An inhibitor of oxidative phosphorylation exploits cancer vulnerability

Jennifer R. Molina, Yuting Sun, Marina Protopopova, +63

Nature Medicine

MedicineAnti-cancer AgentCancer VulnerabilityPharmacologyTumor Microenvironment +2

Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection

Vincenzo Summa, Alessia Petrocchi, Fabio Bonelli, +20

Journal of Medicinal Chemistry

Antiviral DrugMedicinal ChemistryAntiviral Drug DevelopmentResistance Mutation (Virology)Biochemistry +14

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies

Bhavatarini Vangamudi, Thomas A. Paul, Parantu K. Shah, +21

Cancer Research

Atpase DomainExclusive Catalytic SubunitsDrug TargetMolecular BiologyCancer Biology +15

Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor

Steven J. Harper, John A. McCauley, Michael T. Rudd, +32

ACS Medicinal Chemistry Letters

ImmunologyMolecular BiologyPharmacotherapyAntiviral DrugMedicinal Chemistry +17

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

Wylie S. Palmer, G. Poncet-Montange, Gang Liu, +19

Journal of Medicinal Chemistry

Combinatorial ChemistryEpigenetic ChangeX-ray Cocrystal StructuresMolecular BiologyChemical Biology +18

Discovery of α,γ-Diketo Acids as Potent Selective and Reversible Inhibitors of Hepatitis C Virus NS5b RNA-Dependent RNA Polymerase

Vincenzo Summa, Alessia Petrocchi, Paola Pace, +6

Journal of Medicinal Chemistry

Viral ReplicationViral Polymerase StructureMolecular BiologyAntiviral DrugMedicinal Chemistry +17

4,5-Dihydroxypyrimidine Carboxamides and <i>N</i>-Alkyl-5-hydroxypyrimidinone Carboxamides Are Potent, Selective HIV Integrase Inhibitors with Good Pharmacokinetic Profiles in Preclinical Species

Vincenzo Summa, Alessia Petrocchi, Victor G. Matassa, +7

Journal of Medicinal Chemistry

Bioorganic ChemistryPharmacotherapyAntiviral DrugMedicinal Chemistry4,5-Dihydroxypyrimidine Carboxamides +15

HCV NS5b RNA-Dependent RNA Polymerase Inhibitors:  From α,γ-Diketoacids to 4,5-Dihydroxypyrimidine- or 3-Methyl-5- hydroxypyrimidinonecarboxylic Acids. Design and Synthesis

Vincenzo Summa, Alessia Petrocchi, Victor G. Matassa, +5

Journal of Medicinal Chemistry

Viral Polymerase StructureMolecular BiologyAntiviral DrugChemical BiologyMedicinal Chemistry +14

Genetic Events That Limit the Efficacy of MEK and RTK Inhibitor Therapies in a Mouse Model of KRAS-Driven Pancreatic Cancer

Piergiorgio Pettazzoni, Andrea Viale, Parantu K. Shah, +26

Cancer Research

Dihydroxypyrimidine-4-carboxamides as Novel Potent and Selective HIV Integrase Inhibitors

Paola Pace, Maria Emilia Di Francesco, Cristina Gardelli, +15

Journal of Medicinal Chemistry

Combinatorial ChemistryMedicinal ChemistryBioorganic ChemistryInteresting CompoundsBiochemistry +13