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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 147

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

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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

Companies mentionedHitGen ↗
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
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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
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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
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DOI: 10.1021/acs.molpharmaceut.5c00028

Reviews & perspectives
Nature

Mass-spectrometry-based proteomics: from single cells to clinical applications

Tiannan Guo; Judith A Steen; Matthias Mann

This review surveys improvements in proteomics sample preparation, instrumentation, data acquisition, and analysis. It connects single-cell and spatial profiling with protein interactions, modifications, and biomarker discovery in body fluids. Clinical implementation is discussed as an opportunity with remaining challenges, rather than proof that every discovery assay is ready for diagnostic use.

Bioanalysis & Biomarkers
Read guide →Original paper ↗

DOI: 10.1038/s41586-025-08584-0

Original research
IUCrJ

SCXRD, CSP-NMRX and microED in the quest for three elusive polymorphs of meloxicam

Agata Jeziorna; Maura Malinska; Isaac Sugden; Piotr Paluch; Rafał Dolot; Marta K. Dudek

Three elusive meloxicam polymorphs required different structure-determination approaches. Single-crystal X-ray diffraction solved Form III, combined crystal structure prediction and NMR crystallography solved Form II, and electron diffraction resolved Form V, which contains four independent molecules in the asymmetric unit. The comparison highlights complementary strengths and limitations rather than establishing one universally superior crystallographic method.

MicroED structure determinationPharmaceutical solid state
Read guide →Original paper ↗

DOI: 10.1107/s2052252524011898

Original research
IUCrJ

From formulation to structure: 3D electron diffraction for the structure solution of a new indomethacin polymorph from an amorphous solid dispersion

Helen W. Leung; Royston C. B. Copley; Giulio I. Lampronti; Sarah J. Day; Lucy K. Saunders; Duncan N. Johnstone; Paul A. Midgley

3D electron diffraction resolved the structure of the ninth reported indomethacin polymorph, designated sigma, from crystals found within an amorphous solid dispersion. Subsequent experiments produced the same form by solvent evaporation. The work demonstrates structure determination directly from a formulation-related sample containing an excipient; it does not establish improved dissolution or clinical performance for the new form.

MicroED structure determinationPharmaceutical solid stateFormulation Development & Manufacturing
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DOI: 10.1107/s2052252524008121

Original research
Crystal Growth & Design

Polyethylene Glycol-Assisted Melt Crystallization of Two New Piroxicam Polymorphs Revealed by 3D Electron Diffraction

Jiaoyan Xu; Changlin Yao; Shufang Zhang; Xiaodong Zou; Yue Gui; Lei Wang; Hongyi Xu

Two previously unreported piroxicam polymorphs, Forms VIII and IX, emerged through polyethylene glycol-assisted melt crystallization. Their crystal structures were determined by 3D electron diffraction. Comparing the newly solved Form VIII with known Form IV allowed discussion of how differences in intermolecular hydrogen bonding contribute to melting behavior. The study concerns laboratory solid forms rather than validated drug-product performance.

MicroED structure determinationPharmaceutical solid state
Read guide →Original paper ↗

DOI: 10.1021/acs.cgd.4c00951

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