S. Liras

发表

Fmoc-based synthesis of disulfide-rich cyclic peptides.

D. Craik, David A. Price, O. Cheneval, 2014, The Journal of organic chemistry.

The Future of Peptide‐based Drugs

D. Craik, David A. Price, S. Liras, 2013, Chemical biology & drug design.

Nonclassical Size Dependence of Permeation Defines Bounds for Passive Adsorption of Large Drug Molecules.

W. M. Hewitt, Chad E. Townsend, A. Mathiowetz, 2017, Journal of medicinal chemistry.

Peptidic macrocyclization via palladium-catalyzed chemoselective indole C-2 arylation.

K. James, David A. Price, S. Liras, 2012, Chemical communications.

Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase (ACC) Inhibitors Through Liver Targeting.

David A. Price, A. Kalgutkar, S. Liras, 2020, Journal of medicinal chemistry.

A Mild Method for the Preparation of 1,3,4-Oxadiazoles: Triflic Anhydride Promoted Cyclization of Diacylhydrazines

S. Liras, M. Allen, B. E. Segelstein, 2000 .

Chiral Sulfoxide-Induced Single Turn Peptide α-Helicity

F. Jiang, David A. Price, S. Liras, 2016, Scientific Reports.

Exploring Aromatic Chemical Space with NEAT: Novel and Electronically Equivalent Aromatic Template

Brajesh K. Rai, Alan M. Mathiowetz, Meihua Tu, 2012, J. Chem. Inf. Model..

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus

M. Ammirati, J. Treadway, S. Liras, 2011 .

Design and synthesis of truncated EGF-A peptides that restore LDL-R recycling in the presence of PCSK9 in vitro.

M. Ammirati, D. Craik, David A. Price, 2014, Chemistry & biology.

Organic synthesis using bridgehead carbocations and bridgehead enones

S. Liras, G. Kraus, P. J. Thomas, 1989 .

Ring closing metathesis mediated synthesis of 4a-aryloxodecahydroisoquinolines, intermediates in the preparation of novel opiates.

J. Blake, S. Liras, M. P. Allen, 2001, Organic letters.

Designing Orally Bioavailable Peptide and Peptoid Macrocycles

A. Mathiowetz, David A. Price, S. Liras, 2017 .

Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.

Jeffrey R. Chabot, J. Cate, J. Warmus, 2018, Journal of medicinal chemistry.

Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists.

D. Craik, P. Loria, David A. Price, 2015, European journal of medicinal chemistry.

Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue.

A. Mathiowetz, David A. Price, A. Kalgutkar, 2017, Organic & biomolecular chemistry.

Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence

Anne W. Schmidt, N. Grahame, S. Liras, 2011 .

Revisiting N-to-O acyl shift for synthesis of natural product-like cyclic depsipeptides.

A. Mathiowetz, David A. Price, A. Kalgutkar, 2014, Organic letters.

Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.

Jeffrey R. Chabot, P. Loria, C. Halldin, 2017, Angewandte Chemie.

Enantioselective, rhodium catalyzed intramolecular cyclopropanations of homoallylic diazoacetates.

S. Liras, S. Martin, C. Oalmann, 1992 .

A convergent method for the stereoselective synthesis of trisubstituted alkenes

S. Liras, S. Martin, R. Cherney, 1992 .

Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.

Bryan M. Li, David A. Price, A. Kalgutkar, 2013, Journal of medicinal chemistry.

Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.

K. Fennell, J. Pandit, F. Menniti, 2011, Journal of medicinal chemistry.

Biaryl piperidines as potent and selective delta opioid receptor ligands.

Anne W. Schmidt, S. Liras, Ernesto Callegari, 2010, Bioorganic & medicinal chemistry letters.

Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.

Spiros Liras, Anne W. Schmidt, J. Pandit, 2009, Journal of medicinal chemistry.

Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.

F. Menniti, F. Nelson, C. Proulx-Lafrance, 2012, Journal of medicinal chemistry.

A new regiochemical control element for diels-alder reactions

S. Liras, G. Kraus, 1989 .

Applications of vinylogous Mannich reactions. Total syntheses of the Ergot alkaloids rugulovasines A and B and setoclavine.

B. Vu, S. Liras, C. L. Lynch, 2001, Journal of the American Chemical Society.

Novel applications of vinylogous Mannich reactions. Total synthesis of rugulovasines A and B

S. Liras, S. Martin, 1993 .

Small-molecule phosphodiesterase probes: discovery of potent and selective CNS-penetrable quinazoline inhibitors of PDE1

M. Mansour, J. Pandit, F. Menniti, 2014 .

Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.

Spiros Liras, Meihua Tu, J. Pandit, 2007, Journal of medicinal chemistry.

An approach to the skeleton of the securinega alkaloids. The total synthesis of (+/-)-securinine.

S. Liras, J. Bordner, J. Davoren, 2001, Organic letters.

Highly Selective Enantiomer Differentiation in Intramolecular Cyclopropanation Reactions of Racemic Secondary Allylic Diazoacetates.

S. Liras, M. Spaller, M. Doyle, 1996 .

Novel approach to the zaragozic acids. Enantioselective total synthesis of 6,7-dideoxysqualestatin H5.

S. Liras, P. Kym, S. Martin, 2002, The Journal of organic chemistry.

ENANTIO- AND DIASTEREOSELECTIVITY IN THE INTRAMOLECULAR CYCLOPROPANATION OF SECONDARY ALLYLIC DIAZOACETATES

S. Liras, M. Spaller, S. Martin, 1994 .

An efficient synthesis of bridged heterocycles from an Ir(I) bis-amination/ring-closing metathesis sequence.

Spiros Liras, Cristiano R W Guimarães, S. Liras, 2012, Organic letters.

A Convergent Method for the Stereoselective Synthesis of Trisubstituted Alkenes.

S. Liras, S. Martin, R. Cherney, 2010 .

Enantioselective Intramolecular Cyclopropanations of Allylic and Homoallylic Diazoacetates and Diazoacetamides Using Chiral Dirhodium(II) Carboxamide Catalysts

S. Liras, M. Dwyer, M. Doyle, 1995 .

Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.

J. Blake, S. Liras, S. Mclean, 2000, Bioorganic & medicinal chemistry letters.

Enantioselective hydroarylation of bridged [3.2.1] heterocycles: an efficient entry into the homoepibatidine skeleton.

S. Liras, R. A. Brawn, K. McClure, 2013, Organic letters.

Efficient Liver Targeting by Polyvalent Display of a Compact Ligand for the Asialoglycoprotein Receptor.

M. Ammirati, David A. Price, S. Liras, 2017, Journal of the American Chemical Society.

Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products.

Matthew P Jacobson, Katrina W Lexa, Katrina W. Lexa, 2015, Journal of medicinal chemistry.

On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds

Yizhong Zhang, Matthew P. Jacobson, Alan M. Mathiowetz, 2011, Nature chemical biology.

Cyclopropanes as conformationally restricted peptide isosteres. Design and synthesis of novel collagenase inhibitors

S. Liras, S. Martin, C. Oalmann, 1993 .

Cyclic Penta- and Hexaleucine Peptides without N-Methylation Are Orally Absorbed.

Martin J. Stoermer, D. Craik, David A. Price, 2014, ACS medicinal chemistry letters.

Medicinal chemistry design principles for liver targeting through OATP transporters.

A. Mathiowetz, S. Liras, J. Pfefferkorn, 2013, Current topics in medicinal chemistry.

PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.

Roger M. Howard, S. Liras, K. Beaumont, 2020, Journal of medicinal chemistry.

Donated chemical probes for open science

Anton Simeonov, Steve Hitchcock, Stefan Laufer, 2018, eLife.

Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule

J. Cate, S. Liras, Wenfei Li, 2018, bioRxiv.

Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain

J. Doudna, J. Cate, P. Loria, 2017, PLoS biology.

Improving on nature: making a cyclic heptapeptide orally bioavailable.

Spiros Liras, David J Craik, D. Craik, 2014, Angewandte Chemie.

Short Hydrophobic Peptides with Cyclic Constraints Are Potent Glucagon-like Peptide-1 Receptor (GLP-1R) Agonists.

A. Mathiowetz, P. Loria, David A. Price, 2015, Journal of medicinal chemistry.

Biaryl-bridged macrocyclic peptides: conformational constraint via carbogenic fusion of natural amino acid side chains.

James C. Collins, K. James, A. Mathiowetz, 2012, The Journal of organic chemistry.

Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.

Jing Chen, David B Duignan, Robert Aiello, 2012, Journal of medicinal chemistry.

Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.

J. Pandit, F. Menniti, S. Liras, 2018, Journal of Medicinal Chemistry.

A compound that directly and selectively stalls PCSK9 translation

J. Doudna, J. Cate, P. Loria, 2016, bioRxiv.

Title : A compound that directly and selectively stalls PCSK 9 translation 1 2

J. Cate, P. Loria, S. Liras, 2016 .

Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.

A. Mathiowetz, David A. Price, A. Kalgutkar, 2017, Journal of medicinal chemistry.

Rational design and synthesis of an orally bioavailable peptide guided by NMR amide temperature coefficients

David J. Craik, David P. Fairlie, Spiros Liras, 2014, Proceedings of the National Academy of Sciences.

Selective Brain Penetrant PDE 9 A Inhibitor for the Treatment of Cognitive Disorders

Ey, F. Menniti, F. Nelson, 2012 .

Permeability of Cyclic Peptide Macrocycles and Cyclotides and Their Potential as Therapeutics.

S. Liras, K. McClure, 2019, ACS medicinal chemistry letters.

Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides.

A. Mathiowetz, David A. Price, A. Kalgutkar, 2015, Organic letters.

Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance().

Yizhong Zhang, Matthew P Jacobson, Spiros Liras, 2012, MedChemComm.

Use of 3D Properties to Characterize Beyond Rule-of-5 Property Space for Passive Permeation

Cristiano Ruch Werneck Guimarães, Alan M. Mathiowetz, Marina Shalaeva, 2012, J. Chem. Inf. Model..

Synthesis of 4,11-dideoxydaunomycinone by a Claisen/Diels-Alder sequence

S. Liras, G. Kraus, M. Molina, 1989 .

Discovery and pharmacological characterization of a selective delta opiate receptor antagonist (CP-646,777)

Anne W. Schmidt, S. Liras, Ernesto Callegari, 2011 .

Truncated Glucagon-like Peptide-1 and Exendin-4 α-Conotoxin pl14a Peptide Chimeras Maintain Potency and α-Helicity and Reveal Interactions Vital for cAMP Signaling in Vitro*

D. Craik, P. Loria, David A. Price, 2016, The Journal of Biological Chemistry.

Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing.

Kaihong Zhou, Spiros Liras, Meihua Tu, 2018, Journal of the American Chemical Society.

Comparative α-helicity of cyclic pentapeptides in water.

David A. Price, S. Liras, D. Fairlie, 2014, Angewandte Chemie.

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Anne W. Schmidt, F. Menniti, F. Nelson, 2009, Journal of medicinal chemistry.

Functionalization of aromatic amino acids via direct C-H activation: generation of versatile building blocks for accessing novel peptide space.

K. James, S. Liras, A. Guzman-Perez, 2010, Organic letters.

Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.

Laura McDowell, Spiros Liras, Mihaly Hajos, 2012, Journal of medicinal chemistry.

Translational diffusion of cyclic peptides measured using pulsed-field gradient NMR.

A. Mathiowetz, D. Craik, David A. Price, 2014, The journal of physical chemistry. B.

Exploring experimental and computational markers of cyclic peptides: Charting islands of permeability.

Spiros Liras, D. Craik, David A. Price, 2015, European journal of medicinal chemistry.

Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule

J. Cate, S. Liras, Wenfei Li, 2019, Nature Structural & Molecular Biology.

Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling.

P. Loria, David A. Price, S. Liras, 2017, European journal of medicinal chemistry.

Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).

Gregory W. Kauffman, Anne W. Schmidt, S. Liras, 2011, Journal of medicinal chemistry.

Improving on nature: making a cyclic heptapeptide orally bioavailable.

D. Craik, S. Liras, D. Fairlie, 2014, Angewandte Chemie.

Exploring Aromatic Chemical Space with NEAT: Novel and Electronically Equivalent Aromatic Template

A. Mathiowetz, S. Liras, M. Hayward, 2012, Journal of Chemical Information and Modeling.

Translational diffusion of cyclic peptides measured using pulsed-field gradient NMR.

A. Mathiowetz, D. Craik, P. Harvey, 2014, The journal of physical chemistry. B.