D. Heerding

发表

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.

A. Hassell, R. Gampe, J. Axten, 2013, ACS medicinal chemistry letters.

Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.

S. Rabindran, N. Campobasso, V. Sudakin, 2011, Journal of medicinal chemistry.

Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.

K. Ward, K. Erhard, R. Calvo, 2000, Journal of medicinal chemistry.

Discovery of a Novel and Potent Class of FabI-Directed Antibacterial Agents

Martha S. Head, Xiayang Qiu, Cheryl A. Janson, 2002, Antimicrobial Agents and Chemotherapy.

Discovery of Novel AKT Inhibitors with Enhanced Anti-Tumor Effects in Combination with the MEK Inhibitor

Ming-Chih Crouthamel, Rakesh Kumar, S. Rabindran, 2014, PloS one.

Generation and Validation of Intracellular Ubiquitin Variant Inhibitors for USP7 and USP10.

J. Moffat, Taras Makhnevych, S. Sidhu, 2017, Journal of molecular biology.

New benzimidazoles as thrombopoietin receptor agonists.

R. Keenan, D. Heerding, C. Erickson-Miller, 2006, Bioorganic & medicinal chemistry letters.

Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin αvβ3) antagonists

K. Ward, R. Willette, T. Yue, 2003 .

Chapter 23 Small Molecule Inhibitors of AKT/PKB Kinase as a Strategy for Treating Cancer

D. Heerding, S. Verma, I. Safonov, 2007 .

Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.

J. Luengo, A. P. Graves, M. Pappalardi, 2019, ACS medicinal chemistry letters.

Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.

J. Luengo, D. Yamashita, D. Heerding, 2009, Bioorganic & medicinal chemistry letters.

Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia

Peter A. Jones, Philip J. Chapman, P. Grandi, 2021, Nature Cancer.

Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.

G. Warren, R. Copeland, T. J. Lansing, 2008, Journal of medicinal chemistry.

1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI).

C. Janson, A. Fosberry, Ward W. Smith, 2001, Bioorganic & medicinal chemistry letters.

Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI).

Xiayang Qiu, David J Payne, M. Head, 2002, Journal of medicinal chemistry.

New benzylidenethiazolidinediones as antibacterial agents.

D. Heerding, D. Holmes, S. Rittenhouse, 2003, Bioorganic & medicinal chemistry letters.

Structure-activity relationships of novel hematoregulatory peptides.

A. Cuthbertson, D. Heerding, E. Agner, 1996, Journal of medicinal chemistry.

Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).

L. Shewchuk, S. Rabindran, A. Hassell, 2012, Journal of medicinal chemistry.

Studies on the synthesis of (−)-neplanocin A: homochiral preparation of a key cyclopentanoid intermediate

D. Heerding, D. Myles, Soroosh Shambayati, 1988 .

New benzylidenethiazolidinediones as antibacterial agents.

D. Heerding, D. Holmes, S. Rittenhouse, 2003, Bioorganic & medicinal chemistry letters.

Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity.

Robert A Copeland, Anthony E Choudhry, T. Gilmer, 2008, Cancer research.

Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction.

Neysa Nevins, D. Mcnulty, A. Gilmartin, 2014, Nature chemical biology.

Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity

Leanna E. Shuster, K. Evans, S. Sweitzer, 2015, Molecular Pharmacology.

Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors.

Xiaodong Cheng, Xing Zhang, M. Pappalardi, 2022, Structure.

Combinatorial chemistry. Use of an intramolecular ruthenium catalyzed olefin/alkyne metathesis reaction in tandem with a Diels-Alder cycloaddition reaction to construct functionalized hexahydroisoindoles

D. Heerding, W. Huffman, C. Kwon, 1998 .

2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.

J. Luengo, D. Yamashita, D. Heerding, 2010, Bioorganic & medicinal chemistry letters.

Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.

Sharad Verma, Kristin K. Brown, Anthony E Choudhry, 2010, Bioorganic & medicinal chemistry letters.

Aminofurazans as potent inhibitors of AKT kinase.

D. Heerding, E. Minthorn, N. Concha, 2009, Bioorganic & medicinal chemistry letters.

Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.

Douglas W. Thomson, Zhengrong Zhu, J. Boehm, 2022, Journal of medicinal chemistry.

Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.

J. Briand, N. Campobasso, J. Axten, 2010, ACS medicinal chemistry letters.

Abstract 2994: Discovery of selective, noncovalent small molecule inhibitors of DNMT1 as an alternative to traditional DNA hypomethylating agents

J. Briand, R. Prinjha, Mark Cockerill, 2018, Molecular and Cellular Biology / Genetics.

Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c-MYC Protein Levels in Cells.

J. F. Mack, L. Lafrance, R. Rivero, 2021, Journal of medicinal chemistry.

2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.

Kristin K. Brown, J. Luengo, Rakesh Kumar, 2010, Bioorganic & medicinal chemistry letters.

Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity

Leanna E. Shuster, K. Evans, C. Buser, 2015, Molecular Pharmacology.

Design and synthesis of aminopyridine containing biaryls reducing c-MYC protein levels in cells.

J. F. Mack, Leanna E. Shuster, R. Rivero, 2023, Bioorganic & medicinal chemistry letters.

Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors.

Xiaodong Cheng, Xing Zhang, M. Pappalardi, 2022, Structure.