J. Lyssikatos

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Chapter 17. Chemical Inhibitors of Cyclin-dependent Kinases

K. Coleman, J. Lyssikatos, B. Yang, 1997 .

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.

Adam R. Johnson, Jun Liang, J. DeVoss, 2013, Journal of medicinal chemistry.

Inhibition of Growth Factor Signaling by Small-Molecule Inhibitors of ErbB, Raf,and MEK

Ellen R. Laird, E. Laird, J. Lyssikatos, 2006 .

Progress towards therapeutic small molecule MEK inhibitors for use in cancer therapy.

J. Lyssikatos, K. Koch, J. Winkler, 2005, Current topics in medicinal chemistry.

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

Xianrui Zhao, Ignacio Aliagas, Ronen Marmorstein, 2015, ACS medicinal chemistry letters.

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

C. Ly, S. Sideris, S. Malek, 2011, Journal of medicinal chemistry.

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

K. Scearce-Levie, A. Beresford, A. Medhurst, 2012, Journal of medicinal chemistry.

Investigations into the Mechanisms of Pyridine Ring Cleavage in Vismodegib

J. Lyssikatos, H. Wong, C. Hop, 2014, Drug Metabolism and Disposition.

A Versatile Annulation Route to Primary-Amino-Substituted Naphthyridine Esters

J. Lyssikatos, Tao Wang, Zijin Xu, 2013 .

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Jane R Kenny, Michael Siu, Deepak Sampath, 2012, Journal of medicinal chemistry.

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Adam R. Johnson, N. C. Ray, Rohan V Mendonca, 2019, Bioorganic & medicinal chemistry letters.

Total Synthesis and Biological Evaluation of Tiancimycins A and B, Yangpumicin A, and Related Anthraquinone-Fused Enediyne Antitumor Antibiotics.

K. Nicolaou, M. Aujay, J. Lyssikatos, 2020, Journal of the American Chemical Society.

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

C. Ly, S. Sideris, S. Malek, 2012, Journal of medicinal chemistry.

Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451.

Jing Lin, B. D. Cohen, J. Lyssikatos, 2005, Cancer research.

Function and Physiology Lysosomal Storage Disease: Revealing Lysosomal

Sean P. Dougherty, M. Yaylaoglu, L. Honigberg, 2015 .

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

K. Scearce-Levie, A. Beresford, A. Medhurst, 2014, Journal of medicinal chemistry.

Dose-dependent exposure and metabolism of GNE-892, a β-secretase inhibitor, in monkeys: contributions by P450, AO, and P-gp

Xingrong Liu, J. Lyssikatos, C. Hop, 2015, European Journal of Drug Metabolism and Pharmacokinetics.

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.

A. Ebens, C. Noland, J. Lyssikatos, 2019, Journal of medicinal chemistry.

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

S. Sideris, S. Malek, J. Lyssikatos, 2013, Bioorganic & medicinal chemistry letters.

The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.

E. Laird, B. Brandhuber, G. Vigers, 2011, Bioorganic & medicinal chemistry letters.

Non-oxime inhibitors of B-Raf(V600E) kinase.

E. Laird, B. Brandhuber, G. Vigers, 2011, Bioorganic & medicinal chemistry letters.

Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.

J. Lyssikatos, K. Koch, R. Woessner, 2006, Journal of medicinal chemistry.

2.5 – Reactions of Activated Dienes with Aldehydes

M. Bednarski, J. Lyssikatos, 1991 .

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

M. Ultsch, C. Eigenbrot, Leslie B. Lee, 2013, Bioorganic & medicinal chemistry letters.

Minisci alkylations of electron-deficient pyrimidines with alkyl carboxylic acids

J. Lyssikatos, Anthony A. Estrada, D. Shore, 2015 .

Access to Saturated Fused PyrimidineDerivatives via a Flexible N-Vinyl TertiaryEnamide Synthesis

J. Lyssikatos, Anthony A. Estrada, Philippe Bergeron, 2011 .

Mild and General One-Pot Reductionand Cyclization of Aromatic and Heteroaromatic 2-Nitroaminesto Bicyclic 2H-Imidazoles

J. Lyssikatos, B. Chan, Anthony A. Estrada, 2010 .

Streamlined Processes for the Synthesis of a Farnesyl Transferase Inhibitor Drug Candidate

J. Lyssikatos, M. D’Occhio, J. Hawkins, 2004 .

Novel antibody–antibiotic conjugate eliminates intracellular S. aureus

P. S. Andersen, Laura DePalatis, Eric J. Brown, 2015, Nature.

Non-oxime pyrazole based inhibitors of B-Raf kinase.

E. Laird, B. Brandhuber, G. Vigers, 2011, Bioorganic & medicinal chemistry letters.

Potent and selective pyrazole-based inhibitors of B-Raf kinase.

Mike Welch, E. Laird, B. Brandhuber, 2008, Bioorganic & medicinal chemistry letters.

Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.

M. Mingueneau, J. Lyssikatos, T. Bohnert, 2021, Journal of medicinal chemistry.

Cyclic homopentapeptides 1. Analogs of tuberactinomycins and capreomycin with activity against vancomycin-resistant enterococci and Pasteurella

S. Miller, J. Lyssikatos, M. Lemay, 1997 .

Effect of selective LRRK2 kinase inhibition on nonhuman primate lung

Paula Katavolos, Brian K. Fiske, Reina N. Fuji, 2015, Science Translational Medicine.

Biological Characterization of ARRY-142886 (AZD6244), a Potent, Highly Selective Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor

Vivienne Marsh, S. Gross, B. Brandhuber, 2007, Clinical Cancer Research.

The Mutant p53-Conformation Modifying Drug, CP-31398, Can Induce Apoptosis

W. El-Deiry, D. Dicker, F. Rastinejad, 2002, Cancer biology & therapy.

Mitigation of opioid off-target effects and identification of structural drivers of opioid receptor engagement for BACE-1 small molecule inhibitors

Xingrong Liu, J. Lyssikatos, D. Dambach, 2015, Toxicology mechanisms and methods.

Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

J. E. Robinson, J. Lyssikatos, R. K. DeLisle, 2014, ACS medicinal chemistry letters.

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

M. Gill, G. Médard, E. Gancia, 2015, Journal of medicinal chemistry.

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

S. Sideris, L. Friedman, S. Malek, 2013, Journal of medicinal chemistry.

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

M. Belvin, C. Ly, S. Sideris, 2013, ACS medicinal chemistry letters.

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.

M. Volgraf, G. Vigers, Xingrong Liu, 2014, Bioorganic & medicinal chemistry letters.

8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.

K. Scearce-Levie, G. Vigers, Xingrong Liu, 2014, Journal of medicinal chemistry.

Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.

K. Scearce-Levie, M. Volgraf, G. Vigers, 2014, Journal of medicinal chemistry.

Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.

G. Vigers, Xingrong Liu, Darin J. Smith, 2013, Journal of medicinal chemistry.

Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.

K. Scearce-Levie, K. Stark, C. Ly, 2015, Journal of medicinal chemistry.

Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.

Jianping Yin, Xingrong Liu, J. Lyssikatos, 2017, Journal of medicinal chemistry.

Cyclic homopentapeptides 3. Synthetic modifications to the capreomycins and tuberactinomycins: Compounds with activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci

J. Lyssikatos, D. Whipple, R. Chandrasekaran, 1997 .

Cyclic homopentapeptides 2. Synthetic modifications of viomycin

J. Lyssikatos, L. Gerald, J. Clancy, 1997 .

Preparation and separation of antimicrobial agents derived from capreomycin

J. Lyssikatos, A. Allen, Daniel J. Watson, 2010 .

Cyclic Homopentapeptides. Part 3. Synthetic Modifications to the Capreomycins and Tuberactinomycins: Compounds with Activity Against Methicillin-Resistant Staphylococcus aureus and Vancomycin-Resistant Enterococci.

J. Lyssikatos, D. Whipple, R. Chandrasekaran, 1997 .

Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System.

J. Lyssikatos, Suzanne Tay, P. Fan, 2015, ACS medicinal chemistry letters.

Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

C. Brotherton-Pleiss, M. Volgraf, Jun Chen, 2018, Journal of medicinal chemistry.

α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.

Jun Chen, D. Hackos, J. Lyssikatos, 2016, Bioorganic & medicinal chemistry letters.

Germinal‐center kinase‐like kinase co‐crystal structure reveals a swapped activation loop and C‐terminal extension

C. Lukacs, L. Silvian, J. Lyssikatos, 2017, Protein science : a publication of the Protein Society.

Mechanistic Pharmacokinetic-Pharmacodynamic Modeling of BACE1 Inhibition in Monkeys: Development of a Predictive Model for Amyloid Precursor Protein Processing

K. Scearce-Levie, Xingrong Liu, J. Lyssikatos, 2013, Drug Metabolism and Disposition.

Evaluation of PNU-159682 antibody drug conjugates (ADCs).

V. Sisodiya, Samuel A. Williams, M. Aujay, 2020, Bioorganic & medicinal chemistry letters.

Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.

A. Ebens, J. Lyssikatos, John G. Moffat, 2015, Bioorganic & medicinal chemistry letters.

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

Ivana Yen, S. Sideris, S. Malek, 2014, Bioorganic & medicinal chemistry letters.

Dose-dependent exposure and metabolism of GNE-892, a β-secretase inhibitor, in monkeys: contributions by P450, AO, and P-gp

Xingrong Liu, J. Lyssikatos, C. Hop, 2015, European Journal of Drug Metabolism and Pharmacokinetics.

Synthesis of the 4,5 diphosphonate analog of D,L-myo-inositol 4,5-diphosphate

M. Bednarski, J. Lyssikatos, 1993 .

Abstract 2515: Preclinical Development of ARRY-162, A Potent and Selective MEK 1/2 Inhibitor

S. Gross, J. Lyssikatos, K. Koch, 2010 .

Evaluation of Metabolism and Disposition of GDC-0152 in Rats Using 14C Labeling Strategy at Two Different Positions: A Novel Formation of Hippuric Acid from 4-Phenyl-5-Amino-1,2,3-Thiadiazole

J. Ware, J. Lyssikatos, H. Wong, 2013, Drug Metabolism and Disposition.

Design, Synthesis, and Biological Evaluation of Tubulysin Analogues, Linker-Drugs, and Antibody-Drug Conjugates, Insights into Structure-Activity Relationships, and Tubulysin-Tubulin Binding Derived from X-ray Crystallographic Analysis.

K. Nicolaou, B. Nocek, M. Aujay, 2021, The Journal of organic chemistry.

Preclinical development of ARRY-142886, a potent and selective MEK inhibitor

S. Gross, B. Brandhuber, T. Morales, 2004 .

342 Anti-tumor activity, pharmacokinetic and pharmacodynamic effects of the MEK inhibitor ARRY-142886 (AZD6244) in a BxPC3 pancreatic tumor xenograft model

J. Lyssikatos, J. Winkler, S. Eckhardt, 2004 .

Abstract A143: ARRY-380, a selective HER2 inhibitor: From drug design to clinical evaluation.

E. Laird, S. Chia, V. Borges, 2011 .

Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System.

J. Lyssikatos, Suzanne Tay, P. Fan, 2015, ACS medicinal chemistry letters.

Abstract 2515: Preclinical Development of ARRY-162, A Potent and Selective MEK 1/2 Inhibitor

S. Gross, J. Lyssikatos, K. Koch, 2010 .

ARRY-334543, A potent, orally active small molecule inhibitor of EGFR and ErbB-2

T. Morales, J. Lyssikatos, George T. Topalov, 2005 .