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RESEARCH / LITERATURE

Research Literature

Find research, methods, and reviews across our scientific fields.

One collection · Original publication dates · Authors, journals & DOIs

All publications 136

Duplicate DOIs are merged. This is a selected collection, not an exhaustive bibliography.

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Methods
IUCrJ

High-throughput automated molecular replacement for small-molecule MicroED data

Adam Thibodeaux; Guanhong Bu; Lael C. Edwards; Emma Rova Danelius

An automated molecular-replacement workflow solved the electron-diffraction structure of corilagin, a macrocyclic gallotannin that resisted ab initio phasing. Validation used known paritaprevir and grazoprevir structures across several resolution cutoffs. The results suggest an alternative route for flexible or lower-quality small-molecule datasets, with the important condition that chemically appropriate trial conformations must be available.

MicroED structure determination
Read guide →Original paper ↗

DOI: 10.1107/s2052252526002095

Methods
Communications Chemistry

An integrated workflow for the structure elucidation of nanocrystalline powders

Chiara Sabena; Federica Bravetti; Natsuki Miyauchi; Miho Nakafukasako; Yoshitaka Aoyama; Katsuo Asakura; Kiyotaka Konuma; Masahiro Hashimoto; Yusuke Nishiyama; Michele R. Chierotti

An integrated workflow combined MicroED with high-resolution mass spectrometry, database searches, solution and solid-state NMR, and computational calculations. Demonstrations used a pyridoxine–N-acetyl-L-cysteine salt and the peptide fMLF. The approach addressed molecular identity, crystal packing, light-atom assignment, and hydrogen positions, illustrating how complementary measurements can resolve ambiguities that electron diffraction alone may leave in nanocrystalline powders.

MicroED structure determination
Read guide →Original paper ↗

DOI: 10.1038/s42004-026-01902-1

Original research
Small

Rapid Structural Analysis of Natural Products Using MicroED

Jieye Lin; Orel Paz; Johan Unge; Tamir Gonen

Researchers reported MicroED structures for nine chemically diverse natural products whose three-dimensional structures had remained unavailable. The work used microgram quantities and avoided the need to grow large single crystals. It supports MicroED as a practical route for difficult natural-product samples, although the selected examples do not define a universal success rate across all natural products.

MicroED structure determination
Read guide →Original paper ↗

DOI: 10.1002/smll.202511875

Original research
Communications Chemistry

Predicting the ritonavir crisis by revisiting the polymorph landscape with crystal structure prediction and form 4 structure solution

Luca Iuzzolino; Andrew W. Kelly; Mohammad T. Chaudhry; Cristian Jandl; Danny Stam; Alfred Y. Lee

Revisiting ritonavir’s polymorph landscape, the authors examined whether crystal structure prediction could have flagged the risk posed by the less soluble Form 2. They also solved the previously unresolved Form 4 structure using 3D electron diffraction, modeling, and powder X-ray diffraction, finding disorder and thermodynamic instability. The retrospective analysis informs risk assessment rather than guaranteeing future polymorph prediction.

MicroED structure determinationPharmaceutical solid state
Read guide →Original paper ↗

DOI: 10.1038/s42004-025-01814-6

Original research
ChemMedChem

Discovery of Oxyacanthine Dihydrochloride Monohydrate Polymorphs from Obfuscated Samples by Microcrystal Electron Diffraction

Jieye Lin; Orel Paz; Johan Unge; Tamir Gonen

MicroED identified two polymorphic structures of oxyacanthine dihydrochloride monohydrate in samples mislabeled as berbamine dihydrochloride. The forms differed principally in the conformation of a tetrahydroisoquinoline ring. Structural, energetic, and packing analyses suggested a thermodynamic preference between them. The study demonstrates how crystallographic analysis can expose both identity problems and polymorphism in complex natural-product samples.

MicroED structure determinationPharmaceutical solid state
Read guide →Original paper ↗

DOI: 10.1002/cmdc.202500601

Original research
Crystal Growth & Design

Crystal Structure Determination of Inseparable Polymorphic Mixtures by 3D ED/MicroED

Keiyo Nakai; Kuniyoshi Miki; Takashi Kikuchi; Hiroyasu Sato; Keigo Takahira; Robert Bücker; Akito Sasaki; Atsushi Kaga; Ryo Anzai; Mitsuhisa Yamano

3D ED/MicroED determined casopitant mesylate Forms 1 and 3 from one batch of fine powder containing an inseparable polymorphic mixture. Their structures differed through a small packing shift, explaining their very similar powder X-ray diffraction patterns. The work demonstrates how selecting individual microcrystals can resolve structurally similar phases that remain difficult to separate or distinguish in bulk measurements.

MicroED structure determinationPharmaceutical solid state
Read guide →Original paper ↗

DOI: 10.1021/acs.cgd.5c01477

Methods
Bioconjugate Chemistry

Synthesis of DNA-Encoded Bicyclic Peptides via Cysteine-Promoted Cyclization and Amide Condensation Reaction

Yi Gan; Yumei Zeng; Haojie Guan; Wenjun Li; Alex Shaginian; Jin Li; Sen Gao; Guansai Liu

HitGen researchers describe a method for synthesizing DNA-encoded bicyclic peptides using cysteine-promoted cyclization and amide condensation under mild conditions. The abstract reports compatibility with varied sequences and ring sizes. This is discovery-platform chemistry, not evidence that the resulting peptides have oral exposure, clinical efficacy, or validated manufacturing-scale performance.

China-listed CRO/CDMOOral cyclic peptides
Read guide →Original paper ↗

DOI: 10.1021/acs.bioconjchem.5c00455

Original research
Chemical and Pharmaceutical Bulletin

Combination of Microcrystal Electron Diffraction and Solid-State NMR for the Structural Determination of Indomethacin–Nicotinamide Co-crystals

Hidetomo Yokoo; Tatsuo Koide; Tamaki Miyazaki; Yoshitaka Aoyama; Yutaro Ogaeri; Eiichi Yamamoto; Yosuke Demizu; Nahoko Uchiyama

This study characterized indomethacin–nicotinamide cocrystals using MicroED together with solid-state NMR, Raman spectroscopy, and powder X-ray diffraction. MicroED supplied the crystal structure, while NMR helped examine molecular interactions. The combined approach addressed properties that individual methods could not establish alone, offering a pharmaceutical cocrystal workflow relevant to API powders and formulations containing excipients.

MicroED structure determinationPharmaceutical solid state
Read guide →Original paper ↗

DOI: 10.1248/cpb.c25-00377

Methods
Acta Crystallographica Section C

Standards for MicroED

Johan Unge; Brent L. Nannenga; Allen G. Oliver; Tamir Gonen

This standards article examines lessons from the growing body of refined MicroED structures and accessible diffraction data. It discusses quality indicators and proposes community best practices for assessing and reporting results. The recommendations provide a framework for critical evaluation rather than regulatory certification or a guarantee that every structure meets the same quality threshold.

MicroED structure determination
Read guide →Original paper ↗

DOI: 10.1107/s2053229625004875

Original research
New England Journal of Medicine

Vepdegestrant, a PROTAC Estrogen Receptor Degrader, in Advanced Breast Cancer

Mario Campone; Michelino De Laurentiis; Komal Jhaveri; Xichun Hu; Sylvain Ladoire; Anne Patsouris; Claudio Zamagni; Jiuwei Cui; Marina Cazzaniga; Timucin Cil; Katarzyna J Jerzak; Christian Fuentes; Tetsuhiro Yoshinami; Alvaro Rodriguez-Lescure; Ahmet Sezer; Andrea Fontana; Valentina Guarneri; Andrea Molckovsky; Marie-Ange Mouret-Reynier; Umut Demirci; Yongqiang Zhang; Olga Valota; Dongrui R Lu; Marcella Martignoni; Janaki Parameswaran; Xin Zhi; Erika P Hamilton

In the randomized phase 3 VERITAC-2 trial, vepdegestrant improved progression-free survival versus fulvestrant in the ESR1-mutated subgroup, but not significantly in the overall population. The trial enrolled 624 patients with previously treated ER-positive, HER2-negative advanced breast cancer. Grade 3 or higher adverse events occurred more often with vepdegestrant.

Protein degradation / PROTAC
Read guide →Original paper ↗

DOI: 10.1056/nejmoa2505725

Reviews & perspectives
Pharmacological Reviews

Pharmaceutical perspectives on oligonucleotide therapeutics and delivery systems

Dalton W Staller; Flobater I Gawargi; Sanjali S Panigrahi; Paras K Mishra; Ram I Mahato

This review examines RNA species, structure and function, chemical modifications, and delivery systems in the context of therapeutic development. It connects molecular design with stability and distribution and discusses clinical applications available at the time of writing. Its historical approval overview should not be interpreted as a current, exhaustive drug list.

Oligonucleotide Therapeutics & Delivery
Read guide →Original paper ↗

DOI: 10.1016/j.pharmr.2025.100065

Original research
Molecular Pharmaceutics

Structural Analysis of Active Pharmaceutical Ingredients in Tablets Using 3D ED/MicroED

Keiyo Nakai; Takashi Kikuchi; Kuniyoshi Miki; Akito Sasaki; Mitsuhisa Yamano

The study examined API crystals directly in Allegra, Clarith, and Ibrance tablets using selected-area 3D ED/MicroED. Fexofenadine hydrochloride Form I and clarithromycin Form II retained their polymorphs, while palbociclib Form A showed slight lattice shrinkage. The results demonstrate formulation-level structural analysis and emphasize that a lattice change and a new polymorph are different findings.

MicroED structure determinationPharmaceutical solid stateFormulation Development & Manufacturing
Read guide →Original paper ↗

DOI: 10.1021/acs.molpharmaceut.5c00028

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