R. Heald

发表

Potent inhibition of telomerase by small-molecule pentacyclic acridines capable of interacting with G-quadruplexes.

M. Stevens, L. Kelland, M F Stevens, 2001, Molecular pharmacology.

Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance

A. Tutt, A. Nussenzweig, S. Boulton, 2021, Nature Communications.

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Steve Price, E. Bradley, BinQing Wei, 2013, Journal of medicinal chemistry.

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

C. Eigenbrot, Ivana Yen, S. Sideris, 2016, ACS medicinal chemistry letters.

Pharmacodynamics of the G-quadruplex-stabilizing telomerase inhibitor RHPS 4 in vitro : activity in human tumor cells correlates with telomere length and can be enhanced , or antagonized , with cytotoxic agents

C. Laughton, R. Heald, A. Burger, 2005 .

Antitumour polycyclic acridines. Palladium(0) mediated syntheses of quino[4,3,2-kl]acridines bearing peripheral substituents as potential telomere maintenance inhibitors.

M. Stevens, R. Heald, 2003, Organic & biomolecular chemistry.

Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.

M. Belvin, E. Bradley, M. Ultsch, 2013 .

Antitumor polycyclic acridines. 8.(1) Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts.

Charles A Laughton, Chetna Modi, C. Laughton, 2002, Journal of medicinal chemistry.

Recognition and stabilization of quadruplex DNA by a potent new telomerase inhibitor: NMR studies of the 2:1 complex of a pentacyclic methylacridinium cation with d(TTAGGGT)4

M. Searle, E. Gavathiotis, R. Heald, 2001 .

Conformationally restricted analogues of psorospermin: design, synthesis, and bioactivity of natural-product-related bisfuranoxanthones.

L. Hurley, Adam Siddiqui-Jain, T. Dexheimer, 2005, Journal of medicinal chemistry.

Synthesis and properties of bioactive 2- and 3-amino-8-methyl-8H-quino[4,3,2-kl]acridine and 8,13-dimethyl-8H-quino[4,3,2-kl]acridinium salts.

M. Stevens, R. Heald, I. Hutchinson, 2004, Organic & biomolecular chemistry.

Drug recognition and stabilisation of the parallel-stranded DNA quadruplex d(TTAGGGT)4 containing the human telomeric repeat.

M. Searle, E. Gavathiotis, R. Heald, 2003, Journal of Molecular Biology.

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

Ariana Peck, Shiuh-Ming Luoh, Steve Price, 2013, Nature.

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.

Siew K. Yeap, M. Ultsch, C. Eigenbrot, 2022, Journal of medicinal chemistry.

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

Siew K. Yeap, C. Eigenbrot, Ivana Yen, 2016, Journal of medicinal chemistry.

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

Belen Dominguez-Fernandez, C. Eigenbrot, Ivana Yen, 2015, Journal of medicinal chemistry.

Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation

Siew K. Yeap, C. Eigenbrot, Ivana Yen, 2014, Journal of medicinal chemistry.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

S. Steinbacher, Steve Price, E. Gancia, 2016, Journal of medicinal chemistry.

Pharmacodynamics of the G-Quadruplex-Stabilizing Telomerase Inhibitor 3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4) in Vitro: Activity in Human Tumor Cells Correlates with Telomere Length and Can Be Enhanced, or Antagonized, with Cytotoxic Agents

Charles A Laughton, C. Laughton, R. Heald, 2005, Molecular Pharmacology.

Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta.

V. Grinkevich, A. Turnbull, N. Holliday, 2022, Journal of medicinal chemistry.

Small-Molecule Polθ Inhibitors Provide Safe and Effective Tumor Radiosensitization in Preclinical Models

S. Boulton, V. Grinkevich, E. Hammond, 2022, bioRxiv.

Antitumor polycyclic acridines. 20. Search for DNA quadruplex binding selectivity in a series of 8,13-dimethylquino[4,3,2-kl]acridinium salts: telomere-targeted agents.

W. Wilson, J. Mergny, C. Laughton, 2008, Journal of medicinal chemistry.

5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.

Soraya S. Porres, P. Macfaul, P. Kenny, 2009, Bioorganic & medicinal chemistry letters.

Antitumor polycyclic acridines. 17. Synthesis and pharmaceutical profiles of pentacyclic acridinium salts designed to destabilize telomeric integrity.

M. Stevens, R. Heald, J. Cookson, 2005, Journal of medicinal chemistry.

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.

A. K. Forrest, BinQing Wei, M. Ultsch, 2017, ACS medicinal chemistry letters.

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.

Steve Price, BinQing Wei, D. Sutherlin, 2013, Bioorganic & medicinal chemistry letters.

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.

Steve Price, M. Belvin, BinQing Wei, 2013, Bioorganic & medicinal chemistry letters.

Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions.

P. Savy, Steve Price, M. Belvin, 2012, Journal of medicinal chemistry.

Abstract 312: The ATR inhibitor ART0380 shows preclinical efficacy in monotherapy or in combination with gemcitabine, aPD1, PARP inhibitors and topoisomerase 1 poisons

V. Grinkevich, E. Rajendra, M. Ranzani, 2023, Cancer Research.

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.

P. Savy, Steve Price, M. Ultsch, 2014, Bioorganic & medicinal chemistry letters.