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Science

A third of the human proteome never folds into a fixed structure. Its biology, and much of human disease, lives in that motion. Peptone is built to read it, model it, and drug it.

Intrinsically disordered proteins

Most medicines are designed against proteins that hold a fixed shape. Much of what drives human disease never does.

For a century, biology has read a straight line from sequence to structure to function: a chain of amino acids folds into one shape, and that shape does the work. It holds for a large part of the proteome and breaks for the rest. Roughly a third of the residues in the human proteome never fold into a stable structure, and most human proteins carry at least one disordered region. These intrinsically disordered proteins are not broken or unfinished. They do their job precisely because they stay in motion.

How common intrinsic disorder is in the human proteomeTwo horizontal proportion bars on a shared zero to one hundred percent axis. About a third, thirty-three percent, of human proteome residues never fold into a stable structure, and about sixty percent of human proteins carry a disordered region. Each highlighted bar length encodes its percentage from the origin.Human proteome residues33%Never foldFold into a stable structureHuman proteins60%Carry a disordered regionFully structured

Prevalence of intrinsic disorder in the human proteome. About 33% of all residues are predicted never to fold into a stable structure, and close to 60% of human proteins carry at least one disordered region of 30 residues or more. Estimates from PritiĊĦanac et al., A Functional Map of the Human Intrinsically Disordered Proteome (2024).

A folded protein holds one shape. A disordered one does not.

A folded protein settles into a single cooperative structure and presents a stable pocket, the kind of feature a drug can be designed to fit. An intrinsically disordered protein has a defined sequence but no single folded form. It moves continuously through a broad ensemble of interconverting conformations, and that flexibility is the mechanism rather than a defect in it. For these proteins the ensemble is the molecule. A single snapshot does not describe them, and can be actively misleading.

A folded protein holds one shape, a disordered protein does notTwo panels for the same length of polypeptide chain. On the left, a folded protein as a three-dimensional ribbon cartoon: coiled helices, arrow beta strands, and loops packed into one compact domain with a small molecule bound in a single defined pocket. On the right, an intrinsically disordered protein drawn as an overlay of many superimposed backbone conformations that keep interconverting, with no fixed structure and no single pocket.NCFolded proteinOne structure, one pocketNCDisordered proteinAn ensemble of states
Where disease begins

Disorder runs the control points of biology

Disordered regions concentrate at the busiest junctions of the cell: the transcription factors that decide which genes switch on, the signaling proteins that relay messages, and the membraneless condensates that organize the cell interior. Because these roles are central, their failure is severe. Trace many of the most stubborn diseases to their molecular origin and a disordered protein is often waiting there. That same biology defines where we work: oncology, CNS, immunology and inflammation, and longevity.

Transcription factorsp53c-MycAR N-terminal domainEWS-FLI1HIF-1ÎħSignaling hubsp27 Kip14E-BP1BADβ-cateninMembraneless condensatesFUSTDP-43hnRNPA1G3BP1TAF15Where dysregulation drives diseaseOncologyCNSImmunology & inflammationLongevityTranscription factorsp53c-MycAR N-terminal domainEWS-FLI1HIF-1ÎħSignaling hubsp27 Kip14E-BP1BADβ-cateninMembraneless condensatesFUSTDP-43hnRNPA1G3BP1TAF15Where dysregulationdrives diseaseOncologyCNSImmunology & inflammationLongevity
Each tile = 1% of the archive ≈ 2,500 structuresProtein Data Bank · 2026≈250,000experimentally solved structuresX-ray & cryo-EM≈94% · needs a folded structureSolution NMR + SAXS≈6% · the only window onto disorderProtein Data Bank · 2026≈250,000experimentally solved structuresEach tile = 1% of the archive ≈ 2,500 structuresX-ray & cryo-EM≈94% · needs a folded structureSolution NMR + SAXS≈6% · the only window onto disorder

Left out of the structural record

Structural biology was built around methods that need a static, cooperative subject. X-ray crystallography and cryo-electron microscopy resolve a well-ordered structure beautifully and a moving ensemble poorly, so disordered proteins were systematically excluded from the Protein Data Bank. Only a few techniques could observe them in solution at all, chief among them nuclear magnetic resonance, supported by small-angle X-ray scattering. With little to see and less to design against, most of the disordered proteome was set aside as undruggable.

Archive coverage is schematic. Structure counts and methods: RCSB Protein Data Bank.

Frontier AI inherits the gap

The prediction models that reshaped structural biology, from AlphaFold2 and AlphaFold3 to open successors such as OpenFold, Chai-1, and Boltz, all learned from that same archive. Given a sequence they return a single confident, static structure. Ask one for a disordered target, such as the androgen receptor N-terminal domain, and it returns a crisp, convincing shape that the protein never actually holds. The models even flag the problem themselves: their per-residue confidence collapses across the disordered regions, marking the residues that matter most as the least reliable. More data of the same kind does not close the gap.

AlphaFold prediction of the androgen receptorA three-dimensional ribbon model based on the AlphaFold structure AF-P10275. A compact folded core of coiled helices is coloured in high-confidence AlphaFold blues; a large disordered N-terminal domain sprawls around it as a halo of low-to-very-low-confidence orange loops. Pointers explain that the disordered region scores very low confidence because the model has no experimental structures of it to learn from.Model confidence (pLDDT)Very lowConfidentVery highNCFolded domainHigh confidence · pLDDT > 90Disordered N-terminal domainVery low confidence · pLDDT < 50The model is guessingNo experimental structure of thisregion exists to learn from, so itinvents a shape it never holds.AlphaFold prediction of the androgen receptorA three-dimensional ribbon model based on AlphaFold AF-P10275: a high-confidence folded core in blue surrounded by a large disordered N-terminal domain drawn as orange loops, with numbered notes explaining the very low confidence over the disordered region.Model confidence (pLDDT)Very lowConfidentVery highNC1231Folded domainHigh confidence · pLDDT > 902Disordered N-terminal domainVery low confidence · pLDDT < 503The model is guessingNo experimental structure exists to learnfrom, so it invents a shape it never holds.

Based on the AlphaFold prediction (AF-P10275) of the androgen receptor; colouring follows the pLDDT model-confidence scale.

The Peptone approach

We steer the physics with measurement

Because the data does not exist in public archives, we generate it. Peptone reads a target where it actually lives, in solution and in motion, using hydrogen-deuterium exchange mass spectrometry together with magnetic and paramagnetic resonance spectroscopy, including NMR, PRE, and EPR. These experiments are sparse by design and decisive in effect. A small number of well-chosen restraints steer simulation and generative models away from plausible fiction and toward physical reality, collapsing billions of candidate conformations down to the thermodynamically sensible states a protein truly populates.

Sparse experimental restraints steer a broad ensemble into a few statesA broad conformational cloud on the left funnels through a gate of sparse experimental restraints, hydrogen-deuterium exchange mass spectrometry and magnetic and paramagnetic resonance, and resolves into a few thermodynamically sensible states on the right.Broad ensembleSparse measurementResolved statesNCBillions of conformationsHDX-MSNMRPRE / EPRSparse, decisive dataThermodynamically sensibleSparse experimental restraints steer a broad ensemble into a few statesA broad conformational cloud funnels through a gate of sparse experimental restraints, hydrogen-deuterium exchange mass spectrometry and magnetic and paramagnetic resonance, and resolves into a few thermodynamically sensible states.Broad ensembleNCBillions of conformationsSparse measurementHDX-MSNMRPRE / EPRSparse, decisive dataResolved statesThermodynamically sensible

Proof: a rare state made visible

The payoff is a state that no single structure would ever show. Applying multithermal enhanced sampling to ACTR, a well-characterized disordered protein, resolved a rare conformation populated only about three percent of the time: transiently folded, reached across a modest barrier of roughly 13 kilojoules per mole, and competent to bind. The computed ensemble agreed with independent NMR and SAXS measurements. A binding-competent pocket that appears in none of the protein's average structures becomes a defined, addressable target. This is how sparse experiment redirects frontier methods and drives them quickly to physically relevant answers.

A free-energy profile along a conformational coordinate. A broad, deep well holds the extended disordered ground state, most of the ensemble. A modest barrier of about 13 kilojoules per mole separates it from a shallow well holding a rare, compact, bound-like conformation, about three percent of the ensemble, in which helices pack together and a binding-competent pocket opens. Both conformers are the same protein.ACTR apo ensembleOne protein, two conformationsConformational coordinateFree energyA modest barrier~13 kJ/mol, so the fold stays reachableNCDisordered ground stateExtended · ~97% of the ensembleNCRare folded stateCompact · ~3%, a pocket opensEnsemble consistent with NMR + SAXSThe same protein in two conformations: an extended disordered ground state that is most of the ensemble, and a rare compact bound-like state, about three percent, in which helices pack together and a binding-competent pocket opens, separated by a modest barrier of about 13 kilojoules per mole.ACTR · one protein, two statesDisordered ground stateExtended · ~97% of the ensembleA modest barrier~13 kJ/mol, easily crossedRare folded stateCompact · ~3%, a pocket opensEnsemble consistent with NMR + SAXS

Atomistic ensembles of ACTR were generated with multithermal enhanced sampling (On-the-fly Probability Enhanced Sampling, OPES), then reweighted against NMR chemical shifts and paramagnetic relaxation enhancements and independently cross-validated with residual dipolar couplings and small-angle X-ray scattering (SAXS). The reweighted ensemble resolves a rare, bound-like state (about 3%) in which the binding helices pack together, invisible to any single average structure. Streit, Invernizzi, Bottaro, Tamiola and Lindorff-Larsen, Nature Communications 17, 5558 (2026).

Every step serves one purpose

None of this is method for its own sake. Reading real biophysics instead of confident artifacts tightens every design, measure, and decide cycle, and each turn of the loop sharpens the next. The purpose is singular: to generate drugs that stand the scrutiny of clinical trials, against targets that structure-first discovery leaves untouched.

A design, measure and decide loop advances to a candidate, the clinic, and a medicineA tight design, measure and decide loop produces evidence that advances along a rising track through a candidate and clinical trials to a small-molecule medicine that stands the scrutiny of the clinic.From data to the drugEvidenceDesignMeasureDecideEach turn sharpens the nextCandidateDesigned against real statesClinical trialsStands the scrutinyA medicineThe singular purposeA design, measure and decide loop advances to a candidate, the clinic, and a medicineA tight design, measure and decide loop produces evidence that advances down through a candidate and clinical trials to a small-molecule medicine that stands the scrutiny of the clinic.From data to the drugEvidenceDesignMeasureDecideCandidateDesigned against real statesClinical trialsStands the scrutinyA medicineThe singular purpose