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

Nature communications, 2021-06, Vol.12 (1), p.3636-15, Article 3636

2021

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Quantitative, titratable and high-throughput reporter assays to measure DNA double strand break repair activity in cells

Nucleic acids research, 2024-02, Vol.52 (4), p.1736-1752

2024

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

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16589-16621

2022

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

Nature (London), 2013-09, Vol.501 (7466), p.232-236

2013

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Common Marginal Cold Pools

Journal of applied meteorology and climatology, 2015-02, Vol.54 (2), p.339-351

2015

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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

Journal of medicinal chemistry, 2013-06, Vol.56 (11), p.4597-4610

2013

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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)

Journal of medicinal chemistry, 2016-02, Vol.59 (3), p.985-1002

2016

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

Clinical cancer research, 2023-04, Vol.29 (8), p.1631-1642

2023

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

Journal of medicinal chemistry, 2023-03, Vol.66 (5), p.3649-3649

2023

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

Journal of medicinal chemistry, 2014-12, Vol.57 (23), p.10176-10191

2014

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

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.9080-9093

2016

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Drug Recognition and Stabilisation of the Parallel-stranded DNA Quadruplex d(TTAGGGT) 4 Containing the Human Telomeric Repeat

Journal of molecular biology, 2003-11, Vol.334 (1), p.25-36

2003

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Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions

Journal of medicinal chemistry, 2012-05, Vol.55 (10), p.4594-4604

2012

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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

Journal of medicinal chemistry, 2008-02, Vol.51 (4), p.963-975

2008

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Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

ACS medicinal chemistry letters, 2017-09, Vol.8 (9), p.936-940

2017

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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

Molecular pharmacology, 2005-12, Vol.68 (6), p.1551-1558

2005

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The effects of forest management on plant species diversity in a Sierran conifer forest

Forest ecology and management, 2001-06, Vol.146 (1), p.211-222

2001

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Potent Inhibition of Telomerase by Small-Molecule Pentacyclic Acridines Capable of Interacting with G-Quadruplexes

Molecular pharmacology, 2001-11, Vol.60 (5), p.981-988

2001

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Edge effects in mixed conifer group selection openings: tree height response to resource gradients

Forest ecology and management, 2003-07, Vol.179 (1), p.107-121

2003

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Group selection management in conifer forests: relationships between opening size and tree growth

Canadian journal of forest research, 2004-03, Vol.34 (3), p.630-641

2004

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Antitumor Polycyclic Acridines. 17. Synthesis and Pharmaceutical Profiles of Pentacyclic Acridinium Salts Designed To Destabilize Telomeric Integrity

Journal of medicinal chemistry, 2005-11, Vol.48 (23), p.7198-7207

2005

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Antitumor Polycyclic Acridines. 8. Synthesis and Telomerase-Inhibitory Activity of Methylated Pentacyclic Acridinium Salts

Journal of medicinal chemistry, 2002-01, Vol.45 (3), p.590-597

2002

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

Organic & biomolecular chemistry, 2003-10, Vol.1 (19), p.3377-3389

2003

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Conformationally Restricted Analogues of Psorospermin: Design, Synthesis, and Bioactivity of Natural-Product-Related Bisfuranoxanthones

Journal of medicinal chemistry, 2005-04, Vol.48 (8), p.2993-3004

2005

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

Quantitative, titratable and high-throughput reporter assays to measure DNA double strand break repair activity in cells

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

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

Common Marginal Cold Pools

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

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

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)

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

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

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

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

Drug Recognition and Stabilisation of the Parallel-stranded DNA Quadruplex d(TTAGGGT) 4 Containing the Human Telomeric Repeat

Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions

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

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

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

The effects of forest management on plant species diversity in a Sierran conifer forest

Potent Inhibition of Telomerase by Small-Molecule Pentacyclic Acridines Capable of Interacting with G-Quadruplexes

Edge effects in mixed conifer group selection openings: tree height response to resource gradients

Group selection management in conifer forests: relationships between opening size and tree growth

Antitumor Polycyclic Acridines. 17. Synthesis and Pharmaceutical Profiles of Pentacyclic Acridinium Salts Designed To Destabilize Telomeric Integrity

Antitumor Polycyclic Acridines. 8. Synthesis and Telomerase-Inhibitory Activity of Methylated Pentacyclic Acridinium Salts

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

Conformationally Restricted Analogues of Psorospermin: Design, Synthesis, and Bioactivity of Natural-Product-Related Bisfuranoxanthones

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