, 2012, Bioorganic & medicinal chemistry letters.

Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.

E. Lobenhofer, Kristin L. Andrews, B. Herberich, 2015, ACS medicinal chemistry letters.

Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.

J. McCarter, D. Whittington, A. Tasker, 2014, Bioorganic & medicinal chemistry letters.

Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators.

H. Bregman, L. Berry, Liyue Huang, 2017, European journal of medicinal chemistry.

Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.

Daniel J. Freeman, J. McCarter, D. Whittington, 2012, Journal of medicinal chemistry.

Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3).

E. Hu, R. Kunz, Shannon Rumfelt, 2012, Bioorganic & medicinal chemistry letters.

Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V

J. B. Jordan, Kristin L. Andrews, R. Stöcklin, 2018, PloS one.

Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3.

J. Sullivan, C. Gegg, J. Werner, 2015, Journal of medicinal chemistry.

Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.

L. Poppe, Kristin L. Andrews, R. Stöcklin, 2015, Journal of Medicinal Chemistry.

Engineering NaV1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics.

Kristin L. Andrews, B. Herberich, B. Moyer, 2019, ACS chemical biology.

Unfolded Protein Response in Cancer: IRE1α Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability.

A. Tasker, R. Kendall, J. Lipford, 2015, ACS medicinal chemistry letters.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.

R. Wahl, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

R. Wahl, Jiandong Zhang, S. Chmait, 2013, Nature.

The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.

J. McCarter, D. Whittington, Nancy Zhang, 2015, Bioorganic & medicinal chemistry letters.

Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.

K. Rex, J. Canon, B. Herberich, 2019, Journal of medicinal chemistry.

Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.

K. Rex, B. Herberich, Matthew R. Lee, 2016, Journal of medicinal chemistry.

Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.

K. Rex, B. Herberich, Matthew R. Lee, 2016, ACS medicinal chemistry letters.

Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.

Matthew R. Lee, A. Tasker, Bin Wu, 2015, Bioorganic & medicinal chemistry letters.

Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

E. Hu, R. Kunz, Shannon Rumfelt, 2013, Journal of medicinal chemistry.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

E. Hu, R. Kunz, N. Chen, 2014, Journal of medicinal chemistry.

Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.

E. Hu, R. Kunz, Shannon Rumfelt, 2012, Bioorganic & medicinal chemistry letters.

Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.

Daniel J. Freeman, Hongyu Liao, Nancy Zhang, 2011, Journal of medicinal chemistry.

Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the NaV1.7 Inhibitory Peptide GpTx-1.

L. Poppe, B. Moyer, S. McDonough, 2016, Journal of medicinal chemistry.

Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).

Kristin L. Andrews, D. Powers, R. Kendall, 2015, Journal of medicinal chemistry.

1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition.

Kristin L. Andrews, R. Fremeau, M. Chu-Moyer, 2018, Bioorganic & medicinal chemistry letters.

The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.

H. Bregman, Xin Huang, Liyue Huang, 2017, Journal of medicinal chemistry.

Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.

E. Hu, R. Kunz, N. Chen, 2014, Bioorganic & medicinal chemistry.

Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.

E. Hu, Shannon Rumfelt, N. Chen, 2012, Bioorganic & medicinal chemistry letters.

Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.

Dong Liu, Kristin L. Andrews, Zhulun Wang, 2018, Journal of medicinal chemistry.

Sustained inhibition of the NaV1.7 sodium channel by engineered dimers of the domain II binding peptide GpTx-1.

L. Poppe, Kristin L. Andrews, S. Meng, 2015, Bioorganic & medicinal chemistry letters.

Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.

E. Lobenhofer, B. Herberich, A. Tasker, 2015, ACS Medicinal Chemistry Letters.

Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.

L. Poppe, R. Stöcklin, B. Moyer, 2015, Journal of medicinal chemistry.

E. Hu, R. Kunz, N. Chen, 2014, Journal of medicinal chemistry.