Kenton L. Longenecker
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View article: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties Open
Glucocorticoid receptor modulators (GRMs) are an established and successful compound class for the treatment of multiple diseases. In addition, they are an area of high interest as payloads for antibody-drug conjugate s(ADCs) in both immun…
View article: Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex
Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex Open
View article: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties Open
Minimising solvent exposed hydrophobic surface area of payload is identified as a critical design parameter for optimising ADC drug-like properties.
View article: Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties
Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties Open
Correction for ‘Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties’ by Adrian D. Hobson et al. , RSC Med. Chem. , 2024, https://doi.org/10.1039/d3md00540b.
View article: 1403-A PTPN2/N1 inhibitor ABBV-CLS-484 unleashes potent anti-tumor immunity
1403-A PTPN2/N1 inhibitor ABBV-CLS-484 unleashes potent anti-tumor immunity Open
Background Immune checkpoint blockade is effective for a subset of patients across many cancers, but most patients are refractory to current immunotherapies and new approaches are needed to overcome resistance.1 2 The protein ty…
View article: The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity
The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity Open
View article: Supplementary Table S4 from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors
Supplementary Table S4 from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors Open
Structures and PC3 viability IC50 data for compounds in Figure 2.
View article: Supplementary Table S4 from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors
Supplementary Table S4 from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors Open
Structures and PC3 viability IC50 data for compounds in Figure 2.
View article: Wilsbacher et. al. supplement from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors
Wilsbacher et. al. supplement from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors Open
Supplementary methods, tables S1-S3, and supplementary figures 1-7
View article: Wilsbacher et. al. supplement from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors
Wilsbacher et. al. supplement from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors Open
Supplementary methods, tables S1-S3, and supplementary figures 1-7
View article: Data from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors
Data from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors Open
Cancer cells are highly reliant on NAD+-dependent processes, including glucose metabolism, calcium signaling, DNA repair, and regulation of gene expression. Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzym…
View article: Data from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors
Data from Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors Open
Cancer cells are highly reliant on NAD+-dependent processes, including glucose metabolism, calcium signaling, DNA repair, and regulation of gene expression. Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzym…
View article: An anti-PD-1–GITR-L bispecific agonist induces GITR clustering-mediated T cell activation for cancer immunotherapy
An anti-PD-1–GITR-L bispecific agonist induces GITR clustering-mediated T cell activation for cancer immunotherapy Open
Costimulatory receptors such as glucocorticoid-induced tumor necrosis factor receptor–related protein (GITR) play key roles in regulating the effector functions of T cells. In human clinical trials, however, GITR agonist antibodies have sh…
View article: Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors
Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors Open
Cyclin-dependent kinase 9 (CDK9) is a serine/threonine kinase involved in the regulation of transcription elongation. An inhibition of CDK9 downregulates a number of short-lived proteins responsible for tumor maintenance and survival, incl…
View article: Complex of human Melanotransferrin and SC57.32 Fab fragment reveals novel interdomain arrangement with ferric N-lobe and open C-lobe
Complex of human Melanotransferrin and SC57.32 Fab fragment reveals novel interdomain arrangement with ferric N-lobe and open C-lobe Open
View article: Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design
Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design Open
Tumor necrosis factor α (TNFα) is a soluble cytokine that is directly involved in systemic inflammation through the regulation of the intracellular NF-κB and MAPK signaling pathways. The development of biologic drugs that inhibit TNFα has …
View article: Discovery of <i>N</i>-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1<i>H</i>-pyrrolo[2,3-<i>c</i>]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Discovery of <i>N</i>-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1<i>H</i>-pyrrolo[2,3-<i>c</i>]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain Open
The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under clinical development for oncology bind to each of the eight bromodoma…
View article: Structure of human DPEP3 in complex with the SC-003 antibody Fab fragment reveals basis for lack of dipeptidase activity
Structure of human DPEP3 in complex with the SC-003 antibody Fab fragment reveals basis for lack of dipeptidase activity Open
View article: SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT)
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT) Open
View article: Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors
Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors Open
Cancer cells are highly reliant on NAD+-dependent processes, including glucose metabolism, calcium signaling, DNA repair, and regulation of gene expression. Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme for NAD+ …
View article: Crystal structure of full-length <i>Zika virus</i> NS5 protein reveals a conformation similar to <i>Japanese encephalitis virus</i> NS5
Crystal structure of full-length <i>Zika virus</i> NS5 protein reveals a conformation similar to <i>Japanese encephalitis virus</i> NS5 Open
The rapid spread of the recent Zika virus (ZIKV) epidemic across various countries in the American continent poses a major health hazard for the unborn fetuses of pregnant women. To date, there is no effective medical intervention. The non…
View article: Cysteinylation of a monoclonal antibody leads to its inactivation
Cysteinylation of a monoclonal antibody leads to its inactivation Open
Post-translational modifications can have a signification effect on antibody stability. A comprehensive approach is often required to best understand the underlying reasons the modification affects the antibody's potency or aggregation sta…