D. P. Lane

Design-Rules for Stapled Alpha-Helical Peptides with On-Target In Vivo Activity: Application toMdm2/X dual antagonists

The paper develops design rules for stapled alpha-helical peptides to improve in vivo activity and reduce off-target effects, demonstrating significant improvements in potency and safety.

MDM2 inhibitors, nutlin-3a and navtemadelin, retain efficacy in human and mouse cancer cells cultured in hypoxia

This study shows that MDM2 inhibitors nutlin-3a and navtemadelin remain effective in hypoxic conditions in human and mouse cancer cells with wild-type p53, but not in mutant or null p53 cells.

A grappling hook interaction balances self-assembly and chaperone activity of Nucleophosmin 1

The paper investigates how NPM1 self-assembly and chaperone activity interact, finding that oligomerization modulates its ability to prevent amyloid formation.

Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling

This paper identifies macrocyclic peptides that inhibit KRAS signaling by binding to its hydrophobic pocket, showing on-target activity and improved proteolytic stability.

CRISPR enriches for cells with mutations in a p53-related interactome, and this can be inhibited.

The paper shows that CRISPR enriches cells with p53-related mutations and demonstrates that transient p53 inhibition can suppress this effect.

A spindle and thread-mechanism unblocks translation of N-terminally disordered proteins

This study shows that fusing disordered proteins to an engineered spider silk domain improves their translation efficiency and activity in cells.

Conformational ordering of intrinsically disordered peptides for targeting translation initiation

The paper develops bioactive peptides that modulate eIF4E binding by inducing conformational order in intrinsically disordered regions of eIF4G.

bioPROTACs as versatile modulators of intracellular therapeutic targets: Application to proliferating cell nuclear antigen (PCNA)

This paper introduces bioPROTACs as intracellular biologics for targeted protein degradation, demonstrating their effectiveness against PCNA with rapid degradation and functional effects.

The Quantification of Antibody Elements and Receptors subunit expression using qPCR: The Design of VH, VL, CH, CL, FcR subunits primers for a more holistic view of the immune system.

The paper designs qPCR primers to quantify antibody elements and their receptors in PBMC cDNA, enabling a holistic view of immune system gene expression.

De-risking drug discovery of intracellular targeting peptides: screening strategies to eliminate false-positive hits

This paper identifies false-positive peptide inhibitors of KRas using orthogonal assays and cellular screens, highlighting the need for rigorous validation in drug discovery.