A receptor for the immuno-suppressant FK506 is a cis–trans peptidyl-prolyl isomerase

Matthew W. Harding, David Uehling, Stuart L. Schreiber

Nature

Molecular ImmunologySignal TransductionProtein ExpressionBiochemistryCis–trans Peptidyl-prolyl Isomerase +5

Total synthesis of FK506 and an FKBP probe reagent, [C(8),C(9)-13C2]-FK506

Masashi Nakatsuka, John A. Ragan, Tarek Sammakia, +3

Journal of the American Chemical Society

Molecular SciencesChemical MeasurementChemical AnalysisBiochemistryDonut Icon +11

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

Tara Rheault, John Stellwagen, George M. Adjabeng, +15

ACS Medicinal Chemistry Letters

B-raf-driven TumorsAntitumor ActivityHyperactive SignalingTumor BiologyMedicinal Chemistry +14

Dabrafenib; Preclinical Characterization, Increased Efficacy when Combined with Trametinib, while BRAF/MEK Tool Combination Reduced Skin Lesions

Alastair J. King, Marc R. Arnone, Maureen R. Bleam, +12

PLoS ONE

DermatologyTumor BiologySignaling PathwayReceptor Tyrosine KinasePreclinical Characterization +15

Disulfiram when Combined with Copper Enhances the Therapeutic Effects of Temozolomide for the Treatment of Glioblastoma

Xueqing Lun, J. Connor Wells, Natalie Grinshtein, +14

Clinical Cancer Research

Synthesis and Antitumor Activity of Novel Water Soluble Derivatives of Camptothecin as Specific Inhibitors of Topoisomerase I

Michael J. Luzzio, Jeffrey M. Besterman, David L. Emerson, +14

Journal of Medicinal Chemistry

Specific InhibitorsMedicinal ChemistryComplex Enzyme AssayAntitumor ActivityPharmaceutical Chemistry +12

Structure and mechanism of action of the hydroxy–aryl–aldehyde class of IRE1 endoribonuclease inhibitors

Mário Sanches, Nicole M. Duffy, Manisha Talukdar, +20

Nature Communications

Molecular PharmacologyAldehyde DehydrogenaseBiochemistryMedicineNatural Sciences +7

Functional characterization of a PROTAC directed against BRAF mutant V600E

Ganna Posternak, Xiaojing Tang, Pierre Maisonneuve, +27

Nature Chemical Biology

Natural SciencesProtein BiosynthesisBraf Mutant V600eMolecular BiologyProteomics +2

6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases

Edgar R. Wood, Lisa M. Shewchuk, Byron Ellis, +22

Proceedings of the National Academy of Sciences

Combinatorial ChemistryMedicinal ChemistryBiochemistryCovalent BondMedicine +11

Combined deletion of <scp>P</scp> ten and p53 in mammary epithelium accelerates triple‐negative breast cancer with dependency on e <scp>EF</scp> 2 <scp>K</scp>

Jeff C. Liu, Véronique Voisin, Sharon Wang, +10

EMBO Molecular Medicine