Pharmacology and Toxicology

FSH-blocking therapeutic for osteoporosis

1. Sakshi Gera
2. Tan-Chun Kuo
3. Anisa Azatovna Gumerova
4. Funda Korkmaz
5. Damini Sant
6. Victoria DeMambro
7. Karthyayani Sudha
8. Ashley Padilla
9. Geoffrey Prevot
10. Jazz Munitz
11. Abraham Teunissen
12. Mandy MT van Leent
13. Tomas GJM Post
14. Jessica C Fernandes
15. Jessica Netto
16. Farhath Sultana
17. Eleanor Shelly
18. Satish Rojekar
19. Pushkar Kumar
20. Liam Cullen
21. Jiya Chatterjee
22. Anusha Pallapati
23. Sari Miyashita
24. Hasni Kannangara
25. Megha Bhongade
26. Puja Sengupta
27. Kseniia Ievleva
28. Valeriia Muradova
29. Rogerio Batista
30. Cemre Robinson
31. Anne Macdonald
32. Susan Hutchison
33. Mansi Saxena
34. Marcia Meseck
35. John Caminis
36. Jameel Iqbal
37. Maria I New
38. Vitaly Ryu
39. Se-Min Kim
40. Jay J Cao
41. Neeha Zaidi
42. Zahi A Fayad
43. Daria Lizneva
44. Clifford J Rosen
45. Tony Yuen
46. Mone Zaidi

• Curated by eLife

  Evaluation Summary:

  The authors describe a comprehensive characterization of a new humanized FSH blocking antibody (MS-Hu6), which they have studied in-depth in terms of its efficacy on bone and fat tissues. They provide compelling data on mouse and monkey species with a complete evaluation of its pharmacokinetics and biodistribution and characterize its effect for the treatment of obesity and bone loss. It is an important contribution and will be useful to a general readership in endocrinology, bone and fat metabolism.

  (This preprint has been reviewed by eLife. We include the public reviews from the reviewers here; the authors also receive private feedback with suggested changes to the manuscript. The reviewers remained anonymous to the authors.)

Reviewed by eLife

Targeting neutrophils extracellular traps (NETs) reduces multiple organ injury in a COVID-19 mouse model

1. Flavio P. Veras
2. Giovanni F. Gomes
3. Bruna M. S. Silva
4. Diego B. Caetité
5. Cicero J. L. R. Almeida
6. Camila Meirelles S. Silva
7. Ayda H. Schneider
8. Emily S. Corneo
9. Caio S. Bonilha
10. Sabrina S. Batah
11. Ronaldo Martins
12. Eurico Arruda
13. Alexandre T. Fabro
14. José C. Alves-Filho
15. Thiago M. Cunha
16. Fernando Q. Cunha

Reviewed by Rapid Reviews Infectious Diseases, ScreenIT

Methylene Blue Is a Nonspecific Protein–Protein Interaction Inhibitor with Potential for Repurposing as an Antiviral for COVID-19

1. Sung-Ting Chuang
2. Henrietta Papp
3. Anett Kuczmog
4. Rebecca Eells
5. Jose M. Condor Capcha
6. Lina A. Shehadeh
7. Ferenc Jakab
8. Peter Buchwald

Reviewed by ScreenIT

Robust and durable prophylactic protection conferred by RNA interference in preclinical models of SARS-CoV-2

1. Yesseinia I. Anglero-Rodriguez
2. Florian A. Lempp
3. James McIninch
4. Mark K. Schlegel
5. Christopher R. Brown
6. Donald J. Foster
7. Adam B. Castoreno
8. Tuyen Nguyen
9. Megha Subramanian
10. Martin Montiel-Ruiz
11. Hannah Kaiser
12. Anna Sahakyan
13. Roberto Spreafico
14. Svetlana Shulga Morskaya
15. Joseph D. Barry
16. Daniel Berman
17. Stephanie Lefebvre
18. Anne Kasper
19. Timothy Racie
20. Diann Weddle
21. Melissa Mobley
22. Arlin Rogers
23. Joseph Dybowski
24. Saeho Chong
25. Jayaprakash Nair
26. Amy Simon
27. Kevin Sloan
28. Seungmin Hwang
29. Herbert W. Virgin
30. Kevin Fitzgerald
31. Martin A. Maier
32. Gregory Hinkle
33. Christy M. Hebner
34. Akin Akinc
35. Vasant Jadhav

Reviewed by ScreenIT

Differential Activity of Repurposed Drugs as Receptor Binding Domain Antagonists for Omicron and Native Strains of SarsCov2

1. Kranti Meher
2. Saranya K
3. Arpitha Reddy
4. Gopi Kadiyala
5. Subra Iyer
6. Subhramanyam Vangala
7. Satish Chandran
8. Uday Saxena

Reviewed by ScreenIT

Lack of antiviral activity of probenecid in Vero E6 cells and Syrian golden hamsters: a need for better understanding of inter-lab differences in preclinical assays

1. Helen Box
2. Shaun H Pennington
3. Edyta Kijak
4. Lee Tatham
5. Claire H Caygill
6. Rose C Lopeman
7. Laura N Jeffreys
8. Joanne Herriott
9. Joanne Sharp
10. Megan Neary
11. Anthony Valentijn
12. Henry Pertinez
13. Paul Curley
14. Usman Arshad
15. Rajith KR Rajoli
16. Steve Rannard
17. James P. Stewart
18. Giancarlo A Biagini
19. Andrew Owen

Reviewed by ScreenIT

Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs

1. Charlotte Avet
2. Arturo Mancini
3. Billy Breton
4. Christian Le Gouill
5. Alexander S Hauser
6. Claire Normand
7. Hiroyuki Kobayashi
8. Florence Gross
9. Mireille Hogue
10. Viktoriya Lukasheva
11. Stéphane St-Onge
12. Marilyn Carrier
13. Madeleine Héroux
14. Sandra Morissette
15. Eric B Fauman
16. Jean-Philippe Fortin
17. Stephan Schann
18. Xavier Leroy
19. David E Gloriam
20. Michel Bouvier

• Curated by eLife

  Evaluation Summary:

  A challenge to understanding the physiology and therapeutic potential of G protein-coupled receptors (GPCRs) is to understand the range of their couplings to different G proteins. Avet et al developed of a novel set of biosensors to assess the coupling specificity of 100 therapeutically relevant G protein-coupled receptors (GPCRs) to various G protein isoforms and arrestins. The novel screen and results obtained with reference ligands will have broad use for researchers studying GPCRs, potentially impacting discovery of new physiological pathways, understanding adverse effects of currently marketed therapeutics, and discovery of novel, safer therapeutics.

  (This preprint has been reviewed by eLife. We include the public reviews from the reviewers here; the authors also receive private feedback with suggested changes to the manuscript. Reviewer #1 agreed to share their name with the authors.)

Reviewed by eLife

Common coupling map advances GPCR-G protein selectivity

1. Alexander S Hauser
2. Charlotte Avet
3. Claire Normand
4. Arturo Mancini
5. Asuka Inoue
6. Michel Bouvier
7. David E Gloriam

• Curated by eLife

  Evaluation Summary:

  This study is a meta-analysis of previously reported studies on G protein-coupled receptor (GPCR) coupling to G proteins. Three separate data sets that describe the coupling of members of the superfamily of non-sensory GPCRs (~200 genes) to the large family of G protein alpha subunits (~20 genes). The authors try to arrive at a consensus for receptor-G protein coupling from the three data sets, as well as identify and highlight differences or incongruencies. Compiling these vast data sets into a unified format will be extremely useful for investigators to understand receptor and effector relationships. The meta-analysis will help to deconvolute the complex physiology and pharmacology underlying hormone or drug actions acting on receptor superfamilies.

  (This preprint has been reviewed by eLife. We include the public reviews from the reviewers here; the authors also receive private feedback with suggested changes to the manuscript. The reviewers remained anonymous to the authors.)

Reviewed by eLife

In vitro effect of a non-immunosuppressive FKBP ligand, FK1706, on SARS-CoV-2 replication in combination with antivirals

1. William E. Fitzsimmons
2. Tracy L. Hartman
3. Michelle Mendenhall
4. Catherine Z. Chen

Reviewed by ScreenIT

Preclinical Pharmacokinetics and In Vitro Properties of GS-441524, A Potential Oral Drug Candidate for COVID-19 Treatment

1. Amy Q. Wang
2. Natalie R. Hagen
3. Elias C. Padilha
4. Mengbi Yang
5. Pranav Shah
6. Catherine Z. Chen
7. Wenwei Huang
8. Pramod Terse
9. Philip Sanderson
10. Wei Zheng
11. Xin Xu

Reviewed by ScreenIT