Dark Matter Blog

Drug-Likeness and RNA-Targeted Small Molecules

March 13th, 2018
by Thomas Hermann
Associate Professor of Chemistry and Biochemistry at University of California, San Diego and Co-Director, UCSD Center for Drug Discovery Innovation

Only a minuscule fraction of the human genome is devoted to encoding proteins, yet proteins provide nearly 100% of the targets for currently marketed drugs. The few exceptions include antisense and RNAi oligonucleotides, some DNA-binding cancer therapeutics such as doxorubicin and cisplatin, and a chemically diverse group of antibiotics that interfere with bacterial protein biosynthesis […]

RNA Dynamics – A Bug or a Feature?

February 14th, 2018
by Donovan Chin
Director of Computational Drug Discovery, Arrakis

Though not nearly as famous as its double-stranded cousin, RNA is a fascinating molecule and its potential as a drug discovery substrate continues to unfold beyond merely transferring information from DNA into proteins. To perform its role in the cell, RNA must move, contort and adapt to a wide range of functional and regulatory requirements. […]

The prospect of RNA targeting using small molecules

December 13th, 2017
by David Chenoweth, PhD
Associate Professor, Department of Chemistry University of Pennsylvania

Small molecules that bind to macromolecular nucleic acids are well known. Before the 1960s, dyes such as aminoacridines, were utilized by histologists and biologists to image specific sub-nuclear structures.1 This was perhaps the earliest recognition that small molecules can bind macromolecular nucleic acids. In 1961, the first nucleic acid-small molecule binding hypothesis (the “intercalator hypothesis”) […]

Why NOW for Targeting RNA with Small Molecules?

November 28th, 2017
by Russ Petter, PhD
Founder and CSO, Arrakis

In “The Right Stuff,” Tom Wolfe noted that astronauts were granted hero status before their missions, perhaps because no one expected them to return. Happily, Arrakis also has received a lot of laudatory attention just for launching the mission of drugging RNAs with small molecules – before we’ve even achieved it. The plaudits are lovely, […]

RNA State of Mind

October 25th, 2017
by Neil Kubica, PhD
Director of RNA Biology, Arrakis

Perspectives from the ‘Targeting RNA Using Small Molecules’ meeting @NYASciences #rSMs  Our team at Arrakis Therapeutics recently had the pleasure to co-sponsor the ‘Targeting RNA Using Small Molecules’ symposium at the New York Academy of Sciences. While several conference sessions over the years have focused on our favorite topic, including the (in)famous Gordon Conference that […]

Drugging the Undruggable: Transcription Factors

July 12th, 2017
by James Barsoum, PhD
Senior Vice President of Biology, Arrakis

As we battle to expand the reach of modern therapeutics to treat diseases with high unmet need, we confront the limitations in our armamentarium. Most often we are limited by biology – we don’t understand the molecular drivers of disease and consequently don’t know which targets to aim at. But the more frustrating situation is […]

Discovering a New World of RNA-Targeted Medicines

February 27th, 2017
by Michael Gilman, PhD
CEO, Arrakis

So here we are. Nearly two years in the making, much of it focused, fastidious work by founder Russ Petter (of whom much more below), capped by an exhilarating and exhausting sprint to the finish by an outstanding team, Arrakis Therapeutics has now lifted off. Today we announced a $38M Series A financing led by […]

Escaping the Gravitational Pull of “Druggability”

February 22nd, 2017
by Michael Gilman, PhD
CEO, Arrakis

Most old-timers in drug discovery will agree on one thing: It never gets easier. Sure, maybe we learn a little from our mistakes along the way and the toolkit gets steadily flashier. But the easy targets, if ever they were truly easy ones, are long gone. We are left with either inscrutable biology or, even […]

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