Targeted protein degradation is one of the fastest developing fields in medicinal chemistry and chemical biology. Despite significant development in assay technologies and inhibitor discovery, the dev...

Ke et al. review emerging proximity-inducing modalities—phosphorylation-targeting chimera, including PhosTACs, DEPTACs, PhoRCs, and PHICS—that modulate protein phosphorylation via an “event-driven” me...

Proteins lacking defined ligandable pockets remain challenging drug targets. Here, we develop a molecular glue-based PROTAC (MGPROTACs) approach that chemically conjugates a molecular glue stabilizer ...

An analysis of dose, dose frequency, human pharmacokinetics, and potential drug–drug interactions (DDI) was performed on small-molecule oral drugs approved by the FDA from 2020 to 2024 (n = 104). Alth...

Ligand efficiency (LE), defined as the negative binding free energy per heavy atom, is a widely used metric in medicinal chemistry. Yet its mathematical construction embeds a strong size bias that distorts cross-size comparisons, and size-independent variants inherit sensitivity to the arbitrary choice of standard state. This study reviews normalization pitfalls, addresses uncertainty propagation, and introduces a state-invariant, size-normalized metric for efficiency-guided optimization from fragments to leads.

The prolific company creator is staking $50 million on AI drug discovery for cancer and immune diseases, launching a biotech that already has a partnership with Pfizer.

At the end of the day, biotech venture capital is a business and driving returns is the ultimate metric. For twenty years, to deliver on that, I’ve embraced what I call the “first principle” of early ...

Talented people make the magic happen in biotech.  This is the second post in my “Twenty Years In Early Stage Venture” trifecta. Yesterday’s was on Science. Today we’re talking about the People part o...

In the blink of an eye, twenty years have passed: in mid-October 2005, I joined Atlas Venture as a principal on the global life science team.  We closed Fund VII a few months after I joined; and, just...

Cell state plasticity of neuroblastoma cells is linked to therapy resistance. Here, the authors develop a transcriptomic and epigenetic map of indisulam (RBM39 degrader) resistant neuroblastoma, demon...

I spent years spouting conspiracy theories about vaccines. Now, as measles rages in my home of Alberta, I’m trying to convince vax-hesitant parents to inoculate their kids.

The effects of fluorine and chlorine on pharmaceutical systems are compared using a Molecular Matched Pair Analysis. Effects on binding constants, physicochemical properties such as lipophilicity and...

Proteolysis-targeting chimeras (PROTACs) are promising next-generation therapeutics for the degradation of disease-associated proteins. However, optimizing the physicochemical properties of PROTACs, p...

Chemical Inducers of Proximity DNA-Encoded Library (CIP-DEL) screening enables high-throughput discovery of compounds that induce protein–protein interactions, including Proteolysis-Targeting Chimeras...

HHS Secretary RFK Jr. sat down with Scripps News for a wide-ranging interview, discussing mRNA vaccine funding policy changes and a recent shooting at the Centers for Disease Control and Prevention.

Chemical inducers of proximity (CIPs) can elicit durable, and often neomorphic, biological effects through the formation of a ternary complex, even at low equilibrium occupancy of their targets. This ...

GPR75 is one of the most promising emerging targets for the treatment of obesity and related co-morbidities, as its loss of function directly correlates with a decreased body mass index (BMI) in human...

The well documented difficulties associated with direct (hetero)arylation of aza-aromatics (e.g., azines) at the α-position to nitrogen led to a collaborative project between the Willis group at Oxfor...

Molecular glues powerfully control protein proximity but have largely eluded direct screening. A promising avenue for addressing this challenge lies within pinpointing the fundamental features for fun...

Moreno Ballesteros et al. introduce a site-resolved strategy combining genetic code expansion and bioorthogonal chemistry to evaluate how ligand binding sites influence targeted protein degradation. This approach offers a powerful framework to accelerate degrader design, enable target validation, and broadly explore the potential of induced proximity.