Chemical probes and drug leads from advances in synthetic planning and methodology

Design and Evolution of a Macrocyclic Peptide Inhibitor of the Sonic Hedgehog/Patched Interaction

(2017) Andrew E. Owens et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Synthesis of a Bicyclic Azetidine with In Vivo Antimalarial Activity Enabled by Stereospecific, Directed C(sp3)–H Arylation

(2017) Micah Maetani et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A small-molecule allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase

(2017) Samantha Wellington et al.   Nature Chemical Biology

Probes & Drugs portal: an interactive, open data resource for chemical biology

(2017) Ctibor Skuta et al.   NATURE METHODS

Drug development in the era of precision medicine

(2017) Sarah A. Dugger et al.   NATURE REVIEWS DRUG DISCOVERY

Opportunities and challenges in phenotypic drug discovery: an industry perspective

(2017) John G. Moffat et al.   NATURE REVIEWS DRUG DISCOVERY

Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit P. falciparum Dihydroorotate Dehydrogenase

(2017) Micah Maetani et al.   ACS Medicinal Chemistry Letters

Identification of Highly Specific Diversity-Oriented Synthesis-Derived Inhibitors of Clostridium difficile

(2017) Jeremy R. Duvall et al.   ACS Infectious Diseases

Medicinal Chemistry Projects Requiring Imaginative Structure-Based Drug Design Methods

(2016) Nicolas Moitessier et al.   ACCOUNTS OF CHEMICAL RESEARCH

Chemical Biology Probes from Advanced DNA-encoded Libraries

(2016) Hazem Salamon et al.   ACS Chemical Biology

A Multidimensional Diversity-Oriented Synthesis Strategy for Structurally Diverse and Complex Macrocycles

(2016) Feilin Nie et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Drugging Undruggable Molecular Cancer Targets

(2016) John S. Lazo et al.   Annual Review of Pharmacology and Toxicology

Novel diversity-oriented synthesis-derived respiratory syncytial virus inhibitors identified via a high throughput replicon-based screen

(2016) Jeremy R. Duvall et al.   ANTIVIRAL RESEARCH

High-Throughput Assay and Discovery of Small Molecules that Interrupt Malaria Transmission

(2016) David M. Plouffe et al.   Cell Host & Microbe

Photochemical Approaches to Complex Chemotypes: Applications in Natural Product Synthesis

(2016) Markus D. Kärkäs et al.   CHEMICAL REVIEWS

Chemical Space of DNA-Encoded Libraries

(2016) Raphael M. Franzini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Natural Products as Sources of New Drugs from 1981 to 2014

(2016) David J. Newman et al.   JOURNAL OF NATURAL PRODUCTS

Real-Time Biological Annotation of Synthetic Compounds

(2016) Christopher J. Gerry et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Tuberculosis

(2016) Keertan Dheda et al.   LANCET

Strategies for target identification of antimicrobial natural products

(2016) Maya A. Farha et al.   NATURAL PRODUCT REPORTS

Diversity-oriented synthesis yields novel multistage antimalarial inhibitors

(2016) Nobutaka Kato et al.   NATURE

Schizophrenia risk from complex variation of complement component 4

(2016) Aswin Sekar et al.   NATURE

A platform for the discovery of new macrolide antibiotics

(2016) Ian B. Seiple et al.   NATURE

Analysis of protein-coding genetic variation in 60,706 humans

(2016) Monkol Lek et al.   NATURE

High-throughput identification of genotype-specific cancer vulnerabilities in mixtures of barcoded tumor cell lines

(2016) Channing Yu et al.   NATURE BIOTECHNOLOGY

Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition

(2016) Anja F Hohmann et al.   Nature Chemical Biology

Discovery of MRSA active antibiotics using primary sequence from the human microbiome

(2016) John Chu et al.   Nature Chemical Biology

Twenty years on: the impact of fragments on drug discovery

(2016) Daniel A. Erlanson et al.   NATURE REVIEWS DRUG DISCOVERY

Divergent Synthesis and Real-Time Biological Annotation of Optically Active Tetrahydrocyclopenta[c]pyranone Derivatives

(2016) Shawn D. Nelson et al.   ORGANIC LETTERS

Disciplined approach to drug discovery and early development

(2016) Robert M. Plenge   Science Translational Medicine

Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1

(2016) Jason M. Law et al.   ACS Medicinal Chemistry Letters

Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β

(2016) Yikai Wang et al.   ACS Medicinal Chemistry Letters

Diversity-oriented synthetic strategy for developing a chemical modulator of protein–protein interaction

(2016) Jonghoon Kim et al.   Nature Communications

Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments

(2016) Sina Haftchenary et al.   ACS Combinatorial Science

Clostridium difficile infection

(2016) Wiep Klaas Smits et al.   Nature Reviews Disease Primers

The Chemical Space Project

(2015) Jean-Louis Reymond   ACCOUNTS OF CHEMICAL RESEARCH

The application of in silico drug-likeness predictions in pharmaceutical research

(2015) Sheng Tian et al.   ADVANCED DRUG DELIVERY REVIEWS

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

(2015) Peter G. K. Clark et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Regio- and Enantioselective Aza-Diels-Alder Reactions of 3-Vinylindoles: A Concise Synthesis of the Antimalarial Spiroindolone NITD609

(2015) Haifeng Zheng et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Benzo-fused lactams from a diversity-oriented synthesis (DOS) library as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake

(2015) Chris Dockendorff et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

(2015) Stuart L. Schreiber et al.   CELL

Target-Based Identification of Whole-Cell Active Inhibitors of Biotin Biosynthesis in Mycobacterium tuberculosis

(2015) Sae Woong Park et al.   CHEMISTRY & BIOLOGY

Molecular Pathways: Novel Approaches for Improved Therapeutic Targeting of Hedgehog Signaling in Cancer Stem Cells

(2015) Verline Justilien et al.   CLINICAL CANCER RESEARCH

Kinase-Independent Small-Molecule Inhibition of JAK-STAT Signaling

(2015) Danny Hung-Chieh Chou et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery of a Small-Molecule Probe for V-ATPase Function

(2015) Leslie N. Aldrich et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Safety and activity of alisertib, an investigational aurora kinase A inhibitor, in patients with breast cancer, small-cell lung cancer, non-small-cell lung cancer, head and neck squamous-cell carcinoma, and gastro-oesophageal adenocarcinoma: a five-arm phase 2 study

(2015) Bohuslav Melichar et al.   LANCET ONCOLOGY

Molecular Docking and Structure-Based Drug Design Strategies

(2015) Leonardo Ferreira et al.   MOLECULES

Biological targets and mechanisms of action of natural products from marine cyanobacteria

(2015) Lilibeth A. Salvador-Reyes et al.   NATURAL PRODUCT REPORTS

A novel multiple-stage antimalarial agent that inhibits protein synthesis

(2015) Beatriz Baragaña et al.   NATURE

Improving drug discovery with high-content phenotypic screens by systematic selection of reporter cell lines

(2015) Jungseog Kang et al.   NATURE BIOTECHNOLOGY

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

Hit and lead criteria in drug discovery for infectious diseases of the developing world

(2015) Kei Katsuno et al.   NATURE REVIEWS DRUG DISCOVERY

Tackling reproducibility in academic preclinical drug discovery

(2015) Stephen V. Frye et al.   NATURE REVIEWS DRUG DISCOVERY

Small-molecule enhancers of autophagy modulate cellular disease phenotypes suggested by human genetics

(2015) Szu-Yu Kuo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Personalized genomic analyses for cancer mutation discovery and interpretation

(2015) Siân Jones et al.   Science Translational Medicine

Protection and pathology in TB: learning from the zebrafish model

(2015) Annemarie H. Meijer   Seminars in Immunopathology

Killing the hypnozoite – drug discovery approaches to prevent relapse inPlasmodium vivax

(2015) Brice Campo et al.   Pathogens and Global Health

Development and Validation of a Novel Leishmania donovani Screening Cascade for High-Throughput Screening Using a Novel Axenic Assay with High Predictivity of Leishmanicidal Intracellular Activity

(2015) Andrea Nühs et al.   PLoS Neglected Tropical Diseases

From the Biology of PP2A to the PADs for Therapy of Hematologic Malignancies

(2015) Maria Ciccone et al.   Frontiers in Oncology

Aurora Kinase Inhibitors: Current Status and Outlook

(2015) Vassilios Bavetsias et al.   Frontiers in Oncology

Modulators of Hepatic Lipoprotein Metabolism Identified in a Search for Small-Molecule Inducers of Tribbles Pseudokinase 1 Expression

(2015) Marek M. Nagiec et al.   PLoS One

Mutations in the P-Type Cation-Transporter ATPase 4, PfATP4, Mediate Resistance to Both Aminopyrazole and Spiroindolone Antimalarials

(2014) Erika L. Flannery et al.   ACS Chemical Biology

The Evolving Role of Chemical Synthesis in Antibacterial Drug Discovery

(2014) Peter M. Wright et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

PME-1 Modulates Protein Phosphatase 2A Activity to Promote the Malignant Phenotype of Endometrial Cancer Cells

(2014) E. Wandzioch et al.   CANCER RESEARCH

Structure-Based Virtual Screening for Drug Discovery: Principles, Applications and Recent Advances

(2014) Evanthia Lionta et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Diversity-Oriented Synthesis Probe TargetsPlasmodium falciparumCytochrome b Ubiquinone Reduction Site and Synergizes With Oxidation Site Inhibitors

(2014) Amanda K. Lukens et al.   JOURNAL OF INFECTIOUS DISEASES

Diversity-Oriented Synthesis-Facilitated Medicinal Chemistry: Toward the Development of Novel Antimalarial Agents

(2014) Eamon Comer et al.   JOURNAL OF MEDICINAL CHEMISTRY

One-Step Synthesis of Saturated Spirocyclic N-Heterocycles with Stannyl Amine Protocol (SnAP) Reagents and Ketones

(2014) Woon-Yew Siau et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

PI3K and cancer: lessons, challenges and opportunities

(2014) David A. Fruman et al.   NATURE REVIEWS DRUG DISCOVERY

Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY

Phenotypic screening in cancer drug discovery — past, present and future

(2014) John G. Moffat et al.   NATURE REVIEWS DRUG DISCOVERY

Molecular mechanisms of antibiotic resistance

(2014) Jessica M. A. Blair et al.   NATURE REVIEWS MICROBIOLOGY

Spiroindolone KAE609 for Falciparum and Vivax Malaria

(2014) Nicholas J. White et al.   NEW ENGLAND JOURNAL OF MEDICINE

(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance ofPlasmodium

(2014) María Belén Jiménez-Díaz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Toward performance-diverse small-molecule libraries for cell-based phenotypic screening using multiplexed high-dimensional profiling

(2014) M. J. Wawer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain

(2014) Apirat Chaikuad et al.   MedChemComm

Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1)

(2014) Chao Fang et al.   ACS Medicinal Chemistry Letters

Diversity-oriented synthesis as a tool for identifying new modulators of mitosis

(2014) Brett M. Ibbeson et al.   Nature Communications

Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum

(2014) Akhil B. Vaidya et al.   Nature Communications

Discovery of Neuritogenic Compound Classes Inspired by Natural Products

(2013) Pierre-Yves Dakas et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Natural products: A continuing source of novel drug leads

(2013) Gordon M. Cragg et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Cancerous Inhibitor of Protein Phosphatase 2A, an Emerging Human Oncoprotein and a Potential Cancer Therapy Target

(2013) A. Khanna et al.   CANCER RESEARCH

Allostery in Disease and in Drug Discovery

(2013) Ruth Nussinov et al.   CELL

Na+ Regulation in the Malaria Parasite Plasmodium falciparum Involves the Cation ATPase PfATP4 and Is a Target of the Spiroindolone Antimalarials

(2013) Natalie J. Spillman et al.   Cell Host & Microbe

The machinery of macroautophagy

(2013) Yuchen Feng et al.   CELL RESEARCH

Selective HDAC1/HDAC2 Inhibitors Induce Neuroblastoma Differentiation

(2013) Stacey M. Frumm et al.   CHEMISTRY & BIOLOGY

Phenotypic vs. Target-Based Drug Discovery for First-in-Class Medicines

(2013) D C Swinney   CLINICAL PHARMACOLOGY & THERAPEUTICS

mTOR in aging, metabolism, and cancer

(2013) Marion Cornu et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Biodiversity of small molecules – a new perspective in screening set selection

(2013) Paula M. Petrone et al.   DRUG DISCOVERY TODAY

Phenotypic screens as a renewed approach for drug discovery

(2013) Wei Zheng et al.   DRUG DISCOVERY TODAY

Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction in β-Cells with Improved Aqueous Solubility

(2013) Stephen S. Scully et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery for Neglected Diseases: Molecular Target-Based and Phenotypic Approaches

(2013) Ian H. Gilbert   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Small-Molecule Modulators of the Sonic Hedgehog Pathway

(2013) Giannina I. Schaefer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Identification of risk loci with shared effects on five major psychiatric disorders: a genome-wide analysis

(2013)   LANCET

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

Understanding the hepatitis C virus life cycle paves the way for highly effective therapies

(2013) Troels K H Scheel et al.   NATURE MEDICINE

Platforms for antibiotic discovery

(2013) Kim Lewis   NATURE REVIEWS DRUG DISCOVERY

Validating therapeutic targets through human genetics

(2013) Robert M. Plenge et al.   NATURE REVIEWS DRUG DISCOVERY

Antimalarial drug discovery — approaches and progress towards new medicines

(2013) Erika L. Flannery et al.   NATURE REVIEWS MICROBIOLOGY

The Future of Antibiotics and Resistance

(2013) Brad Spellberg et al.   NEW ENGLAND JOURNAL OF MEDICINE

A review of oral toxicity associated with mTOR inhibitor therapy in cancer patients

(2013) Fabiana Martins et al.   ORAL ONCOLOGY

Small-molecule fluorophores and fluorescent probes for bioimaging

(2013) Takuya Terai et al.   PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY

Multiplex Cytological Profiling Assay to Measure Diverse Cellular States

(2013) Sigrun M. Gustafsdottir et al.   PLoS One

Tight Coordination of Protein Translation and HSF1 Activation Supports the Anabolic Malignant State

(2013) S. Santagata et al.   SCIENCE

Diversity-Oriented Synthesis Yields a New Drug Lead for Treatment of Chagas Disease

(2013) Sivaraman Dandapani et al.   ACS Medicinal Chemistry Letters

Identification of Novel Inhibitors of M. tuberculosis Growth Using Whole Cell Based High-Throughput Screening

(2012) Sarah A. Stanley et al.   ACS Chemical Biology

The Spiroindolone Drug Candidate NITD609 Potently Inhibits Gametocytogenesis and Blocks Plasmodium falciparum Transmission to Anopheles Mosquito Vector

(2012) J. C. van Pelt-Koops et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Allosteric regulation of substrate channeling and catalysis in the tryptophan synthase bienzyme complex

(2012) Michael F. Dunn   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Lessons from the Past and Charting the Future of Marine Natural Products Drug Discovery and Chemical Biology

(2012) William H. Gerwick et al.   CHEMISTRY & BIOLOGY

Big pharma screening collections: more of the same or unique libraries? The AstraZeneca–Bayer Pharma AG case

(2012) Thierry Kogej et al.   DRUG DISCOVERY TODAY

Protein tyrosine phosphatases - from housekeeping enzymes to master regulators of signal transduction

(2012) Nicholas K. Tonks   FEBS Journal

Osteopetrosis Mutation R444L Causes Endoplasmic Reticulum Retention and Misprocessing of Vacuolar H+-ATPasea3Subunit

(2012) Ajay Bhargava et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential

(2012) Yassir Younis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries

(2012) Jason T. Lowe et al.   JOURNAL OF ORGANIC CHEMISTRY

Competitive Activity-Based Protein Profiling Identifies Aza-β-Lactams as a Versatile Chemotype for Serine Hydrolase Inhibition

(2012) Andrea M. Zuhl et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion

(2012) Renato A Bauer et al.   Nature Chemical Biology

A diversity-oriented synthesis approach to macrocycles via oxidative ring expansion

(2012) Felix Kopp et al.   Nature Chemical Biology

Chris Lipinski

(2012)   NATURE REVIEWS DRUG DISCOVERY

Autophagy modulation as a potential therapeutic target for diverse diseases

(2012) David C. Rubinsztein et al.   NATURE REVIEWS DRUG DISCOVERY

Genetic causes and mechanisms of distal renal tubular acidosis

(2012) D. Batlle et al.   NEPHROLOGY DIALYSIS TRANSPLANTATION

Application of a Catalytic Asymmetric Povarov Reaction using Chiral Ureas to the Synthesis of a Tetrahydroquinoline Library

(2012) Baudouin Gerard et al.   ACS Combinatorial Science

Build/Couple/Pair Strategy for the Synthesis of Stereochemically Diverse Macrolactams via Head-to-Tail Cyclization

(2012) Mark E. Fitzgerald et al.   ACS Combinatorial Science

Biology-Oriented Synthesis

(2011) Stefan Wetzel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of histone deacetylase 8 selective inhibitors

(2011) Weiping Tang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

The advent and evolution of QSAR at Pomona College

(2011) Corwin Hansch   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Synthesis of Rocaglamide Hydroxamates and Related Compounds as Eukaryotic Translation Inhibitors: Synthetic and Biological Studies

(2011) Christina M. Rodrigo et al.   JOURNAL OF MEDICINAL CHEMISTRY

AMPK and mTOR regulate autophagy through direct phosphorylation of Ulk1

(2011) Joungmok Kim et al.   NATURE CELL BIOLOGY

Large-scale genome-wide association analysis of bipolar disorder identifies a new susceptibility locus near ODZ4

(2011)   NATURE GENETICS

Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators

(2011) D. M. Huryn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors

(2011) D. A. Bachovchin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Quantifying structure and performance diversity for sets of small molecules comprising small-molecule screening collections

(2011) P. A. Clemons et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Organic synthesis toward small-molecule probes and drugs

(2011) S. L. Schreiber   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Solid-phase synthesis and chemical space analysis of a 190-membered alkaloid/terpenoid-like library

(2011) G. Moura-Letts et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

High levels of nuclear heat-shock factor 1 (HSF1) are associated with poor prognosis in breast cancer

(2011) S. Santagata et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Diversity through phosphine catalysis identifies octahydro-1,6-naphthyridin-4-ones as activators of endothelium-driven immunity

(2011) D. Cruz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Enantioselective Pictet–Spengler reactions of isatins for the synthesis of spiroindolones

(2011) Joseph J. Badillo et al.   TETRAHEDRON LETTERS

Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria

(2011) Richard W. Heidebrecht et al.   ACS Medicinal Chemistry Letters

Synthesis of a Novel Suppressor of β-Cell Apoptosis via Diversity-Oriented Synthesis

(2011) Danny Hung-Chieh Chou et al.   ACS Medicinal Chemistry Letters

Biomimetic Photocycloaddition of 3-Hydroxyflavones: Synthesis and Evaluation of Rocaglate Derivatives as Inhibitors of Eukaryotic Translation

(2010) Stéphane P. Roche et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Probing the Probes: Fitness Factors For Small Molecule Tools

(2010) Paul Workman et al.   CHEMISTRY & BIOLOGY

Current strategies for diversity-oriented synthesis

(2010) Sivaraman Dandapani et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

A complex task? Direct modulation of transcription factors with small molecules

(2010) Angela N Koehler   CURRENT OPINION IN CHEMICAL BIOLOGY

Clinical Practice Guidelines for Clostridium difficile Infection in Adults: 2010 Update by the Society for Healthcare Epidemiology of America (SHEA) and the Infectious Diseases Society of America (IDSA)

(2010) Stuart H. Cohen et al.   INFECTION CONTROL AND HOSPITAL EPIDEMIOLOGY

An Aldol-Based Build/Couple/Pair Strategy for the Synthesis of Medium- and Large-Sized Rings: Discovery of Macrocyclic Histone Deacetylase Inhibitors

(2010) Lisa A. Marcaurelle et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Distinct Biological Network Properties between the Targets of Natural Products and Disease Genes

(2010) Vlado Dančík et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Origins and Evolution of Antibiotic Resistance

(2010) J. Davies et al.   MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS

Aurora Kinase Inhibitors - Rising Stars in Cancer Therapeutics?

(2010) A. A. Dar et al.   MOLECULAR CANCER THERAPEUTICS

BRD7 is a candidate tumour suppressor gene required for p53 function

(2010) Jarno Drost et al.   NATURE CELL BIOLOGY

Grand Challenge Commentary: Accessing new chemical space for 'undruggable' targets

(2010) Sivaraman Dandapani et al.   Nature Chemical Biology

The art of the chemical probe

(2010) Stephen V Frye   Nature Chemical Biology

Highly enantioselective synthesis and cellular evaluation of spirooxindoles inspired by natural products

(2010) Andrey P. Antonchick et al.   Nature Chemistry

Resequencing of positional candidates identifies low frequency IL23R coding variants protecting against inflammatory bowel disease

(2010) Yukihide Momozawa et al.   NATURE GENETICS

Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis

(2010) L Meng et al.   ONCOGENE

Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles

(2010) P. A. Clemons et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

An Autophagy-Enhancing Drug Promotes Degradation of Mutant  1-Antitrypsin Z and Reduces Hepatic Fibrosis

(2010) T. Hidvegi et al.   SCIENCE

Spiroindolones, a Potent Compound Class for the Treatment of Malaria

(2010) M. Rottmann et al.   SCIENCE

The Bacterial Cell Envelope

(2010) T. J. Silhavy et al.   Cold Spring Harbor Perspectives in Biology

Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules

(2010) Warren R.J.D. Galloway et al.   Nature Communications

Fifteen years of HIV Protease Inhibitors: raising the barrier to resistance

(2009) Annemarie M.J. Wensing et al.   ANTIVIRAL RESEARCH

Syntheses of aminoalcohol-derived macrocycles leading to a small-molecule binder to and inhibitor of Sonic Hedgehog

(2009) Lee F. Peng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibiting the transcription factor HSF1 as an anticancer strategy

(2009) Luke Whitesell et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Small-molecule modulators of the Sonic Hedgehog signaling pathway

(2009) Benjamin Z. Stanton et al.   Molecular BioSystems

Molecular diversity by design

(2009) Stuart L. Schreiber   NATURE

A small molecule that binds Hedgehog and blocks its signaling in human cells

(2009) Benjamin Z Stanton et al.   Nature Chemical Biology

Artemisinin Resistance inPlasmodium falciparumMalaria

(2009) Arjen M. Dondorp et al.   NEW ENGLAND JOURNAL OF MEDICINE

The SWI/SNF complex and cancer

(2009) D Reisman et al.   ONCOGENE

Antibiotics for Emerging Pathogens

(2009) M. A. Fischbach et al.   SCIENCE

Synthesis of Natural-Product-Like Molecules with Over Eighty Distinct Scaffolds

(2008) Daniel Morton et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Enantioselective Nucleophilic Catalysis: The Synthesis of Aza-β-Lactams through [2+2] Cycloadditions of Ketenes with Azo Compounds

(2008) Jacob M. Berlin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Anti-MRSA Agent Discovery Using Diversity-Oriented Synthesis

(2008) Gemma L. Thomas et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

OPT-80 Eliminates Clostridium difficile and Is Sparing of Bacteroides Species during Treatment of C. difficile Infection

(2008) T. J. Louie et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Structural Mechanism of Demethylation and Inactivation of Protein Phosphatase 2A

(2008) Yongna Xing et al.   CELL

The impact of natural products upon modern drug discovery

(2008) A Ganesan   CURRENT OPINION IN CHEMICAL BIOLOGY

Diversity Synthesis of Complex Pyridines Yields a Probe of a Neurotrophic Signaling Pathway

(2008) B. Lawrence Gray et al.   ORGANIC LETTERS

Genetic Mapping in Human Disease

(2008) D. Altshuler et al.   SCIENCE

Glutamate racemase as a target for drug discovery

(2008) Stewart L. Fisher   Microbial Biotechnology

Towards the Optimal Screening Collection: A Synthesis Strategy

(2007) Thomas E. Nielsen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION