The 11th edition of Harrison's Principles of Internal Medicine welcomes Anthony Fauci to its editorial staff, in addition to more than 85 new contributors. While the organization of the book is similar to previous editions, major emphasis has been placed on disorders that affect multiple organ systems. Important advances in genetics, immunology, and oncology are emphasized. Many chapters of the book have been rewritten and describe major advances in internal medicine. Subjects that received only a paragraph or two of attention in previous editions are now covered in entire chapters. Among the chapters that have been extensively revised are the chapters on infections in the compromised host, on skin rashes in infections, on many of the viral infections, including cytomegalovirus and Epstein-Barr virus, on sexually transmitted diseases, on diabetes mellitus, on disorders of bone and mineral metabolism, and on lymphadenopathy and splenomegaly. The major revisions in these chapters and many

Harrison's Principles of Internal Medicine

Chemistries that Facilitate Nanotechnology Kim E. Sapsford,† W. Russ Algar, Lorenzo Berti, Kelly Boeneman Gemmill,‡ Brendan J. Casey,† Eunkeu Oh, Michael H. Stewart, and Igor L. Medintz*,‡ †Division of Biology, Department of Chemistry and Materials Science, Office of Science and Engineering Laboratories, U.S. Food and Drug Administration, Silver Spring, Maryland 20993, United States ‡Center for Bio/Molecular Science and Engineering Code 6900 and Division of Optical Sciences Code 5611, U.S. Naval Research Laboratory, Washington, D.C. 20375, United States College of Science, George Mason University, 4400 University Drive, Fairfax, Virginia 22030, United States Department of Biochemistry and Molecular Medicine, University of California, Davis, School of Medicine, Sacramento, California 95817, United States Sotera Defense Solutions, Crofton, Maryland 21114, United States

Functionalizing nanoparticles with biological molecules: developing chemistries that facilitate nanotechnology.

The copper(I)-catalyzed 1,2,3-triazole-forming reaction between azides and terminal alkynes has become the gold standard of 'click chemistry' due to its reliability, specificity, and biocompatibility. Applications of click chemistry are increasingly found in all aspects of drug discovery; they range from lead finding through combinatorial chemistry and target-templated in vitro chemistry, to proteomics and DNA research by using bioconjugation reactions. The triazole products are more than just passive linkers; they readily associate with biological targets, through hydrogen-bonding and dipole interactions. The present review will focus mainly on the recent literature for applications of this reaction in the field of medicinal chemistry, in particular on use of the 1,2,3-triazole moiety as pharmacophore.

https://onlinelibrary.wiley.com/doi/pdf/10.1002/asia.201100432

Click Chemistry: 1,2,3‐Triazoles as Pharmacophores

http://pubs.acs.org/doi/pdf/10.1021/cr400460s

Metallodrugs in Medicinal Inorganic Chemistry

Background Metastatic castration-resistant prostate cancer remains fatal despite recent advances. Prostate-specific membrane antigen (PSMA) is highly expressed in metastatic castration-res...

https://www.nejm.org/doi/suppl/10.1056/NEJMoa2107322/suppl_file/nejmoa2107322_appendix.pdf

Lutetium-177-PSMA-617 for Metastatic Castration-Resistant Prostate Cancer.

Evolution of Tc-99m in diagnostic radiopharmaceuticals

Lutetium-177 therapeutic radiopharmaceuticals: linking chemistry, radiochemistry, and practical applications.

A double zwitterionic Schiff base was synthesized using the amino acid l-histidine and o-vanillin (2-hydroxy-3-methoxy benzaldehyde). Both the phenol and carboxyl groups are deprotonated, and the imine nitrogen atom and histidine-imidazole ring are protonated to give the double zwitterion with an intramolecular (imine)N−H+···−O(phenol) hydrogen bond (ketoamine form). Such a ketoamine form in a double zwitterion is assumed in the catalytic cycle of enzymatic transformations of amino acids with the cofactor (vitamin B6) pyridoxal-5′-phosphate (PLP). A high-resolution, low-temperature, single-crystal X-ray diffraction data set on N-o-vanillylidene-l-histidine (also named 3-methoxysalicylidene-l-histidine or N-(2-oxy-3-methoxy-benzylidene)-l-histidine, OVHIS) is used in the analysis of molecular electrostatic properties and intermolecular interactions. All oxygen atoms in the molecule (four in total) are mutually almost coplanar and located (externally) on the same side of molecule. These four O atoms carry s...

N-o-Vanillylidene-L-histidine: Experimental Charge Density Analysis of a Double Zwitterionic Amino Acid Schiff-Base Compound

177Lu-labeled cyclic polyaminophosphonates as potential agents for bone pain palliation.

Designing ideal radiopharmaceuticals for use as bone pain palliatives require the use of a moderate energy β− emitter as a radionuclide and a suitable polyaminophosphonic acid as a carrier molecule. Owing to its suitable decay characteristics [T1/2 = 6.73 d, Eβ(max) = 497 keV, Eγ = 113 keV (6.4%), 208 keV (11%)] as well as the feasibility of large-scale production in adequate specific activity and radionuclidic purity using a moderate flux reactor, 177Lu could be considered as a promising radionuclide for palliative care in painful bone metastasis. The present study was therefore, oriented toward the preparation and biologic evaluation of 177Lu complex of ethylenediaminetetramethylene phosphonic acid (EDTMP) in various animal models, with an aim to prepare a viable radiopharmaceutical for bone pain palliation. 177Lu was produced with a specific activity of ∼12 GBq/mg (∼324 mCi/mg) and radionuclidic purity of 99.98% by irradiation of natural Lu2O3 targeted at a thermal neutron flux of ∼6 × 1013 n/cm2.s for...

Sharmila Banerjee

Papers

Evolution of Tc-99m in diagnostic radiopharmaceuticals

Lutetium-177 therapeutic radiopharmaceuticals: linking chemistry, radiochemistry, and practical applications.

N-o-Vanillylidene-L-histidine: Experimental Charge Density Analysis of a Double Zwitterionic Amino Acid Schiff-Base Compound

177Lu-labeled cyclic polyaminophosphonates as potential agents for bone pain palliation.

177Lu-EDTMP: a viable bone pain palliative in skeletal metastasis.