Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

Loren Lasko, Clarissa G. Jakob, Rohinton Edalji, +36

Nature

Lineage-specific TumoursMedicineImmune Checkpoint InhibitorAnti-cancer AgentTumor Suppressor +6

The Three-dimensional Structures of Antagonistic and Agonistic Forms of the Glucocorticoid Receptor Ligand-binding Domain

Björn Kauppi, Clarissa G. Jakob, Mathias Färnegårdh, +14

Journal of Biological Chemistry

The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

Yupeng He, Sujatha Selvaraju, Michael L. Curtin, +34

Nature Chemical Biology

Protein FunctionSignal TransductionMolecular RegulationPrc2 ComplexMolecular Biology +5

The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity

Kenneth D. Bromberg, Taylor R. H. Mitchell, Anup K. Upadhyay, +28

Nature Chemical Biology

ChromatinChromatin RemodelingEpigenetic ChangeGeneticsGenomic Integrity +8

Crystal Structure and Mutagenic Analysis of the Inhibitor-of-Apoptosis Protein Survivin

Steven W. Muchmore, Jun Chen, Clarissa G. Jakob, +7

Molecular Cell

Crystal StructureBiochemistryNatural SciencesApoptosisMolecular Biology +5

X-ray crystallographic structure of ABT-378 (Lopinavir) bound to HIV-1 protease

Vincent S. Stoll, Wenying Qin, Kent D. Stewart, +9

Bioorganic & Medicinal Chemistry

Virus StructureViral ReplicationHiv-1 ProteaseBiochemistryNatural Sciences +7

Liver-Selective Glucocorticoid Antagonists:  A Novel Treatment for Type 2 Diabetes

Thomas W von Geldern, Noah P. Tu, Philip R. Kym, +23

Journal of Medicinal Chemistry

ImmunologyGlucocorticoidMetabolic SyndromeBile Acid ConjugationBile Acid +14

Discovery of Potent Inhibitors of Dihydroneopterin Aldolase Using CrystaLEAD High-Throughput X-ray Crystallographic Screening and Structure-Directed Lead Optimization

William J. Sanders, V. Nienaber, Claude G. Lerner, +15

Journal of Medicinal Chemistry

Structure reveals function of the dual variable domain immunoglobulin (DVD-Ig™) molecule

Clarissa G. Jakob, Rohinton Edalji, Russell A. Judge, +4

mAbs

Inner Variable DomainImmunologyImmune RegulationMolecular BiologyImmunodominance +22

Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2

Ramzi F. Sweis, Zhi Wang, Mikkel A. Algire, +11

ACS Medicinal Chemistry Letters

Molecular BiologyP53k370 MethylationChemical BiologyCancer BiologyTumor Biology +15