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The Emperor’s New Probes

April 10, 2019

Ubiquitin (Ub) is ubiquitous.  This small, 76-residue protein is used to mark cellular proteins for degradation by the ubiquitin proteasome system (UPS).  Two key enzyme families, Ub ligases and deubiquitylation enzymes (DUBs), are responsible for putting on and taking off … Read more

A Deeper Dive into a Peptide POOL

March 14, 2019

Artificial intelligence (AI) and machine learning are making a large impact on drug discovery and development.  It’s hard to open a copy of C&E News without reading about the latest AI-guided synthetic routes or “smart” models of drug metabolism and … Read more

Grip it & RiPP it

February 11, 2019

Azol(in)es, are important and common motifs in natural products and therapeutics. They are especially abundant in ribosomally synthesized and post-translationally modified peptide natural products (RiPPs) like cyanobactins and thiopeptides and even define an entire subclass of RiPPs dubbed “linear azole-containing … Read more

AMPs Making Noise as Antimalarials

January 4, 2019

This week, the lab has been reading about peptide therapeutics for malaria. Malaria is yet another infectious disease seeing a sharp rise in multi-drug resistant cases in recent years. Artemisinin and artemisinin combination therapies (ACTs) are the “go-to” treatment options … Read more

RaPID Redesigned

December 12, 2018

We’ve previously touched on DELs and some of what they’re doing to revolutionize drug discovery.  mRNA display is a somewhat similar technique that is increasingly being used to discover new high affinity peptide-based ligands for challenging therapeutic targets.  mRNA display … Read more

Re-Arming Arylomycins

November 30, 2018

Recently we delved into the literature on new and improved arylomycin antibiotics, in particular, this recent report in Nature by researchers at Genentech. Arylomycins are a class of macrocyclic peptides known to inhibit the bacterial type I signal peptidase pathway … Read more

Escaping the Endosome

August 31, 2018

Our lab loves peptides and drug discovery has recently been flooded with an interest in them. Peptides can be easy and cost efficient to make and there is an increasing number of techniques for identifying peptides that have a high … Read more

A DEL of a Good Paper

July 13, 2018

DNA-encoded libraries (DELs) have been making a big splash in drug discovery recently. Although the original idea dates back to 1992, DELs seem now to be surpassing traditional high-throughput screening approaches in terms of cost, scale, and speed and promise … Read more

The Lure of Fungal RiPPs

June 30, 2018

Fungi have always been an important source of biologically active natural products.  The modern age of antibiotics was ushered in by the discovery of penicillin, isolated from molds of Penicillium.  Since then, many blockbuster drugs have been fully or partially … Read more

Thinking About Piperazic Acid-Containing Natural Products

June 8, 2018

We’ve been reading the recent work of the Del Valle lab at USF and reflecting on the intriguing chemistry of what they call N-amino peptides (NAPs).  The unique structural and electronic features of NAPs make them potentially useful as peptidomimetics … Read more