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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.
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.
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.
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.
This industry-linked evaluation examined 30 samples from Amgen process and medicinal chemistry groups. Fifteen crystal structures were elucidated using 40 hours of microscope time. For the chiral compounds whose structures were solved, dynamical refinement assigned the correct absolute stereochemistry. The study provides an observed sample-set outcome rather than a universal success rate for pharmaceutical materials.
Researchers used MicroED to determine the crystal structures of ranitidine hydrochloride Forms 1 and 2. The resulting structures agreed with previously reported X-ray diffraction structures. The work presents a focused pharmaceutical proof of applicability for small-quantity or microcrystalline API samples, while retaining the need to control crystal form, hydration, and residual solvents through complementary quality assessments.
This community overview summarizes developments discussed at a MicroED symposium and workshop. It covers access to instrumentation, small-molecule and biomolecular applications, data collection, processing software, reporting, and validation. For pharmaceutical readers, it helps connect individual experimental demonstrations to the operational requirements of a complete workflow, without presenting an industrial validation study.
Researchers determined two polymorphic crystal structures of the oral macrocyclic drug paritaprevir within the same MicroED experiment. The forms differed in macrocycle and substituent conformations. Docking suggested that one conformation could fit the viral protease binding pocket. The structural and computational results inform conformational analysis but do not establish a difference in clinical performance between polymorphs.
An automated low-dose 3D electron diffraction workflow identified six phases in a melt-crystallized griseofulvin–polyethylene glycol system. More than 230 datasets were collected and processed in three days. The researchers resolved known drug polymorphs and inclusion complexes alongside an elusive new inclusion-complex phase, then related the two inclusion-complex polymorphs to their structural stability differences.
A randomized phase 2 study evaluated oral JNJ-77242113, an IL-23 receptor antagonist peptide, against placebo for 16 weeks in plaque psoriasis. The study reported a dose-response relationship for skin improvement. This is candidate-specific human evidence; it does not establish oral bioavailability or clinical success for other cyclic peptides.
The review describes MicroED methodology and recent advances across small organic molecules, materials, and biological structures. It explains how diffraction from very small crystals extends the experimental toolkit. Pharmaceutical readers can use it for broader methodological context, while recognizing that its cross-disciplinary examples do not constitute a dedicated benchmark of routine API polymorph screening.
MicroED analysis of mirabegron nanocrystals revealed two molecular conformers within the asymmetric unit and a hydrogen-bonded packing arrangement. The authors compared these solid-state conformations with a previously reported receptor-bound model and discussed differences. The two conformers are not, by themselves, evidence of two separate polymorphs; the study concerns molecular conformation within the observed crystal structure.
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